Tag: 600-700

Integration of multi-scale molecular modeling approaches with experiments for the in silico guided design and discovery of novel hERG-Neutral antihypertensive oxazalone and imidazolone derivatives and analysis of their potential restrictive effects on cell proliferation was written by Durdagi, Serdar;Aksoydan, Busecan;Erol, Ismail;Kantarcioglu, Isik;Ergun, Yavuz;Bulut, Gulay;Acar, Melih;Avsar, Timucin;Liapakis, George;Karageorgos, Vlasios;Salmas, Ramin E.;Sergi, Baris;Alkhatib, Sara;Turan, Gizem;Yigit, Berfu Nur;Cantasir, Kutay;Kurt, Bahar;Kilic, Turker. And the article was included in European Journal of Medicinal Chemistry in 2018.Name: 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate This article mentions the following:

AT1 antagonists is the most recent drug class of mols. against hypertension and they mediate their actions through blocking detrimental effects of angiotensin II (A-II) when acts on type I (AT1) A-II receptor. The effects of AT1 antagonists are not limited to cardiovascular diseases. AT1 receptor blockers may be used as potential anti-cancer agents – due to the inhibition of cell proliferation stimulated by A-II. Therefore, AT1 receptors and the A-II biosynthesis mechanisms are targets for the development of new synthetic drugs and therapeutic treatment of various cardiovascular and other diseases. Multi-scale mol. modeling approaches were performed and it is found that oxazolone and imidazolone derivatives reveal similar/better interaction energy profiles compared to the FDA approved sartan mols. at the binding site of the AT1 receptor. In silico-guided designed hit mols. were then synthesized and tested for their binding affinities to human AT1 receptor in radioligand binding studies, using [¹²⁵I-Sar¹-Ile⁸] AngII. Among the compounds tested, 19d (4′-((4-(4-bromobenzylidene)-2-butyl-5-oxo-4,5-dihydro-1H-imidazol-1-yl)methyl)[1,1′-biphenyl]-2-carbonitrile) and 9j (4-(2-bromobenzylidene)-2-butyl-1-((2′-(2-trityl-2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl)methyl)-1H-imidazol-5(4H)-one) mols. bound to receptor in a dose response manner and with relatively high affinities. Next, cytotoxicity and wound healing assays were performed for these hit mols. Since hit mol. 19d led to deceleration of cell motility in all three cell lines (NIH3T3, A549, and H358) tested in this study, this mol. is investigated in further tests. In two cell lines (HUVEC and MCF-7) tested, 19d induced G2/M cell cycle arrest in a concentration dependent manner. Adherent cells detached from the plates and underwent cell death possibly due to apoptosis at 19d concentrations that induced cell cycle arrest. In the experiment, the researchers used many compounds, for example, 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5Name: 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate).

1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5) belongs to imidazole derivatives. Many natural products, especially alkaloids, contain the imidazole ring. These imidazoles share the 1,3-C3N2 ring but feature varied substituents. Imidazole derivatives have antibacterial, antifungal and anticancer functionality. It interacts with DNA and also binds to protein and stops cell division.Name: 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Formulation and In Vitro, In Vivo Correlation Between Two Candesartan Cilexetil Tablets was written by Zaid, Abdel Naser;Radwan, Asma;Jaradat, Nidal;Mousa, Ayman;Ghazal, Nadia;Bustami, Rana. And the article was included in Clinical Pharmacology in Drug Development in 2018.HPLC of Formula: 145040-37-5 This article mentions the following:

