Design of a series of bicyclic HIV-1 integrase inhibitors. Part 2: Azoles: Effective metal chelators

Giang Le; Nick Vandegraaff; David I. Rhodes; Eric D. Jones; Jonathan A V Coates; Neeranat Thienthong; Lisa J. Winfield; Long Lu; Xinming Li; Changjiang Yu; Xiao Feng; John J. Deadman

doi:10.1016/j.bmcl.2010.07.081

Design of a series of bicyclic HIV-1 integrase inhibitors. Part 2: Azoles: Effective metal chelators

Giang Le, Nick Vandegraaff, David I. Rhodes, Eric D. Jones, Jonathan A V Coates, Neeranat Thienthong, Lisa J. Winfield, Long Lu, Xinming Li, Changjiang Yu, Xiao Feng, John J. Deadman

Research output: Contribution to journal › Article › Research › peer-review

38 Citations (Scopus)

Abstract

Synthesis of a diverse set of azoles and their utilizations as an amide isostere in the design of HIV integrase inhibitors is described. The Letter identified thiazole, oxazole, and imidazole as the most promising heterocycles. Initial SAR studies indicated that these novel series of integrase inhibitors are amenable to lead optimization. Several compounds with low nanomolar inhibitory potency are reported.

Original language	English
Pages (from-to)	5909-5912
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	19
DOIs	https://doi.org/10.1016/j.bmcl.2010.07.081
Publication status	Published - 1 Oct 2010
Externally published	Yes

Keywords

Inhibitor
Integrase
Metal chelator
Synthesis

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2010.07.081

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Le, G., Vandegraaff, N., Rhodes, D. I., Jones, E. D., Coates, J. A. V., Thienthong, N., Winfield, L. J., Lu, L., Li, X., Yu, C., Feng, X., & Deadman, J. J. (2010). Design of a series of bicyclic HIV-1 integrase inhibitors. Part 2: Azoles: Effective metal chelators. Bioorganic and Medicinal Chemistry Letters, 20(19), 5909-5912. https://doi.org/10.1016/j.bmcl.2010.07.081

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doi = "10.1016/j.bmcl.2010.07.081",

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T1 - Design of a series of bicyclic HIV-1 integrase inhibitors. Part 2

T2 - Azoles: Effective metal chelators

AU - Le, Giang

AU - Vandegraaff, Nick

AU - Rhodes, David I.

AU - Jones, Eric D.

AU - Coates, Jonathan A V

AU - Thienthong, Neeranat

AU - Winfield, Lisa J.

AU - Lu, Long

AU - Li, Xinming

AU - Yu, Changjiang

AU - Feng, Xiao

AU - Deadman, John J.

PY - 2010/10/1

Y1 - 2010/10/1

N2 - Synthesis of a diverse set of azoles and their utilizations as an amide isostere in the design of HIV integrase inhibitors is described. The Letter identified thiazole, oxazole, and imidazole as the most promising heterocycles. Initial SAR studies indicated that these novel series of integrase inhibitors are amenable to lead optimization. Several compounds with low nanomolar inhibitory potency are reported.

AB - Synthesis of a diverse set of azoles and their utilizations as an amide isostere in the design of HIV integrase inhibitors is described. The Letter identified thiazole, oxazole, and imidazole as the most promising heterocycles. Initial SAR studies indicated that these novel series of integrase inhibitors are amenable to lead optimization. Several compounds with low nanomolar inhibitory potency are reported.

KW - Inhibitor

KW - Integrase

KW - Metal chelator

KW - Synthesis

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DO - 10.1016/j.bmcl.2010.07.081

M3 - Article

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SN - 0960-894X

VL - 20

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EP - 5912

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 19

ER -

Design of a series of bicyclic HIV-1 integrase inhibitors. Part 2: Azoles: Effective metal chelators

Abstract

Keywords

UN SDGs

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