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
Medicinal Chemistry
Title:Synthesis, Antimycobacterial, Antiviral, Antimicrobial Activity and QSAR Studies of N2-acyl isonicotinic Acid Hydrazide Derivatives
Volume: 9 Issue: 1
Author(s): Vikramjeet Judge, Balasubramanian Narasimhan, Munish Ahuja, Dharmarajan Sriram, Perumal Yogeeswari, Erik De Clercq, Christophe Pannecouque and Jan Balzarini
Affiliation:
Keywords: Antimicrobial, Antitubercular, Antiviral, N2-acyl Isoniazid, QSAR
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.
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Judge Vikramjeet, Narasimhan Balasubramanian, Ahuja Munish, Sriram Dharmarajan, Yogeeswari Perumal, De Clercq Erik, Pannecouque Christophe and Balzarini Jan, Synthesis, Antimycobacterial, Antiviral, Antimicrobial Activity and QSAR Studies of N2-acyl isonicotinic Acid Hydrazide Derivatives, Medicinal Chemistry 2013; 9 (1) . https://dx.doi.org/10.2174/1573406411309010053
DOI https://dx.doi.org/10.2174/1573406411309010053 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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