87637-30-7

Upstream product

• 2103-99-3 4-(4-chlorophenyl)-2-thiazolamine 
• 98-88-4 benzoyl chloride 
• 536-38-9 4-chlorobenzoylmethyl bromide 
• 614-23-3 N-benzoylthiourea 
• 99-91-2 para-chloroacetophenone 

Downstream Products

• 103966-17-2 1-(4-p-chlorophenylthiazol-2-yl)-5-phenyltetrazole 
• 103966-25-2 2-phenyl-5-p-chlorophenylthiazolo<3,2-b>-s-triazole 
• 64343-57-3 N-(4-p-chlorophenylthiazole-2-yl)phenylimidoyl chloride 

Relevant academic research and scientific papers

Molecular properties prediction, synthesis, and antimicrobial activity of bis(azolyl)sulfonamidoacetamides

A library of bis(azolyl)sulfonamidoacetamides was prepared by the reaction of azolylsulfonylamines with azolylchloroacetamides in the presence of pyridine/4-(dimethylamino)pyridine (DMAP) under ultrasonication. The reaction proceeded well with DMAP, resulting in a higher yield of the products. The antimicrobial activity of the compounds indicated that N-{5-[N-(2-{[4-(4-chloro-1H-pyrrol-2-yl)-1H-imidazol-2-yl)amino}-2-oxoethyl)sulfamoyl]-4-phenylthiazol-2-yl}benzamide (22a), N-{5-[N-(2-{[4-(4-chloro-1H-pyrrol-2-yl)-1H-imidazol-2-yl]amino}-2-oxoethyl)sulfamoyl]-4-(4-chlorophenyl)thiazol-2-yl}benzamide (22c), and N-{5-[N-(2-{[4-(4-chloro-1H-pyrrol-2-yl)-1H-imidazol-2-yl]amino}-2-oxoethyl)sulfamoyl]-4-(4-chloro-phenyl)-1H-imidazol-2-yl}benzamide (24c) exhibited a low minimal inhibitory concentration (MIC) against Bacillus subtilis, equal to the standard drug, chloramphenicol. Compounds 22c and 24c also showed low MICs against Aspergillus niger, equal to the standard drug, ketoconazole. The molecular properties of the synthesized molecules were studied to identify druglikeness properties of the target compounds. On the basis of molecular properties prediction, 19a, 19b, 20b, 20c, 21a–c, 22b, 22c, and 23a–c can be treated as drug candidates.

4-(4-Chlorophenyl)thiazol-2-amines as pioneers of potential neurodegenerative therapeutics with anti-inflammatory properties based on dual DNase I and 5-LO inhibition

Eleven new 4-(4-chlorophenyl)thiazol-2-amines were synthesized and, together with nine known derivatives, evaluated in vitro for inhibitory properties towards bovine pancreatic DNase I. Three compounds (18–20) inhibited DNase I with IC50 values

Synthesis and antimicrobial activity of bisazolylsulfonyl amines

A variety of bisazolylsulfonyl amines have been prepared from azolylsulfonyl chlorides and azolylsulfonamides and their antimicrobial activity studied. The chloro substituted bisthiazolylsulfonyl amines exhibit pronounced antibacterial activity against B.

2-amino-4-arylthiazole derivatives as anti-giardial agents: Synthesis, biological evaluation and QSAR studies

A series of seven 2-amino-4-arylthiazoles were prepared following Hantzsch's modified method under microwave irradiation. A set of 50 derivatives was obtained and the in vitro activity against Giardia intestinalis was evaluated. The results on the biological activity revealed that, in general, the N-(5-bromo-4-aryl-thiazol-2-yl)-acetamide scaffold showed high bioactivity. In particular, compounds 6e (IC50= 0.39 μM) and 6b (IC50= 0.87 μM) were found to be more potent than the positive control metronidazole. Citoxicity and acute toxicity tests performed showed low toxicity and high selectivity of the most active compounds (6e SI = 139, 6b SI = 52.3). A QSAR analysis was applied to a data set of 37 obtained 2-amino-4-arylthiazoles derivatives and the best model described a strongly correlation between the anti-giardiasic activity and molecular descriptors as E2M, RDF115m, F10, MATS6v, and Hypnotic-80, with high statistical quality. This finding indicates that N-substituted aminothiazole scaffold should be investigated for the development of highly selective anti-giardial agent.

PhCOCI-Py/basic alumina as a versatile reagent for benzoylation in solvent-free conditions

A solvent-free procedure using PhCOCl-Py/basic alumina under microwave irradiation has been developed for N-, O- and S-benzoylation.

Synthesis of 2,5-Diarylthiazolo-s-triazoles

2,5-Diarylthiazolo-s-triazoles (II) have been synthesised via 1-(4-arylthiazol-2-yl)-5-aryltetrazoles (VII).Compounds (VII) have been synthesised by the reaction of 2-aroylamino-4-arylthiazoles (V) with phosphorus pentachloride, and azidolysis of t