Fragment Based Approach for the Investigation of HIV-1 Integrase Inhibition

Abstract

HIV-1 integrase (IN) inhibition of a novel series of quinoline derivatives was investigated. The compounds were designed on the basis of quinoline molecular scaffolds that attempt to mimic the basic naphtyridine motif of the L-870810 HIV-1 IN inhibitor. It appeared that the IN inhibition of the novel compounds was limited by the electroacceptor substitution within quinoline. Although the compounds studied here indicate structural similarity to L-870810, they are much less efficient than this compound. This can be explained by differences in conformations and apparent magnesium complexing ability in the naphtyridine and quinoline based amides.

RP-HPLC determination of lipophilicity in series of quinoline derivatives

“…Compounds 39-49 were synthesized according to the procedure showed below [38,39]. The KolbeSchmidt reaction was used to generate the carboxylic acids which further reacted with the appropriate amine in presence of ethyldimethylaminopropyl carbodiimide (EDCI) to afford an amide.…”

Substituted Amides of Quinoline Derivatives: Preparation and Their Photosynthesis-inhibiting Activity

“…bis-[8-Hydroxy-2-methylquinoline-7-carboxylic acid]-1,2-etylamide (8). Product was obtained according to ref [27]. bis-[8-Hydroxy-2-methylquinoline-7-carboxylic acid]-1,3-propylamide (9).…”

A convenient and efficient C–OH bond activation, PdCl2(PPh3)2catalyzed, C–C bond formation of tautomerizable quinolinones with the aid of BOP reagent and boronic acids

“…[58][59][60][61] In addition, some compounds display substantial antiviral activity in HIV-infected cells, [62][63][64][65][66][67] anticancer, [68][69][70][71][72] antimalarial activities. 73-78 A number of methods have been developed for the synthesis of 2-35 substituted quinolines.…”