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

32 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

Access to Document

10.1016/j.bmcl.2010.07.081

Link to publication in Scopus

Cite this

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

Le, Giang ; Vandegraaff, Nick ; Rhodes, David I. ; Jones, Eric D. ; Coates, Jonathan A V ; Thienthong, Neeranat ; Winfield, Lisa J. ; Lu, Long ; Li, Xinming ; Yu, Changjiang ; Feng, Xiao ; Deadman, John J. / Design of a series of bicyclic HIV-1 integrase inhibitors. Part 2 : Azoles: Effective metal chelators. In: Bioorganic and Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 19. pp. 5909-5912.

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Design of a series of bicyclic HIV-1 integrase inhibitors. Part 2 : Azoles: Effective metal chelators. / Le, Giang; Vandegraaff, Nick; Rhodes, David I.; Jones, Eric D.; Coates, Jonathan A V; Thienthong, Neeranat; Winfield, Lisa J.; Lu, Long; Li, Xinming; Yu, Changjiang; Feng, Xiao; Deadman, John J.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 20, No. 19, 01.10.2010, p. 5909-5912.

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

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