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New isoniazid derivatives with improved pharmaco-toxicological profile: Obtaining, characterization and biological evaluation

Dragostin, Ionut and Dragostin, Oana M and Samail, Sangram Keshari and Dash, Saumya and Tatia, Rodica and Dragan, Maria and Confederat, Luminita and Ghiciuc, Cristina M and Diculencu, Daniela and Lupusoru, Catalina E and Zamfir, Carmen L (2019) New isoniazid derivatives with improved pharmaco-toxicological profile: Obtaining, characterization and biological evaluation. In: EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 137 .

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Official URL: https://dx.doi.org/10.1016/j.ejps.2019.104974

Abstract

Tuberculostatic drugs are the most common drug groups with global hepatotoxicity. Awareness of potentially severe hepatotoxic reactions is vital, as hepatic impairment can be a devastating and often fatal condition. The treatment problems that may arise, within this class of medicines, are mainly of two types: adverse reactions (collateral, toxic or hypersensitive reactions) and the initial or acquired resistance of Mycobacterium tuberculosis to one or more antituberculosis drugs. Prevention of adverse reactions, increase treatment adherence and success rates, providing better control of tuberculosis (TB). In this regard, obtaining new drugs with low toxicity and high tuberculostatic potential is essential. Thus, in this work, we have designed or synthesized new derivatives of isoniazid (INH), such as new Isonicotinoylhydrazone (INH-a, INH-b and INH-c). These derivatives demonstrated good biocompatibility, antimicrobial property similar to that of parent isoniazid and last but not least, a significantly improved Pharmacotoxicological profile compared to that of isoniazid.

Item Type: Journal Article
Publication: EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
Publisher: ELSEVIER
Additional Information: copyright for this article belongs to ELSEVIER
Keywords: Isoniazid; Isonicotinoylhydrazone; Tuberculosis; Biocompatibility; Antimicrobial; Hepatotoxicity
Department/Centre: Division of Chemical Sciences > Materials Research Centre
Date Deposited: 18 Sep 2019 09:14
Last Modified: 18 Sep 2019 09:14
URI: http://eprints.iisc.ac.in/id/eprint/63553

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