1-[2-(Diphenylmethoxy)ethyl]-2-methyl-5-nitroimidazole: a potent lead for the design of novel NNRTIs

R Silvestri; M Artico; S Massa; T Marceddu; F De Montis; P La Colla

doi:10.1016/s0960-894x(99)00664-2

1-[2-(Diphenylmethoxy)ethyl]-2-methyl-5-nitroimidazole: a potent lead for the design of novel NNRTIs

Bioorg Med Chem Lett. 2000 Feb 7;10(3):253-6. doi: 10.1016/s0960-894x(99)00664-2.

Authors

R Silvestri¹, M Artico, S Massa, T Marceddu, F De Montis, P La Colla

Affiliation

¹ Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Università di Roma La Sapienza, Rome, Italy.

PMID: 10698447
DOI: 10.1016/s0960-894x(99)00664-2

Abstract

A novel family of non-nucleoside reverse transcriptase inhibitors (NNRTIs) active at submicromolar concentrations was discovered. The new derivatives are 1-[2-(diarylmethoxy)ethyl]imidazoles bearing substituents both at benzene and imidazole rings. The most potent derivatives were those having nitro and methyl groups as substituents in the imidazole ring. Among 10 test derivatives compound 6d was found to be as potent as nevirapine and was selected as a lead for further studies.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-HIV Agents / chemical synthesis*
Anti-HIV Agents / pharmacology
Cell Line
Nitroimidazoles / chemical synthesis*
Nitroimidazoles / pharmacology
Reverse Transcriptase Inhibitors / chemical synthesis*
Reverse Transcriptase Inhibitors / pharmacology
Structure-Activity Relationship

Substances

1-(2-(diphenylmethoxy)ethyl)-2-methyl-5-nitroimidazole
Anti-HIV Agents
Nitroimidazoles
Reverse Transcriptase Inhibitors