Drug Res (Stuttg) 2013; 63(04): 192-197
DOI: 10.1055/s-0033-1334964
Original Paper
© Georg Thieme Verlag KG Stuttgart · New York

Design, Synthesis and Docking Studies of New 4-hydroxyquinoline-3-carbohydrazide Derivatives as Anti-HIV-1 Agents

Z. Hajimahdi
1   Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
R. Zabihollahi
2   Hepatitis and AIDS department, Pasteur institute of Iran, Tehran, Iran
M. R. Aghasadeghi
2   Hepatitis and AIDS department, Pasteur institute of Iran, Tehran, Iran
A. Zarghi
1   Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
› Author Affiliations
Further Information

Publication History

received 18 November 2012

accepted 31 January 2013

Publication Date:
13 March 2013 (online)


A new class of 4-hydroxyquinoline-3-carbohydrazide derivatives was prepared and evaluated for its anti-HIV activity. The primary bioassay results indicated that most of tested compounds possess moderate inhibitory properties against HIV-1 virus (NL4-3) in Hela cells cultures. Our results also indicated that compounds 6d and 7e were the most potent anti-HIV agents among the synthesized compounds with inhibition rate of 32 and 28% at concentration of 100 μM, respectively. A docking study using the later crystallographic data available for PFV integrase including its complexes with Mg2+ and raltegravir, showed that the designed compounds bind into the active site of integrase such that carboxylic and hydroxyl groups of 4-hydroxyquinoline-3-carbohydrazide chelate the Mg2 + ion. Interestingly, all of the synthesized compounds were found to present no significant cytotoxicity at concentration of 100 μM. Therefore, these compounds can provide a very good basis for the development of new anti-HIV-1 agents.

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