Month: October 2022

Khalil-Moghaddam, Shiva; Shahvelayati, Ashraf Sadat; Aliahmadi, Atousa published the artcile< Synthesis and antioxidant properties of two new derivatives of indeno-benzofuran>, Safety of 1-carboxymethyl-3-methylimidazolium chloride, the main research area is pyrogallol ninhydrin adduct preparation green chem antioxidant.

Ninhydrin reacts with poly-phenols in different ratios to produce tetracyclic adducts. Here, pyrogallol was used as a polyphenol compound In the company of acidic ionic liquid (AIL), there was a selective reaction between the ortho-site of polyphenol and the ninhydrin’s carbonyl group. Mono-adduct (1:1) and bis-adduct (2:1) were prepared using 1-(carboxymethyl)-3-methyl-1H-imidazolium chloride (mcmimCl) as a solvent and catalyst. Moreover, the antioxidant activity of these adducts was investigated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical assay and butylated hydroxytoluene (BHT) was considered to be standard The results indicated that mono-adduct showed the strongest antioxidant activity (IC50 = 5.289μg/mL).

Journal of Chemical Health Risks published new progress about Antioxidants. 700370-07-6 belongs to class imidazoles-derivatives, and the molecular formula is C6H9ClN2O2, Safety of 1-carboxymethyl-3-methylimidazolium chloride.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Radhakrishnan, Harikrishnan; Javitz, Harold S.; Bhatnagar, Parijat published the artcile< Lentivirus Manufacturing Process for Primary T-Cell Biofactory Production>, Recommanded Product: 7H-Purin-2-amine, the main research area is FRalpha HDAC CAR T cell growth viral infection; CAR T cells; cell engineering; cell manufacturing; drug delivery; high-titer lentivirus production.

A process for maximizing the titer of lentivirus particles, deemed to be a necessity for transducing primary cells, is developed. Lentivirus particles, with a set of transgenes encoding an artificial cell-signaling pathway, are used to transform primary T cells as vectors for calibrated synthesis of desired proteins in situ, i.e., T-cell biofactory cells. The process is also used to generate primary T cells expressing antigen-specific chimeric antigen receptors, i.e., CAR T cells. The two differently engineered primary T cells are expanded and validated for their resp. functions, i.e., calibrated synthesis of desired proteins upon engaging the target cells, which is specific for the T-cell biofactory cells, and cytolysis of the target cells common to both types of cells. The process is compliant with current Good Manufacturing Practices and can be used to support the scale-up for clin. translation.

Advanced Biosystems published new progress about Biomarkers. 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Recommanded Product: 7H-Purin-2-amine.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Lu, Zhongyang; Li, Yanchun; Syn, Wing-Kin; Wang, Zhewu; Lopes-Virella, Maria F.; Lyons, Timothy J.; Huang, Yan published the artcile< Amitriptyline inhibits nonalcoholic steatohepatitis and atherosclerosis induced by high-fat diet and LPS through modulation of sphingolipid metabolism>, Reference of 6823-69-4, the main research area is atherosclerosis nonalcoholic steatohepatitis amitriptyline antiatherosclerotic sphingolipid; acid sphingomyelinase; amitriptyline; diabetes; inflammation; nonalcoholic steatohepatitis.

