Design, Synthesis and Anti-Hiv-1 Evaluation of a Series of 5-Hydroxypyridine-4-One Derivatives As Possible Integrase Inhibitors

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Design, Synthesis and Anti-Hiv-1 Evaluation of a Series of 5-Hydroxypyridine-4-One Derivatives As Possible Integrase Inhibitors Publisher

Rostami M¹ ; Sirous H¹ ; Zabihollahi R² ; Aghasadeghi MR² ; Sadat SM² ; Namazi R² ; Saghaie L¹ ; Memarian HR³ ; Fassihi A¹

Show Affiliations

1. Department of Medicinal Chemistry, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan, 81746-73461, Iran
2. Department of Hepatitis and AIDS, Pasteur Institute of Iran, Tehran, Iran
3. Department of Chemistry, Faculty of Sciences, University of Isfahan, Isfahan, 81746-73441, Iran

Source: Medicinal Chemistry Research Published:2015

Abstract

A series of 5-hydroxypyridine-4-one derivatives were synthesized and subjected to HIV-1 replication inhibition assay. Docking studies provide a detailed molecular binding model for this class of compounds interacting with integrase enzyme. All of the derivatives were recognized potent in the docking studies in terms of both the estimated free energy change of binding and interactions with integrase key elements. 5a, 5c, 5d, 5h and 5n exhibited good anti-HIV-1 activities in cell-based assay. Compound 5d was the most potent derivative not only in vitro but also in silico. 5c and 5h offered the highest therapeutic indices. Suboptimal lipophilicity of 6b, 6g, 6i, 6j, 6l and 5m made them inactive in assays, despite the high activity in the docking studies. © 2015 Springer Science+Business Media New York.

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Style	Citing Format
MLA	Rostami M, et al.. "Design, Synthesis and Anti-Hiv-1 Evaluation of a Series of 5-Hydroxypyridine-4-One Derivatives As Possible Integrase Inhibitors." Medicinal Chemistry Research, vol. 24, no. 12, 2015, pp. 4113-4127.
APA	Rostami M, Sirous H, Zabihollahi R, Aghasadeghi MR, Sadat SM, Namazi R, Saghaie L, Memarian HR, Fassihi A (2015). Design, Synthesis and Anti-Hiv-1 Evaluation of a Series of 5-Hydroxypyridine-4-One Derivatives As Possible Integrase Inhibitors. Medicinal Chemistry Research, 24(12), 4113-4127.
Chicago	Rostami M, Sirous H, Zabihollahi R, Aghasadeghi MR, Sadat SM, Namazi R, Saghaie L, Memarian HR, Fassihi A. "Design, Synthesis and Anti-Hiv-1 Evaluation of a Series of 5-Hydroxypyridine-4-One Derivatives As Possible Integrase Inhibitors." Medicinal Chemistry Research 24, no. 12 (2015): 4113-4127.
Harvard	Rostami M et al. (2015) 'Design, Synthesis and Anti-Hiv-1 Evaluation of a Series of 5-Hydroxypyridine-4-One Derivatives As Possible Integrase Inhibitors', Medicinal Chemistry Research, 24(12), pp. 4113-4127.
Vancouver	Rostami M, Sirous H, Zabihollahi R, Aghasadeghi MR, Sadat SM, Namazi R, et al.. Design, Synthesis and Anti-Hiv-1 Evaluation of a Series of 5-Hydroxypyridine-4-One Derivatives As Possible Integrase Inhibitors. Medicinal Chemistry Research. 2015;24(12):4113-4127.
BibTex	@article{ author = {Rostami M and Sirous H and Zabihollahi R and Aghasadeghi MR and Sadat SM and Namazi R and Saghaie L and Memarian HR and Fassihi A}, title = {Design, Synthesis and Anti-Hiv-1 Evaluation of a Series of 5-Hydroxypyridine-4-One Derivatives As Possible Integrase Inhibitors}, journal = {Medicinal Chemistry Research}, volume = {24}, number = {12}, pages = {4113-4127}, year = {2015} }
RIS	TY - JOUR AU - Rostami M AU - Sirous H AU - Zabihollahi R AU - Aghasadeghi MR AU - Sadat SM AU - Namazi R AU - Saghaie L AU - Memarian HR AU - Fassihi A TI - Design, Synthesis and Anti-Hiv-1 Evaluation of a Series of 5-Hydroxypyridine-4-One Derivatives As Possible Integrase Inhibitors JO - Medicinal Chemistry Research VL - 24 IS - 12 SP - 4113 EP - 4127 PY - 2015 ER -

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