6775-40-2Relevant articles and documents
Molecular properties prediction, synthesis, and antimicrobial activity of bis(azolyl)sulfonamidoacetamides
Siva sankar,Narendra babu,Rekha, Tamatam,Padmaja, Adivireddy,Padmavathi, Venkatapuram
, (2021/05/13)
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.
Synthesis of carboxamide and sulfonyl carboxamide linked heterocycles under green conditions
Gaddam, Lakshmi Teja,Thata, Sreenivasulu,Adivireddy, Padmaja,Venkatapuram, Padmavathi
, p. 43 - 54 (2019/11/11)
Direct coupling of heteroaldehydes with heteroaryl amines / sulfonylamines is performed under green conditions using PEG-400 in the presence of oxidant CCl3CN/H2O2. The presence of electron withdrawing substituents on heteroaldehydes increased the yield. Further heteroaryl amines favor the reaction when compared with heteroaryl sulfonylamines.
Fragment-Based Approach to Targeting Inosine-5′-monophosphate Dehydrogenase (IMPDH) from Mycobacterium tuberculosis
Trapero, Ana,Pacitto, Angela,Singh, Vinayak,Sabbah, Mohamad,Coyne, Anthony G.,Mizrahi, Valerie,Blundell, Tom L.,Ascher, David B.,Abell, Chris
, p. 2806 - 2822 (2018/04/23)
Tuberculosis (TB) remains a major cause of mortality worldwide, and improved treatments are needed to combat emergence of drug resistance. Inosine 5′-monophosphate dehydrogenase (IMPDH), a crucial enzyme required for de novo synthesis of guanine nucleotid