Affiliation:
1. Punjab Biotechnology Incubator, Mohali, Punjab-160071, India
2. Regional Advance Water Testing Laboratory,
Mohali, Punjab-160 059, India
3. Division of Research and Development, Lovely Professional University, Phagwara,
Punjab-144 411, India
4. Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology
(Banaras Hindu University), Varanasi, UP, 221005, India
5. Biocon Bristol Myers Squibb Syngene International Pvt.
Ltd., Bangalore-560 099, India
Abstract
Background:
Pyrazole scaffolds have gained importance in drug discovery and development
for various pharmacological activities like antiviral, antifungal, anticancer, antidepressant, antiinflammatory,
antibacterial, etc. Additionally, the pyrazole moiety has shown potent anti-HIV activity
as a core heterocycle or substituted heterocycles derivatives (mono, di, tri, tetra, and fused pyrazole
derivatives). To assist the development of further potential anti-HIV agents containing pyrazole
nucleus, here we have summarized pyrazole containing anti-HIV compounds that have been reported
by researchers all over the world for the last two decades.
Objective:
Objective: The present review concentrates on an assortment of pyrazole containing compounds,
particularly for potential therapeutic activity against HIV.
Methods:
Google Scholar, Pubmed, and SciFinder were searched databases with ‘‘pyrazol’’ keywords.
Further, the year of publication and keywords ‘‘Anti-HIV’’ filter was applied to obtain relevant
reported literature for anti-HIV agents containing pyrazole as a core or substituted derivatives.
Results:
This review article has shown the comprehensive compilation of 220 compounds containing
pyrazole nucleus and possessing anti-HIV activity by sorting approximately 40 research articles from
2001 to date. 1-(4-Benzoylpiperazin-1-yl)-2-(4-fluoro-7-(1H-pyrazol-3-yl)-1H-pyrrolo[2,3-c]pyridin-
3-yl)ethane-1,2-dione (13), 3-(3-(2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl)-4-fluoro-1H-pyrrolo[2,3-
c]pyridin-7-yl)-1H-pyrazole-5-carboxamide (31), 3-(3-(2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl)-4-
fluoro-1H-pyrrolo[2,3-c]pyridin-7-yl)-1H-pyrazole-5-carboxamide (88), 3-cyanophenoxypyrazole
derivative (130), and 4-(4-chlorophenyl)-5-(4-methyl-5-((4-nitrophenyl)diazenyl)thiazol-2-yl)-3-
phenyl-5,6-dihydro-4H-pyrazolo[4,3-d]isoxazole (178) were the most potent mono-, di-, tri-, tetrasubstituted,
and fused pyrazole derivatives, respectively, which have shown potent anti-HIV activity
among all the described derivatives as compared with standard anti-HIV drugs.
Conclusion:
This review article provides an overview of the potential therapeutic activity of pyrazole
derivatives against HIV that will be helpful for designing pyrazole containing compounds for
anti-HIV activity.
Publisher
Bentham Science Publishers Ltd.