Tag: M.W=300-350

Li, Jing published the artcileRepurposing of Antazoline Hydrochloride as an Inhibitor of Hepatitis B Virus DNA Secretion, Formula: C17H20ClN3, the publication is Virologica Sinica (2021), 36(3), 501-509, database is CAplus and MEDLINE.

Hepatitis B virus (HBV) belongs to Hepadnaviridae family and mainly infects hepatocytes, which can cause acute or chronic hepatitis. Currently, two types of antiviral drugs are approved for chronic infection clin.: interferons and nucleos(t)ide analogs. However, the clin. cure for chronic infection is still rare, and it is a huge challenge for all researchers to develop high-efficiency, safe, non-tolerant, and low-toxicity anti-HBV drugs. Antazoline hydrochloride is a first-generation antihistamine with anticholinergic properties, and it is commonly used to relieve nasal congestion and in eye drops. Recently, an in vitro high-throughput evaluation system was constructed to screen nearly 800 compounds from the Food and Drug Administration (FDA)-approved Drug Library. We found that arbidol hydrochloride and antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC₅₀ of 4.321 μmol/L and 2.910 μmol/L in HepAD38 cells, resp. Moreover, the antiviral effects and potential mechanism of action of antazoline hydrochloride were studied in different HBV replication systems. The results indicate that antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells, with an EC₅₀ of 2.349 μmol/L. These findings provide new ideas for screening and research related to HBV agents.

Virologica Sinica published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, Formula: C17H20ClN3.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Bekele, Anbessa published the artcileDevelopment and validation of HPTLC densitometric method for simultaneous determination of antazoline hydrochloride and tetryzoline hydrochloride in eye drop and its application as stability indicator, Category: imidazoles-derivatives, the publication is Thai Journal of Pharmaceutical Sciences (2013), 37(3), 134-145, database is CAplus.

A sensitive, selective, precise, accurate, and stability indicating high-performance thin layer chromatog. (HPTLC)-densitometric method for anal. of antazoline hydrochloride and tetryzoline hydrochloride was developed. The method employed HPTLC aluminum plates precoated with silica gel 60 F₂₅₄ as the stationary phase. The solvent system consisted of Et acetate:MeOH:ammonia (10:10:1, volume/volume/v). Densitometric anal. of drugs was carried out in the absorbance mode at 216 nm. This system gave compact spots for both antazoline hydrochloride (R_f 0.60) and tetryzoline hydrochloride (R_f 0.31). Both drugs were subjected to stress test conditions like acid/alkali hydrolysis, oxidation by hydrogen peroxide, dry heat treatment, and photo degradation The spots for products of degradation were well resolved from the spots of resp. intact drugs. The linear regression data for the calibration plots showed good linear relationship with r² of 0.9979 and 0.9990 in the concentration range of 200-1800 ng/band for antazoline hydrochloride and 160-1440 ng/band for tetryzoline hydrochloride, resp. The results indicated that the drugs are susceptible to degradation, to different extent under the different conditions.

Thai Journal of Pharmaceutical Sciences published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, Category: imidazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Youssef, M. K. published the artcileStudies on sorption affinity of polyvinyl chloride towards certain drugs, Related Products of imidazoles-derivatives, the publication is Bulletin of the Faculty of Pharmacy (Cairo University) (1974), 13(1), 15-21, database is CAplus.

Poly(vinyl chloride) [9002-86-2] had considerable sorption affinity towards tetracycline-HCl (I) [64-75-5] and chloramphenicol [56-75-7] but no sorption affinity towards antazoline-HCl [2508-72-7], with the highest affinity shown by I. The addition of KCl decreased the sorption affinity of the plastic granules for the antibiotics.

Bulletin of the Faculty of Pharmacy (Cairo University) published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C6H17NO3Si, Related Products of imidazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Ponce, Yovani Marrero published the artcileAtom-based 2D quadratic indices in drug discovery of novel tyrosinase inhibitors: results of In Silico studies supported by experimental results, Safety of N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, the publication is QSAR & Combinatorial Science (2007), 26(4), 469-487, database is CAplus.

