The current approach is to develop new and effective antituberculotic agents by sunthesizing new isoniazid derivatives.Isoniazid is used as anti-tuberculotic drug alon and with the combination with other antibiotics. The review of literature survey reveals that maximum of antimicrobial agents contains heterocyclic rings in their structure. The antimicrobial activity of many antibiotics is increased by attaching heterocyclic rings like azetidine, thiozole, oxazole, indole, imidazole etc with the antibiotics.number of potent medicinal agents consists of azetidine, thiazolidine, oxazolidine and imidazolidine ring in their structure having good antimicrobial potency. From the consideration of the above factors research work was aimed to synthesize isoniazid derivatives and evaluate for antimicrobial, antifungal and anti-tuberculotic activity as compared to standard drugs.