In this study, the in vitro and in vivo interchangeability between generic candesartan 16 mg and the branded formulation was assessed. The in vitro release of these products was conducted in 3 pH media (1.2, 5.0, and 6.8), and similarity factors (f2) were calculated This bioequivalence study was a randomized, 2-period crossover study that included 42 healthy adult male subjects under fasting conditions with a 9-day washout. The pharmacokinetic (PK) parameters AUC_0-last, AUC_0-∞, and C_max, t_max, and the elimination half-life time were assessed based on the plasma concentrations of candesartan, using a newly developed and validated liquid chromatog.-tandem mass spectrometry bioanal. method with acceptable degrees of linearity, sensitivity, precision, and accuracy. The geometric mean (ng.h/mL) of the AUC0-∞ for the test and brand was 1595.49 and 1620.54, resp., and the C_max (ng/mL) was 160.91 and 160.88, resp. The 90%CIs of geometric mean ratios (test-to-reference ratios) were 98.26%, 98.45%, and 99.86% for AUC_0-last, AUC_0-∞, and Cmax resp. These PK parameters lie within the US Food and Drug Administration- and European Medicines Agency-specified bioequivalence limit (80%-125%). Both products were well tolerated by all the subjects. The tested drug product was bioequivalent to the reference drug and had the same safety profile. In the experiment, the researchers used many compounds, for example, 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5HPLC of Formula: 145040-37-5).

1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5) belongs to imidazole derivatives. Imidazole derivatives generally have good solubility in protic solvents. Simple imidazole derivatives, such as 1H-imidazole, 2-methyl-1H-imidazole, and 1,2-dimethylimidazole, have very high solubility in water. Many drugs contain an imidazole ring, such as certain antifungal drugs, the nitroimidazole series of antibiotics, and the sedative midazolam.HPLC of Formula: 145040-37-5

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Integration of multi-scale molecular modeling approaches with experiments for the in silico guided design and discovery of novel hERG-Neutral antihypertensive oxazalone and imidazolone derivatives and analysis of their potential restrictive effects on cell proliferation was written by Durdagi, Serdar;Aksoydan, Busecan;Erol, Ismail;Kantarcioglu, Isik;Ergun, Yavuz;Bulut, Gulay;Acar, Melih;Avsar, Timucin;Liapakis, George;Karageorgos, Vlasios;Salmas, Ramin E.;Sergi, Baris;Alkhatib, Sara;Turan, Gizem;Yigit, Berfu Nur;Cantasir, Kutay;Kurt, Bahar;Kilic, Turker. And the article was included in European Journal of Medicinal Chemistry in 2018.Name: 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate This article mentions the following:

AT1 antagonists is the most recent drug class of mols. against hypertension and they mediate their actions through blocking detrimental effects of angiotensin II (A-II) when acts on type I (AT1) A-II receptor. The effects of AT1 antagonists are not limited to cardiovascular diseases. AT1 receptor blockers may be used as potential anti-cancer agents – due to the inhibition of cell proliferation stimulated by A-II. Therefore, AT1 receptors and the A-II biosynthesis mechanisms are targets for the development of new synthetic drugs and therapeutic treatment of various cardiovascular and other diseases. Multi-scale mol. modeling approaches were performed and it is found that oxazolone and imidazolone derivatives reveal similar/better interaction energy profiles compared to the FDA approved sartan mols. at the binding site of the AT1 receptor. In silico-guided designed hit mols. were then synthesized and tested for their binding affinities to human AT1 receptor in radioligand binding studies, using [¹²⁵I-Sar¹-Ile⁸] AngII. Among the compounds tested, 19d (4′-((4-(4-bromobenzylidene)-2-butyl-5-oxo-4,5-dihydro-1H-imidazol-1-yl)methyl)[1,1′-biphenyl]-2-carbonitrile) and 9j (4-(2-bromobenzylidene)-2-butyl-1-((2′-(2-trityl-2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl)methyl)-1H-imidazol-5(4H)-one) mols. bound to receptor in a dose response manner and with relatively high affinities. Next, cytotoxicity and wound healing assays were performed for these hit mols. Since hit mol. 19d led to deceleration of cell motility in all three cell lines (NIH3T3, A549, and H358) tested in this study, this mol. is investigated in further tests. In two cell lines (HUVEC and MCF-7) tested, 19d induced G2/M cell cycle arrest in a concentration dependent manner. Adherent cells detached from the plates and underwent cell death possibly due to apoptosis at 19d concentrations that induced cell cycle arrest. In the experiment, the researchers used many compounds, for example, 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5Name: 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate).

1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5) belongs to imidazole derivatives. Many natural products, especially alkaloids, contain the imidazole ring. These imidazoles share the 1,3-C3N2 ring but feature varied substituents. Imidazole derivatives have antibacterial, antifungal and anticancer functionality. It interacts with DNA and also binds to protein and stops cell division.Name: 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Formulation and In Vitro, In Vivo Correlation Between Two Candesartan Cilexetil Tablets was written by Zaid, Abdel Naser;Radwan, Asma;Jaradat, Nidal;Mousa, Ayman;Ghazal, Nadia;Bustami, Rana. And the article was included in Clinical Pharmacology in Drug Development in 2018.HPLC of Formula: 145040-37-5 This article mentions the following:

In this study, the in vitro and in vivo interchangeability between generic candesartan 16 mg and the branded formulation was assessed. The in vitro release of these products was conducted in 3 pH media (1.2, 5.0, and 6.8), and similarity factors (f2) were calculated This bioequivalence study was a randomized, 2-period crossover study that included 42 healthy adult male subjects under fasting conditions with a 9-day washout. The pharmacokinetic (PK) parameters AUC_0-last, AUC_0-∞, and C_max, t_max, and the elimination half-life time were assessed based on the plasma concentrations of candesartan, using a newly developed and validated liquid chromatog.-tandem mass spectrometry bioanal. method with acceptable degrees of linearity, sensitivity, precision, and accuracy. The geometric mean (ng.h/mL) of the AUC0-∞ for the test and brand was 1595.49 and 1620.54, resp., and the C_max (ng/mL) was 160.91 and 160.88, resp. The 90%CIs of geometric mean ratios (test-to-reference ratios) were 98.26%, 98.45%, and 99.86% for AUC_0-last, AUC_0-∞, and Cmax resp. These PK parameters lie within the US Food and Drug Administration- and European Medicines Agency-specified bioequivalence limit (80%-125%). Both products were well tolerated by all the subjects. The tested drug product was bioequivalent to the reference drug and had the same safety profile. In the experiment, the researchers used many compounds, for example, 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5HPLC of Formula: 145040-37-5).

1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5) belongs to imidazole derivatives. Imidazole derivatives generally have good solubility in protic solvents. Simple imidazole derivatives, such as 1H-imidazole, 2-methyl-1H-imidazole, and 1,2-dimethylimidazole, have very high solubility in water. Many drugs contain an imidazole ring, such as certain antifungal drugs, the nitroimidazole series of antibiotics, and the sedative midazolam.HPLC of Formula: 145040-37-5

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Development and evaluation of rapidly disintegrating tablets of Candesartan was written by Ansari, Mohammad Pravej;Iqbal, Majid Md.;Saraswat, Rohit. And the article was included in World Journal of Pharmaceutical Research in 2019.Quality Control of 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate This article mentions the following:

In the present work, Rapidly disintegrating tablets of Cadesartan cilexetil were designed with a view to enhance patient compliance by direct compression method. In the direct compression method, crospovidone, croscarmellose sodium, sodium starch glycolate as superdisintegrants were used along with Sweeteners and flavours were used to enhance the organoleptic properties of tablet. Tablets were prepared by direct compression technique. Directly compressible microcrystalline cellulose to enhance mouth feel. Prepared tablets were evaluated for thickness, uniformity of weight, hardness, friability, wetting time, in -vitro disintegration time, drug content and in vitro drug release. Short-term stability (40°C / 75% RH for 3 mo) and drug-excipient interaction study (IR spectroscopy) are also were studied. Disintegration time and drug release were taken as the basis to optimize the rapidly disintegrating tablet. All the formulations were evaluated for the influence of disintegrates and their concentrations on the characteristics of rapid disintegrating tablets mainly in terms of disintegration time and dissolution studies. The disintegration time of all formulation showed less than 37 s. Among the three superdisintegrants used, Crospovidon showed less disintegrating time followed by croscarmellose sodium and sodium starch gycolate. The relative efficiency of different superdisintegrants to improve the drug rate of tablets was in order, crospovidon > Croscarmellose sodium > sodium starch gycolate. In the experiment, the researchers used many compounds, for example, 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5Quality Control of 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate).