Herein we present results of QSAR studies of tyrosinase inhibitors employing one of the atom-based TOMOCOMD-CARDD (acronym of TOpol. Mol. COMputer Design-Computer Aided “Rational” Drug Design) descriptors, mol. quadratic indexes, and Linear Discriminant Anal. (LDA) as pattern recognition method. In this way, a database of 246 organic chems., reported as tyrosinase inhibitors having great structural variability, was analyzed and presented as a helpful tool, not only for theor. chemists but also for other researchers in this area. In total, 12 LDA-based QSAR models were obtained, the first six with the non-stochastic total and local quadratic indexes and the six remaining models with the stochastic mol. descriptors. The best two models for the non-stochastic and stochastic mol. descriptors, showed an appropriate overall accuracy (92.68 and 89.10%, resp.) and a high Matthews correlation coefficient (C of 0.85 and of 0.84, correspondingly) when applied to the training set. External validation series were also used to validate the obtained models; the 91.67% (C = 0.82) and 90.00% (C = 0.78), were correctly classified, resp. To show the possibilities of the present approach for the ligand-based virtual screening of tyrosinase inhibitors, the developed models were used afterwards in a simulation of a virtual search for tyrosinase inhibitors. For instance, more than 93% (93.33%) and 96% (96.66%) of the screened chems. were correctly classified by the two best LDA-based QSAR models developed with non-stochastic and stochastic quadratic indexes, resp. Finally, the combination of the obtained models permitted the selection/identification of new diterpenoidal alkaloid leads as tyrosinase inhibitors. The found activity is supported by observed inhibitory effects on mushroom tyrosinase enzyme, even comparable with some reference tyrosinase inhibitors. These results support a role for TOMOCOMD-CARDD descriptors in the biosilico discovery of novel tyrosinase inhibitors from large databases of chem. structures (virtual or “in silico”), which may be used to prevent or treat pigmentation disorders.

QSAR & Combinatorial Science published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, Safety of N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Yokota, Shin-ichi published the artcileEffects of imidazoline and nonimidazoline alpha-adrenergic agents, including xylazine, medetomidine, yohimbine, tolazoline, and atipamezole, on aggregation of bovine and equine platelets, Related Products of imidazoles-derivatives, the publication is American Journal of Veterinary Research (2013), 74(3), 395-402, database is CAplus and MEDLINE.

Objective: To investigate effects of various imidazoline and nonimidazoline α-adrenergic agents on aggregation and antiaggregation of bovine and equine platelets. Sample: Blood samples obtained from 8 healthy adult cattle and 16 healthy adult Thoroughbreds. Procedures: Aggregation and antiaggregation effects of various imidazoline and nonimidazoline α-adrenergic agents on bovine and equine platelets were determined via a turbidimetric method. Collagen and ADP were used to initiate aggregation. Results: Adrenaline, noradrenaline, or α-adrenoceptor agents alone did not induce changes in aggregation of bovine or equine platelets or potentiate ADP- or collagen-induced platelet aggregation. Adrenaline and the α₂-adrenoceptor agonist clonidine had an inhibitory effect on ADP- and collagen-induced aggregation of bovine platelets. The α₂-adrenoceptor antagonists phentolamine and yohimbine also inhibited collagen-induced aggregation of bovine platelets. Noradrenaline, other α-adrenoceptor agonists (xylazine, oxymetazoline, and medetomidine), and α-adrenoceptor antagonists (atipamezole, idazoxan, tolazoline, and prazosin) were less effective or completely ineffective in inhibiting ADP- and collagen-induced aggregation of bovine platelets. The imidazoline α₂-adrenoceptor agonist oxymetazoline submaximally inhibited collagen-induced aggregation of equine platelets, and the α₂-adrenoceptor antagonist idazoxan, along with phentolamine and yohimbine, also inhibited collagen-induced aggregation of equine platelets. The imidazoline compound antazoline inhibited both ADP- and collagen-induced aggregation of equine platelets. Conclusions and Clin. Relevance: Several drugs had effects on aggregation of platelets of cattle and horses, and EDs of ADP and collagen also differed between species. The α₂-adrenoceptor agonists (xylazine and medetomidine) and antagonists (tolazoline and atipamezole) may be used by bovine and equine practitioners without concern for adverse effects on platelet function and hemostasis.

