8-Quinolinamines and Their pro prodrug conjugates as potent blood-Schizontocidal antimalarial agents☆

Add time:09/04/2019    Source:sciencedirect.com

Synthesis and antimalarial activities of N8-(4-amino-1-methylbutyl)-5-alkoxy-4-ethyl-6-methoxy-8-quinolinamines (5) and their pro prodrug analogues (6–7) prepared by covalently linking 5 to the redox-sensitive (8) and esterase-sensitive (9) linkers through the amide linkage are reported. The most effective 8-quinolinamines [5c (R=C5H11) and 5f (R=C8H17)] have exhibited in vitro and in vivo biological efficacy superior to that of the standard drug chloroquine against both drug-sensitive and drug-resistant malaria strains. Analogues 6–7 were evaluated for in vivo blood-schizontocidal activity as potential pro prodrug models for the primary amino group containing 8-quinolinamines (5). The most effective pro prodrug analogue (6c) has displayed promising activities against drug-sensitive and drug-resistant strains of Plasmodia in vivo.

We also recommend Trading Suppliers and Manufacturers of 4-QuinolinaMine, 7-chloro-, hydrochloride (1:1) (cas 114306-27-3). Pls Click Website Link as below: cas 114306-27-3 suppliers

Prev:Original articleDifferential expression on mitochondrial tryparedoxin peroxidase (mTcTXNPx) in Trypanosoma cruzi after ferrocenyl diamine hydrochlorides treatments
Next:Synthesis, antimalarial, antileishmanial, and antimicrobial activities of some 8-quinolinamine analogues)