Work

Synthesis and Anti-HIV Activity of Some Heterodimers [NRTI]-Glycyl-Succinyl-[Trovirdine Analogue] of Known HIV-1 Reverse Transcriptase Inhibitors

Year: 2003

Type: article

Abstract: Expected for their ability to inhibit HIV replication, four heterodimers with a Nucleoside Reverse Transcriptase Inhibitor (NRTI) and a Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) bound by a linker arm were designed and synthesized. For the NRTIs, d4U, d2U, d4T and 5'-O-acetyl-5-(3-hydroxypropynyl)d2U were chosen. For the NNRTI, a Trovirdine Analogue (belonging to the phenethylthiazolylthiourea class) was chosen. The conjugation of the two different inhibitors (NRTI and NNRTI) was performed using the succinyl-glycine moiety as a spontaneously cleavable linker.

Source: Journal of Enzyme Inhibition and Medicinal Chemistry

DOI: 10.1080/1475636032000069846

Authors: Elena Sugeac, Christine Fossey, Daniel Ladurée, Sylvie Schmidt, Geraldine Laumond, Anne-marie Aubertin

Institution: Centre d'Etudes et de Recherche sur le Médicament de Normandie

Language: English

Topic: HIV/AIDS drug development and treatment

Subfield: Infectious Diseases

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: bronze

Funder: Styrelsen för Internationellt Utvecklingssamarbete