American Journal of Veterinary Research published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C8H6F3NO, Related Products of imidazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Yokota, Shin-ichi published the artcileEffects of Imidazoline and Non-Imidazoline α-Adrenergic Agents on Rabbit Platelet Aggregation, Category: imidazoles-derivatives, the publication is Pharmacology (2013), 91(3-4), 135-144, database is CAplus and MEDLINE.

Imidazoline α₂-adrenergic agents exert complex effects on mammalian platelet aggregation. Although non-adrenergic, imidazoline (I) receptors have been revealed in human platelets, there is limited information about imidazoline’s action on platelet aggregation. This study aimed to investigate aggregatory and anti-aggregatory effects of various imidazoline or non-imidazoline α-adrenergic agents on rabbit platelets. Aggregatory responses of agents on rabbit platelets were examined by turbidimetric method. Radioligand binding assay to platelet I₁ and I₂ receptors was performed using [³H]-clonidine and [³H]-idazoxan, resp. Results: Aggregation was not induced by α-adrenoceptor agonists alone. Adrenaline and noradrenaline produced dose-dependent potentiation of ADP- or collagen-induced aggregation. Imidazoline adrenoceptor agonists clonidine and p-aminoclonidine also potentiated ADP-induced platelet aggregation. The α₂-adrenoceptor antagonists and/or certain imidazoline adrenergic agents inhibited adrenaline-potentiated aggregation in a dose-dependent manner, whereas α₁-adrenoceptor antagonists and non-imidazoline α-adrenergic agents were either ineffective or less effective in inhibiting adrenaline-potentiated aggregation. Rabbit platelets did not have I₁ receptors, but had I₂ receptors, indicating that adrenaline-potentiated platelet aggregation was inhibited by idazoxan, but not by imidazoline compounds clonidine and oxymetazoline. These results demonstrated that α₂-adrenoceptor-blocking agents and/or imidazoline α-adrenergic agents effectively inhibit adrenaline-potentiated platelet aggregation. It is proposed that imidazoline structure in part plays a role in the inhibition of adrenaline-potentiated aggregation.

Pharmacology published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C9H6N2O2, Category: imidazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Pec, Pavel published the artcileInhibition of pig kidney diamine oxidase by some 4,5-dihydroimidazole derivatives, Synthetic Route of 2508-72-7, the publication is Acta Universitatis Palackianae Olomucensis, Facultas Rerum Naturalium (1988), 91(Chem. 27), 227-34, database is CAplus.

The inhibitory activity of some physiol. interesting 4,5-dihydroimidazole derivatives on the activity of diamine oxidase (EC 1.4.3.6) was investigated. The enzyme was isolated from the cortex of pig kidney. Using 2-Me, 2-benzyl, (tolazoline), 2-N(4-tolyl)-N-(3-hydroxyphenyl)aminomethyl (phentolamine), 2-(1-naphthyl)methyl (naphazoline), 2-(2,6-dimethyl-4-tert-butylphenyl)methyl (xylometazoline) and 2-(N-phenyl-N-benzylamino)methyl (antazoline) 4,5-dihydro-imidazoles, the enzyme inhibition was noncompetitive in all cases. The K_i values were in the range 0.2-1.5 mM. The relations among inhibitor structure, K_i, and possible physiol. effects were discussed.

Acta Universitatis Palackianae Olomucensis, Facultas Rerum Naturalium published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, Synthetic Route of 2508-72-7.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Molderings, G. J. published the artcileInhibitory presynaptic imidazoline receptors on sympathetic nerves in the rabbit aorta differ from I₁– and I₂-imidazoline binding sites, Quality Control of 2508-72-7, the publication is Naunyn-Schmiedeberg’s Archives of Pharmacology (1995), 351(5), 507-16, database is CAplus and MEDLINE.