We reported previously that increased acid sphingomyelinase (ASMase)-catalyzed hydrolysis of sphingomyelin, which leads to increases in ceramide and sphingosine 1 phosphate, played a key role in the synergistic upregulation of proinflammatory cytokines by palmitic acid (PA), a major saturated fatty acid, and lipopolysaccharide (LPS) in macrophages. Since macrophages are vital players in nonalcoholic steatohepatitis (NASH) and atherosclerosis, we assessed the effect of ASMase inhibition on NASH and atherosclerosis cooperatively induced by high-PA-containing high-fat diet (HP-HFD) and LPS in LDL receptor-deficient mice. Interestingly, immunohistochem. study showed that amitriptyline, but not GW4869, strongly reduced hepatic inflammation. Furthermore, results showed that both amitriptyline and GW4869 attenuated atherosclerosis. To elucidate the underlying mechanisms whereby amitriptyline inhibited both NASH and atherosclerosis, but GW4869 only inhibited atherosclerosis, we found that amitriptyline, but not GW4869, downregulated proinflammatory cytokines in macrophages. Finally, we found that inhibition of sphingosine 1 phosphate production is a potential mechanism whereby amitriptyline inhibited proinflammatory cytokines. Collectively, this study showed that amitriptyline inhibited NASH and atherosclerosis through modulation of sphingolipid metabolism in LDLR-/- mice, indicating that sphingolipid metabolism in macrophages plays a crucial role in the linkage of NASH and atherosclerosis.

American Journal of Physiology published new progress about Atherosclerosis. 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Reference of 6823-69-4.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

De Bie, D. A.; Van Der Plas, H. C.; Geurtsen, G. published the artcile< Didehydrohetarenes. XX. Reactions of 4- and 5-haloimidazoles with lithium piperidide in piperidine>, Recommanded Product: 5-Bromo-1-methyl-1H-imidazole, the main research area is halo imidazole lithium piperidide reaction.

On treatment of 5-halo-1-methyl-imidazole with lithium piperidide in piperidine, an addition-elimination reaction giving 1-methyl-5-piperidinoimidazole, transhalogenation giving 4-halo-1-methylimidazole and a meta substitution yielding the 1-methyl-2-piperidinoimidazole, were observed. No indication for the occurrence of a 4,5-didehydro-1-methylimidazole was obtained.

Recueil des Travaux Chimiques des Pays-Bas published new progress about 1003-21-0. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Recommanded Product: 5-Bromo-1-methyl-1H-imidazole.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Patutina, Olga; Chiglintseva, Daria; Bichenkova, Elena; Gaponova, Svetlana; Mironova, Nadezhda; Vlassov, Valentin; Zenkova, Marina published the artcile< Dual miRNases for triple incision of miRNA target: design concept and catalytic performance>, Safety of 7H-Purin-2-amine, the main research area is microRNA21 microRNAR155 microRNA17a oligonucleotide peptide catalysis; RNA cleavage; RNase H; anti-miRNA therapy; artificial ribonuclease; miRNase; oligonucleotide-peptide conjugate; oncogenic miRNA.

Irreversible destruction of disease-associated regulatory RNA sequences offers exciting opportunities for safe and powerful therapeutic interventions against human pathophysiol. In 2017, for the first time we introduced miRNAses-miRNA-targeted conjugates of a catalytic peptide and oligonucleotide capable of cleaving an miRNA target. Herein, we report the development of Dual miRNases against oncogenic miR-21, miR-155, miR-17 and miR-18a, each containing the catalytic peptide placed in-between two short miRNA-targeted oligodeoxyribonucleotide recognition motifs. Substitution of adenines with 2-aminoadenines in the sequence of oligonucleotide “”shoulders”” of the Dual miRNase significantly enhanced the efficiency of hybridization with the miRNA target. It was shown that sequence-specific cleavage of the target by miRNase proceeded metal-independently at pH optimum 5.5-7.5 with an efficiency varying from 15% to 85%, depending on the miRNA sequence. A distinct advantage of the engineered nucleases is their ability to addnl. recruit RNase H and cut miRNA at three different locations. Such cleavage proceeds at the central part by Dual miRNase, and at the 5′- and 3′-regions by RNase H, which significantly increases the efficiency of miRNA degradation Due to increased activity at lowered pH Dual miRNases could provide an addnl. advantage in acidic tumor conditions and may be considered as efficient tumor-selective RNA-targeted therapeutic.

Molecules published new progress about MicroRNA-155 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Safety of 7H-Purin-2-amine.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Begtrup, Mikael; Larsen, Peter published the artcile< Alkylation, acylation, and silyation of azoles>, Formula: C4H5BrN2, the main research area is azole alkylation solvent effect; acylation azole anion; silylation azole anion; methylation benzylation azole anion.

