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Piroxicam Analogs: Design, Synthesis, Docking Study and Biological Evaluation as Promising Anti-HIV-1 Agents

[ Vol. 18 , Issue. 2 ]

Author(s):

Ali Imani, Sepehr Soleymani, Rouhollah Vahabpour, Zahra Hajimahdi* and Afshin Zarghi*   Pages 209 - 219 ( 11 )

Abstract:


Background: Taking the well-known drug, Piroxicam as a lead compound, we designed and synthesized two series of 1,2-benzothiazines 1,1-dioxide derivatives to assay their ability in inhibition of HIV-1 replication in cell culture.

Objective: In this study, we describe the synthesis, docking study and biological evaluation of 1,2- benzothiazines 1,1-dioxide derivatives.

Results: Most of the new compounds were active in the cell-based anti-HIV-1 assay with EC50 < 50 μM. Among them, compound 7g was found to be the most active molecule. Docking study using 3OYA pdb code on the most active molecule 7g with EC50 values of 10 μM showed a similar binding mode to the HIV integrase inhibitors.

Conclusion: Since all the compounds showed no remarkable cytotoxicity (CC50> 500 μM), the designed scaffold is promising structure for the development of new anti-HIV-1 agents.

Keywords:

Synthesis, docking, autodock Vina, 1, 2-benzothiazines 1, 1-dioxide, piroxicam, anti-HIV-1, integrase.

Affiliation:

Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Hepatitis and AIDS department, Pasteur institute of Iran, Tehran, Medical Lab Technology Department, School of Allied Medical Sciences, Shahid Beheshti University of Medical Sciences, Tehran, Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran



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