N2-benzyloxycarbonylguan-9-yl acetic acid derivatives as HIV-1 reverse transcriptase non-nucleoside inhibitors with decreased loss of potency against common drug-resistance mutations

Kassim F. Adebambo; Samantha Zanoli; Michael G. Thomas; Reynel Cancio; Nicola M. Howarth; Giovanni Maga

doi:10.1002/cmdc.200700045

N²-benzyloxycarbonylguan-9-yl acetic acid derivatives as HIV-1 reverse transcriptase non-nucleoside inhibitors with decreased loss of potency against common drug-resistance mutations

Kassim F. Adebambo, Samantha Zanoli, Michael G. Thomas, Reynel Cancio, Nicola M. Howarth, Giovanni Maga

School of Engineering & Physical Sciences

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

8 Citations (Scopus)

Abstract

(Chemical Equation Presented) Beating the RT mutants: A novel class of N²-Cbz-guan-9-yl acetic acid derivatives is endowed with anti-HIV-1 reverse transcriptase (RT) activity in the low micromolar range. These compounds have improved efficacy towards drug-resistant RT mutants relative to nevirapine and efavirenz. Their unique scaffold and interesting resistance profiles warrant further development. © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.

Original language	English
Pages (from-to)	1405-1409
Number of pages	5
Journal	ChemMedChem
Volume	2
Issue number	10
DOIs	https://doi.org/10.1002/cmdc.200700045
Publication status	Published - 8 Oct 2007

Keywords

Antiviral agents
Drug resistance
Kinetic analysis
NNRTIs
Slow binding

UN SDGs

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

Access to Document

10.1002/cmdc.200700045

Cite this

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title = "N2-benzyloxycarbonylguan-9-yl acetic acid derivatives as HIV-1 reverse transcriptase non-nucleoside inhibitors with decreased loss of potency against common drug-resistance mutations",

abstract = "(Chemical Equation Presented) Beating the RT mutants: A novel class of N2-Cbz-guan-9-yl acetic acid derivatives is endowed with anti-HIV-1 reverse transcriptase (RT) activity in the low micromolar range. These compounds have improved efficacy towards drug-resistant RT mutants relative to nevirapine and efavirenz. Their unique scaffold and interesting resistance profiles warrant further development. {\textcopyright} 2007 Wiley-VCH Verlag GmbH & Co. KGaA.",

keywords = "Antiviral agents, Drug resistance, Kinetic analysis, NNRTIs, Slow binding",

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journal = "ChemMedChem",

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N²-benzyloxycarbonylguan-9-yl acetic acid derivatives as HIV-1 reverse transcriptase non-nucleoside inhibitors with decreased loss of potency against common drug-resistance mutations. / Adebambo, Kassim F.; Zanoli, Samantha; Thomas, Michael G. et al.
In: ChemMedChem, Vol. 2, No. 10, 08.10.2007, p. 1405-1409.

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

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AU - Zanoli, Samantha

AU - Thomas, Michael G.

AU - Cancio, Reynel

AU - Howarth, Nicola M.

AU - Maga, Giovanni

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KW - Kinetic analysis

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KW - Slow binding

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