1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5) belongs to imidazole derivatives. Imidazole derivatives generally have good solubility in protic solvents. Simple imidazole derivatives, such as 1H-imidazole, 2-methyl-1H-imidazole, and 1,2-dimethylimidazole, have very high solubility in water. Imidazole is incorporated into many important biological compounds. The most pervasive is the amino acid histidine, which has an imidazole side-chain. Histidine is present in many proteins and enzymes, e.g. by binding metal cofactors, as seen in hemoglobin.Quality Control of 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

17-a-estradiol late in life extends lifespan in aging UM-HET3 male mice; nicotinamide riboside and three other drugs do not affect lifespan in either sex was written by Harrison, David E.;Strong, Randy;Reifsnyder, Peter;Kumar, Navasuja;Fernandez, Elizabeth;Flurkey, Kevin;Javors, Martin A.;Lopez-Cruzan, Marisa;Macchiarini, Francesca;Nelson, James F.;Bitto, Alessandro;Sindler, Amy L.;Cortopassi, Gino;Kavanagh, Kylie;Leng, Lin;Bucala, Richard;Rosenthal, Nadia;Salmon, Adam;Stearns, Timothy M.;Bogue, Molly;Miller, Richard A.;Markewych, Adrian. And the article was included in Aging Cell in 2021.Reference of 145040-37-5 This article mentions the following:

In genetically heterogeneous mice produced by the CByB6F1 x C3D2F1 cross, the “non-feminizing” estrogen, 17-α-estradiol (17aE2), extended median male lifespan by 19% (p < 0.0001, log-rank test) and 11% (p = 0.007) when fed at 14.4 ppm starting at 16 and 20 mo, resp. 90th percentile lifespans were extended 7% (p = 0.004, Wang-Allison test) and 5% (p = 0.17). Body weights were reduced about 20% after starting the 17aE2 diets. Four other interventions were tested in males and females: nicotinamide riboside, candesartan cilexetil, geranylgeranylacetone, and MIF098. Despite some data suggesting that nicotinamide riboside would be effective, neither it nor the other three increased lifespans significantly at the doses tested. The 17aE2 results confirm and extend our original reports, with very similar results when started at 16 mo compared with mice started at 10 mo of age in a prior study. The consistently large lifespan benefit in males, even when treatment is started late in life, may provide information on sex-specific aspects of aging. In the experiment, the researchers used many compounds, for example, 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5Reference of 145040-37-5).

1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5) belongs to imidazole derivatives. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has become an important synthon in the development of new drugs. Imidazole based anticancer drug find applications in cancer chemotherapy. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC).Reference of 145040-37-5

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Host-Guest Interactions between Candesartan and Its Prodrug Candesartan Cilexetil in Complex with 2-Hydroxypropyl-β-cyclodextrin: On the Biological Potency for Angiotensin II Antagonism was written by Ntountaniotis, Dimitrios;Andreadelis, Ioannis;Kellici, Tahsin F.;Karageorgos, Vlasios;Leonis, Georgios;Christodoulou, Eirini;Kiriakidi, Sofia;Becker-Baldus, Johanna;Stylos, Evgenios K.;Chatziathanasiadou, Maria V.;Chatzigiannis, Christos M.;Damalas, Dimitrios E.;Aksoydan, Busecan;Javornik, Uros;Valsami, Georgia;Glaubitz, Clemens;Durdagi, Serdar;Thomaidis, Nikolaos S.;Kolocouris, Antonios;Plavec, Janez;Tzakos, Andreas G.;Liapakis, George;Mavromoustakos, Thomas. And the article was included in Molecular Pharmaceutics in 2019.Computed Properties of C33H34N6O6 This article mentions the following:

Renin-angiotensin aldosterone system inhibitors are for a long time extensively used for the treatment of cardiovascular and renal diseases. AT1 receptor blockers (ARBs or sartans) act as antihypertensive drugs by blocking the octapeptide hormone Angiotensin II to stimulate AT1 receptors. The antihypertensive drug candesartan (CAN) is the active metabolite of candesartan cilexetil (Atacand, CC). Complexes of candesartan and candesartan cilexetil with 2-hydroxylpropyl-β-cyclodextrin (2-HP-β-CD) were characterized using high-resolution electrospray ionization mass spectrometry and solid state ¹³C cross-polarization/magic angle spinning NMR (CP/MAS NMR) spectroscopy. The ¹³C CP/MAS results showed broad peaks especially in the aromatic region, thus confirming the strong interactions between cyclodextrin and drugs. This exptl. evidence was in accordance with mol. dynamics simulations and quantum mech. calculations The synthesized and characterized complexes were evaluated biol. in vitro. It was shown that as a result of CAN’s complexation, CAN exerts higher antagonistic activity than CC. Therefore, a formulation of CC with 2-HP-β-CD is not indicated, while the formulation with CAN is promising and needs further investigation. This intriguing result is justified by the binding free energy calculations, which predicted efficient CC binding to 2-HP-β-CD, and thus, the mol.’s availability for release and action on the target is diminished. In contrast, CAN binding was not favored, and this may allow easy release for the drug to exert its bioactivity. In the experiment, the researchers used many compounds, for example, 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5Computed Properties of C33H34N6O6).

1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5) belongs to imidazole derivatives. Imidazole derivatives generally have good solubility in protic solvents. Simple imidazole derivatives, such as 1H-imidazole, 2-methyl-1H-imidazole, and 1,2-dimethylimidazole, have very high solubility in water. Imidazole based anticancer drug find applications in cancer chemotherapy. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC).Computed Properties of C33H34N6O6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Effect of salt formation on γ-cyclodextrin solubilization of irbesartan and candesartan and the chemical stability of their ternary complexes was written by Jansook, Phatsawee;Hnin, Hay Marn;Praphanwittaya, Pitsiree;Loftsson, Thorsteinn;Stefansson, Einar. And the article was included in Journal of Drug Delivery Science and Technology in 2022.Electric Literature of C33H34N6O6 This article mentions the following:

Angiotensin II receptor blockers (ARBs) are unstable compounds and have relatively low aqueous solubility, which may hamper their bioavailability. The present study aimed to increase the aqueous solubility of ARBs by the formation of cyclodextrin (CD) inclusion complex and determine their chem. stability in aqueous solutions The pH- solubility of drugs and their phase-solubility profiles were determined, and the results showed that the solubility of drugs increased by forming inclusion complexes with γ-cyclodextrin (γCD) and by increasing their intrinsic solubility in phosphate buffer (pH 7.5). The formation of irbesartan/γCD (IRB/γCD) and candesartan cilexetil/γCD (CAC/γCD) inclusion complexes was confirmed by mol. docking. To enhance the γCD solubilization of drugs, salt formation using various organic salts was also investigated. Of these, Tris was the most powerful, followed by sodium acetate, as they significantly increased the γCD solubilization of IRB and CAC. However, chem. instability was observed, particularly at high salt concentrations, where they provided a higher IRB and CAC solubility Thus, the balance of optimum drug solubility and its chem. stability in aqueous solutions should be considered in formulation development. In the experiment, the researchers used many compounds, for example, 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5Electric Literature of C33H34N6O6).