Performing alkylation, acylation, and silylation reactions in sep. deprotonation and nucleophilic displacement steps allows for better control of reaction conditions and facilitates problem handling in these processes. In the alkylation of azoles, the alkylating agents and solvents possess individual reaction capabilities which seem to be approx. additive. Monoalkylation occurs if the sum of the normalized reaction potentials is equal or larger than the pKa value of the azole. Dialkylation is avoided by keeping the sum of the normalized reaction potentials below the pKa value of the alkylazole. The applicability of these principles is demonstrated by the development of effective procedures for the methylation, benzylation, acetylation, methoxycarbonylation, and trimethylsilylation of azoles.

Acta Chemica Scandinavica published new progress about Acylation. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Formula: C4H5BrN2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Seelam, Preethi P.; Mitra, Abhijit; Sharma, Purshotam published the artcile< Pairing interactions between nucleobases and ligands in aptamer:ligand complexes of riboswitches: crystal structure analysis, classification, optimal structures, and accurate interaction energies>, Formula: C5H5N5, the main research area is nucleobases ligands riboswitches crystal structure.

In the present work, 67 crystal structures of the aptamer domains of RNA riboswitches are chosen for anal. of the structure and strength of hydrogen bonding (pairing) interactions between nucleobases constituting the aptamer binding pockets and the bound ligands. A total of 80 unique base:ligand hydrogen-bonded pairs containing at least two hydrogen bonds were identified through visual inspection. Classification of these contacts in terms of the interacting edge of the aptamer nucleobase revealed that interactions involving the Watson-Crick edge are the most common, followed by the sugar edge of purines and the Hoogsteen edge of uracil. Alternatively, classification in terms of the chem. constitution of the ligand yields five unique classes of base:ligand pairs: base:base, base:amino acid, base:sugar, base:phosphate, and base:other. This indicates that these contacts are well-defined RNA aptamer:ligand interaction motifs. The anal. was further extended to study the biol. importance of base:ligand interactions in the binding pocket of the tetrahydrofolate riboswitch and thiamine pyrophosphate riboswitch. Overall, our study helps in understanding the structural and energetic features of base:ligand pairs in riboswitches, which could aid in developing meaningful hypotheses in the context of RNA:ligand recognition. This can, in turn, contribute toward current efforts to develop antimicrobials that target RNAs.

RNA published new progress about Amino acids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Formula: C5H5N5.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Vechetti, Ivan J. Jr; Peck, Bailey D.; Wen, Yuan; Walton, R. Grace; Valentino, Taylor R.; Alimov, Alexander P.; Dungan, Cory M.; Van Pelt, Douglas W.; von Walden, Ferdinand; Alkner, Bjorn; Peterson, Charlotte A.; McCarthy, John J. published the artcile< Mechanical overload-induced muscle-derived extracellular vesicles promote adipose tissue lipolysis>, Safety of p-Benzenediacrylanilide, 4′,4′′-di-2-imidazolin-2-yl-, dihydrochloride, the main research area is skeletal muscle extracellular vesicle adipose tissue lipolysis; adipose tissue; extracellular vesicles; lipolysis; microRNAs; skeletal muscle.

How regular phys. activity is able to improve health remains poorly understood. The release of factors from skeletal muscle following exercise has been proposed as a possible mechanism mediating such systemic benefits. We describe a mechanism wherein skeletal muscle, in response to a hypertrophic stimulus induced by mech. overload (MOV), released extracellular vesicles (EVs) containing muscle-specific miR-1 that were preferentially taken up by epidydimal white adipose tissue (eWAT). In eWAT, miR-1 promoted adrenergic signaling and lipolysis by targeting Tfap2α, a known repressor of Adrβ3 expression. Inhibiting EV release prevented the MOV-induced increase in eWAT miR-1 abundance and expression of lipolytic genes. Resistance exercise decreased skeletal muscle miR-1 expression with a concomitant increase in plasma EV miR-1 abundance, suggesting a similar mechanism may be operative in humans. Altogether, these findings demonstrate that skeletal muscle promotes metabolic adaptations in adipose tissue in response to MOV via EV-mediated delivery of miR-1.

