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Preparation and anti-HIV activity of N-3 amino substituted thymidine nucleoside analogs |
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| Authors: | Michel Maillard Jean-Claude Florent Marc Lemaî tre Francoise Begassat Alain Bugnicourt Chantal Ferrieux Christine Rombi Elizabeth Pacaud Dominique Thierry Aurelio Zerial Claude Monneret David S. Grierson |
| Affiliation: | a Institut de Chimie des Substances Naturelles CNRS, ave de la Terrasse, 91198 Gifsur-Yvette, France b Service de Chimie, CNRS, URA 1387, Institut Curie, Section de Biologie, 26 rue d'Ulm, Paris Cedes 05 France c Rhône-Poulenc Rorer S.A., CVRA, 13 Quai Jules Guesda, BP 14, 94403 Vitry-sur-Seine Cedex, France d SARAM, IPSN, CBN, BP 6, 92260 Fontenay-aus-Rose France |
| Abstract: | The N-3 amino derivatives of ddT, AZT, 3′-FddT, and D4T were prepared by electrophilic amination of the parent compounds. Although compounds , , and were essentially inactive, N-3 amino AZT (RP67042) maintained activity and displayed lower toxicity and a longer plasmatic halflife compared to AZT. |
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