The involvement of imidazoline receptors in modulation of noradrenaline release was investigated in the rabbit aorta preincubated with [³H]noradrenaline and superfused with physiol. salt solution containing cocaine, corticosterone and propranolol. After blockade of α₂-autoreceptors by rauwolscine, the elec. evoked tritium overflow was inhibited by various imidazolines and guanidines. The rank order of potency was BDF 7579 (4-chloro-2-isoindolinylguanidine) ≥ BDF 6143 (4-chloro-2-(2-imidazolin-2-ylamino)-isoindoline) > BDF 6100 [2-(2-imidazolin-2-ylamino)-isoindoline] > clonidine > ST587 (2-(2-chloro-5-trifluoromethylphenylimino)imidazolidine nitrate) ≥ cirazoline > tolazoline > idazoxan > phentolamine. Comparison of the potencies of these drugs with those previously found for the presynaptic imidazoline receptors in the rabbit pulmonary artery revealed a very good correlation. In contrast, no pos. correlation was found with their affinities for the I₁– and I₂-imidazoline binding sites in bovine adrenal medullary membranes and with their lipophilicity (log P values). The elec. evoked tritium overflow was also inhibited by the recently identified endogenous imidazoline receptor ligand agmatine, but was not affected by amiloride. In further series of experiments, the ability of putative antagonist at presynaptic imidazoline receptors to counteract the inhibitory effect of imidazoline derivatives was determined Amiloride, imidazole-4-acetic acid and 1-benzylimidazole did not attenuate the inhibitory effect of BDF 6143 on the elec. evoked tritium overflow. In contrast, rauwolscine antagonized the inhibitory effect of various imidazolines; rauwolscine was clearly less potent in antagonizing the effect of clonidine, BDF 6143 and cirazoline (apparent pA₂ 6.48-7.32) than in antagonizing that of oxymetazoline and moxonidine (apparent pA₂ 8.33 and 8.12, resp.). In a final series of experiments, BDF 6143 (under the conditions applied a selective agonist at presynaptic imidazoline receptors) proved to be considerably less potent in inhibiting tritium overflow evoked by high K⁺ than by elec. stimulation, whereas moxonidine (in rabbit aorta a selective agonist at presynaptic α₂-adrenoceptors) exhibited similar potency in inhibiting the overflow evoked by both methods of stimulation. It is concluded that noradrenaline release in the rabbit aorta is inhibited via both α₂-autoreceptors and presynaptic imidazoline receptors which can be activated by the endogenous imidazoline receptor ligand agmatine. The occurrence of such an α₂-adrenoceptor-independent mechanism is compatible with the ability of K⁺ ions to attenuate the inhibitory effect of an imidazoline receptor agonist but not of an α₂-adrenoceptor agonist, since susceptibility to K⁺ ions has been suggested to be a typical feature of imidazoline recognition sites. The presynaptic imidazoline receptor in rabbit aorta appears to be identical with the previously characterized presynaptic imidazoline receptor in rabbit pulmonary artery, but differs clearly from the I₁ and I₂ binding sites in the bovine adrenal medulla.

Naunyn-Schmiedeberg’s Archives of Pharmacology published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, Quality Control of 2508-72-7.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Rooney, E. K. published the artcileInteraction of antihistamines with lipid bilayers, Safety of N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, the publication is Biochemical Pharmacology (1979), 28(14), 2199-205, database is CAplus and MEDLINE.

All the 10 H₁-antagonists tested reduced the phase transition temperature of a dipalmitoyl phosphatidylcholine lipid bilayer. The binding constants for the drug to the lipid were calculated The H₂-antagonists, cimetidine (I) [51481-61-9] and metiamide [34839-70-8] had no effect on the lipid phase transition temperatures

Biochemical Pharmacology published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, Safety of N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Coston, Alain published the artcileTest of reserpine-induced pontogeniculooccipital spikes in the cat, Computed Properties of 2508-72-7, the publication is Journal de Pharmacologie (1976), 7(3), 409-14, database is CAplus.

The effects of various psychotropic agents on reserpine [50-55-5]-induced pontogeniculooccipital (PGO) spikes were studied in cats. Tricyclic antidepressants dose-dependently antagonized reserpine with clomipramine-HCl [17321-77-6] having the greatest effect. Phenelzine bisulfate [156-51-4] also inhibited reserpine activity. Of the antihistaminics studied dexchlorpheniramine maleate [2438-32-6] and mepyramine maleate [59-33-6] caused the greatest decrease in PGO spikes but were less effective than clomipramine. Orphenadrine-HCl [341-69-5] decreased PGO spikes while dopa [59-92-7] had no effect. A marked decrease in PGO points was also observed with chlordiazepoxide [58-25-3]. Thus, the response of reserpine-induced PGO spikes is an effective means of studying the effects of antidepressants on central reserpine [50-55-5] uptake.

Journal de Pharmacologie published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, Computed Properties of 2508-72-7.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem