Recent Advances on Isoniazide Derivatives

Title: Recent Advances on Isoniazide Derivatives

Volume: 7 Issue: 1

Author(s): Jarmila Vinsova, Ales Imramovsky, Josef Jampilek, Juana Ferriz Monreal and Martin Dolezal

Affiliation:

Keywords: Isoniazide, isoniazide derivatives, M. tuberculosis, multidrug-resistance, antimycobacterial activity, structureactivity relationships

Abstract: Tuberculosis remains the leading cause of mortality worldwide even in the 21st century. This review summarises all facts concerning a front-line antituberculotic drug isoniazide – metabolism, mechanism of activity and resistance. The antimycobacterial pharmacophore moiety of isoniazide has been introduced in a number of various types of molecules (about 510 derivatives have been found) to improve their activity against Mycobacteria species, as well as their multidrug-resistant strains. Several Schiff bases, hydrazones, hydrazides and metal complexes of isoniazide have shown very good activity. Various types of the most active isoniazide derivatives classified according to their structure are reported, their lipophilicity has been calculated and structure-activity relationships are discussed. The original new highly active isoniazide prodrug forms prepared at the Faculty of Pharmacy, Charles University, Czech Republic are presented in a separate chapter of the paper.

Cite this article as:

Vinsova Jarmila, Imramovsky Ales, Jampilek Josef, Monreal Ferriz Juana and Dolezal Martin, Recent Advances on Isoniazide Derivatives, Anti-Infective Agents in Medicinal Chemistry 2008; 7 (1) . https://dx.doi.org/10.2174/187152108783329780