663953-28-4Relevant academic research and scientific papers
8-Quinolinamines and their pro prodrug conjugates as potent blood-schizontocidal antimalarial agents
Vangapandu, Suryanarayana,Sachdeva, Sandeep,Jain, Meenakshi,Singh, Savita,Singh, Prati Pal,Kaul, Chaman Lal,Jain, Rahul
, p. 4557 - 4568 (2003)
Synthesis and antimalarial activities of N 8-(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=C 8H17)] 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.
