Synthesis, antimicrobial and anti-inflammatory activities of some new N-substituted sulphonyl indole-3-heterocyclic derivatives

ABSTRACT

A series of I-substituted sulfonyl indole -3-pyrazolines [4a-j and 5-a-j] and isoxazolines [6a-j] were prepared and tested for their antimicrobial and anti-inflammatory activities. The preparation of compounds 4-6a-j was achieved by treatment of the corresponding chalcones 3a-j with hydrazine hydrate in absolute ethanol, hydrazine hydrate in the presence of glacial acetic acid, and with hydroxylamine hydrochloride in absolute ethanol. The purified products were screened for their antimicrobial activity towards Gram positive, Gram negative bacteria and fungi and also for their anti-inflammatory activity using the carrageenan-induced rat paw oedema. Evaluation of the compounds revealed remarkable antibacterial activity reflected by their ability to inhibit Gram positive and Gram negative bacteria, and also revealed remarkable anti-inflammatory activity reflected by their ability to reduce the carrageenan-induced inflammation in rats