Medicinal Chemistry

Author(s): Vikramjeet Judge, Balasubramanian Narasimhan, Munish Ahuja, Dharmarajan Sriram, Perumal Yogeeswari, Erik De Clercq, Christophe Pannecouque and Jan Balzarini

DOI: 10.2174/1573406411309010053

Synthesis, Antimycobacterial, Antiviral, Antimicrobial Activity and QSAR Studies of N2-acyl isonicotinic Acid Hydrazide Derivatives

Page: [53 - 76] Pages: 24

  • * (Excluding Mailing and Handling)

Abstract

A series of N2-acyl isonicotinic acid hydrazides (1-17) was synthesized and tested for its in vitro antimycobacterial activity against Mycobacterium tuberculosis and the results indicated that the compound, isonicotinic acid N'- tetradecanoyl-hydrazide (12) was more active than the reference compound isoniazid. The results of antimicrobial activity of the synthesized compounds against S. aureus, B. subtilis, E. coli, C. albicans and A. niger indicated that compounds with dichloro, hydroxyl, tri-iodo and N2 –tetradecanoyl substituent were the most active ones. The antiviral activity studies depicted that none of the tested compounds were active against DNA or RNA viruses. The multi-target QSAR model was found to be effective in describing the antimicrobial activity of N2-acyl isonicotinic acid hydrazides.

Keywords: Antimicrobial, Antitubercular, Antiviral, N2-acyl Isoniazid, QSAR