Abstract We report the synthesis of 4‐aryl‐2‐piperidone, 4‐arylpiperidine motifs, antituberculosis molecule Q203 (Telacebec) and its analogues. Direct lactamization β ‐C−H arylated N ‐phthaloyl δ ‐aminopentanoic acid carboxamides yielded 4‐aryl‐2‐piperidone (4‐aryl‐ ‐valerolactam) scaffolds. The required were assembled via Pd(II)‐catalyzed, 8‐aminoquinoline‐aided, sp 3 activation arylation meth...

current researches have showed that n3, n5-diaryl-2, 6-dimethyl -1, 4-dihydropyrine-3, 5- dicarboxamide analogues demonstrate notable anti-tubercular activity. in this study, hantzsch condensation was used to design and synthesize new analogues of dihydropyridine (dhp). different diary carboxamides were inserted at positions 3 and 5 of the dhp ring. 4(5)-chloro-2-ethyl-5(4)-imidazolyl moiety wa...

Levofloxacin carboxamides with certain amino acids were prepared through an amide linkage to the acid (glycine, histidine, or serine). These subjected in silico molecular docking evaluation on
 
 DNA gyrase predict their antibacterial activity using GOLD suite. The binding affinities very significant and encouraged synthesis of suggested for intensive evaluation. also Swiss ADME softw...

ABSTRACT. A series of new thiophene derivatives was prepared through nucleophilic substitution reactions the precursor N-(4-substituted-phenyl)-5-(2-chloroacetamido)-4-cyano-3-methylthiophene-2-‎carboxamides 4a and 4b with different sulfur and/or nitrogen reagents (namely; mercaptoacetic acid, 2-mercaptobenzothiazole, 5-(phenylamino)-1,3,4-thiadiazole-2-thiol, 2-mercapto-4,6-dimethylnicotinonit...

A series of 2-aminopyridine-3-carboxamide derivatives against c-Met were designed and synthesized by employing bioisosteric replacement of heterocyclic moieties with the amide bond. The structure-activity relationship (SAR) at various positions of the scaffold was explored. In this study, a promising compound (S)-24o with a c-Met IC(50) of 0.022 μM was identified. The compound exhibited dose-de...

NBS-mediated addition-elimination reaction of sulfonamides/carboxamides and formamides afforded N-sulfonylamidines and N-formylarylamides, respectively, depending on the different mechanism of elimination. Hydrogen bond-induced proton transfer leads to enhanced reactivities and was proposed as the key driving force for the reaction to take place. The protocol demonstrates the possibility of con...