Synthesis of certain heterodimers expected as HIV-1 reverse transcriptase inhibitors.
Expected for the ability to inhibit HIV replication, we report the synthesis of two heterodimers of the general formula: [2NRTI]-C5-GLY-SUCCINYL-Npiperazinyl-[NNRTI] (18, 19) containing both a Nucleoside Reverse Transcriptase Inhibitor (10, 11) and a Non-Nucleoside Reverse Transcriptase Inhibitor (8) [Trovirdine Analogue belonging of the phenethyl thiazolyl thiourea class] connected through the "succinyl-glycine" spontaneously cleavable linker.
Ladurée
D
D
Centre d'Etudes et de Recherche sur le Médicament de Normandie U.F.R. des Sciences Pharmaceutiques, Caen, France.
Sugeac
E
E
Fossey
C
C
Schmidt
S
S
Laumond
G
G
Aubertin
A M
AM
D019281:Dimerization; D015497:HIV-1 / Q000187:drug effects / Q000502:physiology*; D007202:Indicators and Reagents; D008958:Models, Molecular; D015394:Molecular Structure; D011725:Pyridines / Q000737:chemistry; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D014779:Virus Replication / Q000187:drug effects*
D007202:Indicators and Reagents; D011725:Pyridines; D018894:Reverse Transcriptase Inhibitors; C095511:trovirdine