Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants.

doi:10.1021/jm0708230

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Community

Back to search

Article

Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants.

Journal of medicinal chemistry - 27 Dec 2007

Mugnaini Claudia, Alongi Maddalena, Togninelli Andrea, Gevariya Harsukh, Brizzi Antonella, Manetti Fabrizio, Bernardini Cesare, Angeli Lucilla, Tafi Andrea, Bellucci Luca, Corelli Federico, Massa Silvio, Maga Giovanni, Samuele Alberta, Facchini Marcella, Clotet-Codina Imma, Armand-Ugón Mercedes, Esté José A, Botta Maurizio

Abstract excerpt

A series of novel S-DABO analogues, characterized by different substitution patterns at positions 2, 5, and 6 of the heterocyclic ring, were synthesized in a straightforward fashion by means of parallel synthesis and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). Most of the compounds proved to be highly active on the wild-type enzyme both in enzymatic and cellular assays, with one of...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Anti-HIV Agents

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to HIV-1

Share to HIV Reverse Transcriptase

Share to Pyrimidines

Share to Quantitative Structure-Activity Relationship

Share to Recombinant Proteins

Share to Reverse Transcriptase Inhibitors

Share to Sulfides

Source

Open in PubMed

Identifiers

PMID: 18052319
DOI: 10.1021/jm0708230

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants.PMID 18052319Read ↗

Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.Semantic proximity Read ↗

5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.Semantic proximity Read ↗

5-Alkyl-2-alkylamino-6-(2,6-difluorophenylalkyl)-3,4-dihydropyrimidin-4(3H)-ones, a new series of potent, broad-spectrum non-nucleoside reverse transcriptase inhibitors belonging to the DABO family.Semantic proximity Read ↗

Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.Semantic proximity Read ↗

A multidisciplinary approach for the identification of novel HIV-1 non-nucleoside reverse transcriptase inhibitors: S-DABOCs and DAVPs.Semantic proximity Read ↗

Recent Advances in the DABOs Family as Potent HIV-1 non-Nucleoside Reverse Transcriptase InhibitorsSemantic proximity Read ↗

Synthesis and biological evaluation of 6-substituted 5-alkyl-2-(phenylaminocarbonylmethylthio)pyrimidin-4(3H)-ones as potent HIV-1 NNRTIs.Semantic proximity Read ↗

Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.Semantic proximity Read ↗

Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.Semantic proximity Read ↗

Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.Semantic proximity Read ↗

Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C variant.Semantic proximity Read ↗

TSAO Compounds: The Comprehensive Story of a Unique Family of HIV- 1 Specific Inhibitors of Reverse TranscriptaseSemantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.