Synthesis and blood-schizontocidal antimalarial activities of 2-substituted/2,5-disubstituted-8-quinolinamines and some of their amino acid conjugates

Meenakshi Jain; Suryanarayana Vangapandu; Sandeep Sachdeva; Rahul Jain

doi:10.1016/j.bmc.2003.12.029

Synthesis and blood-schizontocidal antimalarial activities of 2-substituted/2,5-disubstituted-8-quinolinamines and some of their amino acid conjugates

Bioorg Med Chem. 2004 Mar 1;12(5):1003-10. doi: 10.1016/j.bmc.2003.12.029.

Authors

Meenakshi Jain¹, Suryanarayana Vangapandu, Sandeep Sachdeva, Rahul Jain

Affiliation

¹ Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Punjab 160 062, India.

PMID: 14980613
DOI: 10.1016/j.bmc.2003.12.029

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Amino Acids / chemistry
Amino Acids / pharmacology
Aminoquinolines / chemical synthesis*
Aminoquinolines / pharmacology*
Animals
Antimalarials / chemical synthesis*
Antimalarials / pharmacology
Drug Resistance
Drug Resistance, Multiple
Plasmodium berghei / drug effects
Plasmodium yoelii / drug effects
Primaquine
Structure-Activity Relationship

Substances

Amino Acids
Aminoquinolines
Antimalarials
Primaquine