1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5) belongs to imidazole derivatives. 1H-imidazole is an imidazole tautomer which has the migrating hydrogen at position 1. It is a conjugate base of an imidazolium cation. It is a conjugate acid of an imidazolide. It is a tautomer of a 4H-imidazole. Imidazole also acts as a microtubule destabilizing agents and inhibits topoisomerase and Cytochrome P450 Family 26 Subfamily A Member 1 (CYP26A1) enzymes.Electric Literature of C33H34N6O6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

The effects of cardiac drugs on human erythrocyte carbonic anhydrase I and II isozymes was written by Argan, Onur;Cikrikci, Kubra;Baltaci, Aybike;Gencer, Nahit. And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2020.Safety of 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate This article mentions the following:

Cardiovascular diseases are the leading cause of mortality worldwide. In recent years, the relationship between carbonic anhydrase inhibitors and atherosclerosis has attracted attention. In this study, we aimed to determine the in vitro effects of 35 frequently used cardiac drugs on human carbonic anhydrase I (hCA I) and II (hCA II). The inhibitory effects of the drugs on hCA I and hCA II were determined with both the hydratase and esterase methods. The most potent inhibitors observed were propafenone (hCA I: 2.8μM and hCA II: 3.02μM) and captopril (hCA I: 1.58μM and hCA II: 6.25μM). Isosorbide mononitrate, propranolol, furosemide, and atorvastatin were also potent inhibitors. The inhibitor constant, K_i, value from the Lineweaver-Burk plot for propafenone was 2.38μM for hCA I and 2.97μM for hCA II. The tested cardiac drugs showed potent in vitro inhibition of the hCA I and II isoenzymes. Especially, in patients with atherosclerotic heart disease, these drugs may be preferred primarily due to the beneficial effects of carbonic anhydrase inhibition on atherosclerosis. In the experiment, the researchers used many compounds, for example, 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5Safety of 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate).

1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5) belongs to imidazole derivatives. Many natural products, especially alkaloids, contain the imidazole ring. These imidazoles share the 1,3-C3N2 ring but feature varied substituents. Imidazole based anticancer drug find applications in cancer chemotherapy. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC).Safety of 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Controlling a Cohort: Use of Mirabilis-Based Purge Calculations to Understand Nitrosamine-Related Risk and Control Strategy Options was written by Burns, Michael J.;Teasdale, Andrew;Elliott, Eric;Barber, Chris G.. And the article was included in Organic Process Research & Development in 2020.Application In Synthesis of 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate This article mentions the following:

The recent discovery of nitrosamines within marketed drugs, such as Valsartan, has led to changes within the regulatory landscape. Most notably, the requirement for a risk evaluation of the presence of nitrosamines within the drug product has been extended from sartan-type tetrazole containing drugs to all marketed products. The largest inherent risks associated with a drug substance will generally arise from impurity formation and carryover in the synthetic manufacturing process. Despite the classification of nitrosamines within the cohort of concern, the understanding of their behavior based on physicochem. properties is unaffected by this status, and as such all control options laid out in ICH M7 should be considered acceptable. This communication aims to show how the use of purge calculations, utilizing the Mirabilis software, fully de-risked nitrosamine concerns related to the development of Candesartan cilexetil. Aligned to the principles of impurity control in the ICH M7 guideline, this provided a suitable strategy to determine, and subsequently demonstrate control of, the nitrosamine risk. In the experiment, the researchers used many compounds, for example, 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5Application In Synthesis of 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate).

1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5) belongs to imidazole derivatives. Imidazole is the basic core of some natural products such as histidine, purine, histamine and DNA based structures, etc. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has been usedin the lysis, wash and elution buffer for the purification of histidine tagged Sonic Hedgehog(shh-N) protein, in elution buffer in stepwise gradient for the purification of histidine tagged aldo keto reductases using nickel affinity chromatography, as a component of homogenization buffer for the purification of phagosomal compartments from dendritic cells.Application In Synthesis of 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem