SYNTHESIS OF C2-SYMMETRICAL INHIBITORS OF THE HIV-1 PROTEASE, WITH N,N'-SUBSTITUTED ETHYLENEDIAMIDE AND ETHYLENEDIAMINE LINKERS

Authors
MAZALEYRAT JP RAGE I SAVRDA J MOUNA M WAKSELMAN M BOULAY R LELIEVRE Y
Citation
Jp. Mazaleyrat et al., SYNTHESIS OF C2-SYMMETRICAL INHIBITORS OF THE HIV-1 PROTEASE, WITH N,N'-SUBSTITUTED ETHYLENEDIAMIDE AND ETHYLENEDIAMINE LINKERS, Bioorganic & medicinal chemistry letters, 4(5), 1994, pp. 653-656
Citations number
21
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
5
Year of publication
1994
Pages
653 - 656
Database
ISI
SICI code
0960-894X(1994)4:5<653:SOCIOT>2.0.ZU;2-U
Abstract
Coupling of Z-(L)-phenylalanine with either ethylenediamine or N,N-dim ethylethylenediamine, followed by N-deprotection and either direct cou pling with Z-(L)-valine or amide reduction prior to coupling, gave C2- symmetric compounds [Z-Val-Phe-N(R)CH2-]2 (R = H, CH3) and [Z-Val-Phe( PSICH2-N)-N(R)CH2-]2 (R = H, CH3, CH2COOH, CH2CH2OH) which were modera tely active inhibitors of the HIV-1 protease.