FASEB Journal published new progress about 3′-Untranslated region Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Safety of p-Benzenediacrylanilide, 4′,4′′-di-2-imidazolin-2-yl-, dihydrochloride.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Caldero-Rodriguez, Naishka E.; Ortiz-Rodriguez, Luis A.; Gonzalez, Andres A.; Crespo-Hernandez, Carlos E. published the artcile< Photostability of 2,6-diaminopurine and its 2'-deoxyriboside investigated by femtosecond transient absorption spectroscopy>, Application In Synthesis of 452-06-2, the main research area is photostability 26DAP 26DAPd femtosecond transient absorption spectroscopy.

UV radiation (UVR) from the sun is essential for the prebiotic syntheses of nucleotides, but it can also induce photolesions such as the cyclobutane pyrimidine dimers (CPDs) to RNA or DNA oligonucleotide in prebiotic Earth. 2,6-Diaminopurine (26DAP) has been proposed to repair CPDs in high yield under prebiotic conditions and be a key component in enhancing the photostability of higher-order prebiotic DNA structures. However, its electronic relaxation pathways have not been studied, which is necessary to know whether 26DAP could have survived the intense UV fluxes of the prebiotic Earth. We investigate the electronic relaxation mechanism of both 26DAP and its 2′-deoxyribonucleoside (26DAP-d) in aqueous solution using steady-state and femtosecond transient absorption measurements that are complemented with electronic-structure calculations The results demonstrate that both purine derivatives are significantly photostable to UVR. It is shown that upon excitation at 287 nm, the lowest energy 1ππ* state is initially populated. The population then branches following two relaxation coordinates in the 1ππ* potential energy surface, which are identified as the C2- and C6-relaxation coordinates. The population following the C6-coordinate internally converts to the ground state nonradiatively through a nearly barrierless conical intersection within 0.7 ps in 26DAP or within 1.1 ps in 26DAP-d. The population that follows the C2-relaxation coordinate decays back to the ground state by a combination of nonradiative internal conversion via a conical intersection and fluorescence emission from the 1ππ* min. in 43 ps and 1.8 ns for the N9 and N7 tautomers of 26DAP, resp., or in 70 ps for 26DAP-d. Fluorescence quantum yields of 0.037 and 0.008 are determined for 26DAP and 26DAP-d, resp. Collectively, it is demonstrated that most of the excited state population in 26DAP and 26DAP-d decays back to the ground state via both nonradiative and radiative relaxation pathways. This result lends support to the idea that 26DAP could have accumulated in large enough quantities during the prebiotic era to participate in the formation of prebiotic RNA or DNA oligomers and act as a key component in the protection of the prebiotic genetic alphabet.

Physical Chemistry Chemical Physics published new progress about Absorption spectroscopy (Femtosecond Transient). 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Application In Synthesis of 452-06-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Rheault, Tara R.; Donaldson, Kelly H.; Cheung, Mui published the artcile< Convenient synthesis of heteroaryl-linked benzimidazoles via microwave-assisted boronate ester formation>, Quality Control of 1003-21-0, the main research area is halobenzimidazole pinacolatoboron boration microwave; benzimidazolylboronate preparation Suzuki Miyaura cross coupling; benzimidazole heteroaryl preparation.

N-Substituted 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-benzimidazoles were conveniently accessed via microwave-assisted synthesis. Subsequent Suzuki-Miyaura cross-coupling with heteroaryl halides proceeded to give a wide variety of heteroarylbenzimidazoles.

Tetrahedron Letters published new progress about Aryl halides Role: RCT (Reactant), RACT (Reactant or Reagent). 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Quality Control of 1003-21-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem