Recent isoniazid derivatives as anti-tubercular agents : review article

Abstract EN

Tuberculosis (TB) remains a global pandemic.

Isoniazid (INH) is an extensively studied antiTB medicine.

However, the recently emerged MDR and TDR TBs have posed challenges to the scientific community to produce more effective anti-TB agents possessing potent effects on the two strains of TB, lesser toxicity and drug interactions with current drugs, reduce the duration of therapy, and have a new mechanism of action to avoid recurrence of MDR.

Accordingly, based on the abnormal lipophilic character of the cell wall of M.

tuberculosis, novel lipophilic isoniazid derivatives have been prepared as hybrids of pyrrole, pyrazole, pyrazoline, triazole, triazine, azetidinone, quinoline, quinolone, thiazolidinone, isatin, cinnamic acid, furoxan, and Schiff bases of certain aldehydes and ketone.

This strategy has resulted in the development of some promising INH hybrids as anti-TB agents, for example, LL-3858 that progressed to the advanced stage of phase II clinical trial.

This review provides a summary of the novel INH-hybrids/ derivatives as anti-TB agents.

It is expected that safer and effective drugs, including these INH-hybrids/ derivatives, may be approved in the future by drug regulatory authorities globally.