Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors

Claudia Mugnaini; Fabrizio Manetti; José A Esté; Imma Clotet-Codina; Giovanni Maga; Reynel Cancio; Maurizio Botta; Federico Corelli

doi:10.1016/j.bmcl.2006.03.080

Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3541-4. doi: 10.1016/j.bmcl.2006.03.080. Epub 2006 Apr 18.

Authors

Claudia Mugnaini¹, Fabrizio Manetti, José A Esté, Imma Clotet-Codina, Giovanni Maga, Reynel Cancio, Maurizio Botta, Federico Corelli

Affiliation

¹ Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Via De Gasperi, 2 I-53100 Siena, Italy.

PMID: 16621553
DOI: 10.1016/j.bmcl.2006.03.080

Abstract

S-Aryl-S-DABO derivatives, a novel subclass of S-DABO anti-HIV-1 agents, were synthesized via Ullmann type reaction starting from the corresponding 2-thiouracils by the aid of microwave irradiation. The results of their evaluation as inhibitors of RT are reported together with their antiviral activity in cellular assays.

Publication types

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

MeSH terms

Anti-HIV Agents / chemical synthesis*
Anti-HIV Agents / pharmacology*
Anti-HIV Agents / radiation effects
Binding Sites
Cell Death / drug effects
Cell Line
HIV Reverse Transcriptase / antagonists & inhibitors
HIV-1 / drug effects*
Humans
Microbial Sensitivity Tests
Microwaves
Molecular Structure
Pyrimidines / chemical synthesis*
Pyrimidines / chemistry
Pyrimidines / pharmacology*
Reverse Transcriptase Inhibitors / chemical synthesis
Reverse Transcriptase Inhibitors / pharmacology
Reverse Transcriptase Inhibitors / radiation effects
Stereoisomerism
Structure-Activity Relationship

Substances

Anti-HIV Agents
Pyrimidines
Reverse Transcriptase Inhibitors
HIV Reverse Transcriptase