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Recent Advances on Isoniazide Derivatives

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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.

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

Document Type: Research Article

Publication date: January 1, 2008

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  • Anti-Infective Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of new anti-infective agents.
    Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of current topics in anti-infective medicinal chemistry.

    Anti-Infective Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in anti-infective drug discovery.
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