99314-92-8Relevant academic research and scientific papers
HIV INTEGRASE INHIBITORS
-
Page/Page column 18, (2009/09/08)
Pyridopyrimidine carboxamide compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein R1, R2, R3, R4, R5 and R6 are defined herein. The compounds ar
Synthesis and mutagenic potency of structural isomers of 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine
Chrisman,Knize,Tanga
experimental part, p. 1641 - 1649 (2009/08/09)
(Chemical Equation Presented) Synthesis of 2-amino-1-methyl-6- phenylimidazo[4,5-b]pyridine (PhIP), three structural isomers, and two desphenyl PhIP congeners has been carried out. Mutagenic potency was evaluated using S. typhimurium strain TA98 in the Ames test. Mutagenic potency increased in relation to structural features in these heterocyclic amines that allow extended resonance between the phenyl and imidazo[4,5-b]pyridine N2-amino substituents. By contrast, PhIP isomers, whose substitution disallows involvement of the phenyl group in their ammoimidazo resonance hybrids, and desphenyl congeners were from 86- to 234-fold less mutagenic than PhIP.
3-Hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylates-fast access to a heterocyclic scaffold for HIV-1 integrase inhibitors
Kinzel, Olaf D.,Ball, Richard G.,Donghi, Monica,Maguire, Courtney K.,Muraglia, Ester,Pesci, Silvia,Rowley, Michael,Summa, Vincenzo
scheme or table, p. 6556 - 6558 (2009/04/05)
An efficient and reliable synthesis of the heterocyclic scaffold methyl-3-hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylate is described. The scope of the synthesis regarding the introduction of substituents on the pyrido-fused ring is explored.
HIV INTEGRASE INHIBITORS
-
Page/Page column 41, (2008/06/13)
Pyridopyrimidine carboxamide compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: Formula (I); wherein R1, R2, R3, R4, R5 and R6 are defined herein. The
