1-[2-(Diphenylmethoxy)ethyl]-2-methyl-5-nitroimidazole: a potent lead for the design of novel NNRTIs. NLM AIDSLINE Important note: Information in this article was accurate in 2000. The state of the art may have changed since the publication date.

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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. Unique Identifier : AIDSLINE MED/20162273
Silvestri R; Artico M; Massa S; Marceddu T; De Montis F; La Colla P; Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di; Studi Farmaceutici, Universita di Roma La Sapienza, Rome, Italy.


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.


Keywords: JOURNAL ARTICLE Anti-HIV Agents/*CHEMICAL SYNTHESIS/PHARMACOLOGY Cell Line Nitroimidazoles/*CHEMICAL SYNTHESIS/PHARMACOLOGY Reverse Transcriptase Inhibitors/*CHEMICAL SYNTHESIS/PHARMACOLOGY Structure-Activity Relationship Support, Non-U.S. Gov't

KWDjournalarticleanti-hivagents/KWDchemicalsynthesis/pharmacologycelllinenitroimidazoles/KWDchemicalsynthesis/pharmacologyreversetranscriptaseinhibitors/KWDchemicalsynthesis/pharmacologystructure-activityrelationshipsupport,non-uKWDsKWDgov't
000630
A0061952


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