Synthesis and blood-schizontocidal antimalarial activities of 2-substituted/2,5-disubstituted-8-quinolinamines and some of their amino acid conjugates.
Thirteen new analogues (32-40, 45-48) of recently discovered potent blood-schizontocidal antimalarial agent, 2-tert-butylprimaquine (2) are synthesized and evaluated for in vivo antimalarial activities against drug-sensitive P. berghei strain and multi-drug resistant P. yoelii nigeriensis strain. Two of the amino acid conjugates (47-48) have exhibited potent antimalarial activities similar to that of 2 against both drug-sensitive and multi-drug resistant strains.
Jain
Meenakshi
M
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Punjab 160 062, India.
Vangapandu
Suryanarayana
S
Sachdeva
Sandeep
S
Jain
Rahul
R
D000596:Amino Acids / Q000737:chemistry / Q000494:pharmacology; D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D004351:Drug Resistance; D018432:Drug Resistance, Multiple; D010962:Plasmodium berghei / Q000187:drug effects; D010967:Plasmodium yoelii / Q000187:drug effects; D011319:Primaquine; D013329:Structure-Activity Relationship
D000596:Amino Acids; D000634:Aminoquinolines; D000962:Antimalarials; D011319:Primaquine