Synthesis of some 1-acetylindoline-5-sulphonylamino acid derivatives and studies of their antimicrobial activities.

The synthesis of a series of 1-acetylindoline-5-sulphonylamino acids and some of the corresponding methyl esters and hydrazides (II-XXIII) is described. Coupling of 1-acetylindoline-5-sulphonylamino acids with amino acid methyl ester hydrochlorides in THF-Et3N medium, using the dicyclohexylcarbodiimide method gave the desired 1-acetylindoline-5-sulphonyldipeptide methyl esters (XXIV-XXVIII). Most of the synthetic 1-acetylindoline-5-sulphonylamino acid and dipeptide derivatives (II-XXVII) were found to possess various antimicrobial activities against a number of microorganisms.