Synthesis of glycosylated beta-amino hydroxamates as new class of antimalarials.
Glycosylated beta-amino acids (3-18, 38, 39), obtained by hydrolysis of glycosylated beta-amino esters on reaction with hydroxylamine hydrochloride in presence of DIC/DCC afforded glycosyl beta-amino hydroxamates (19-34, 40, 41) in fair to good yields. Compounds (19-34, 40, 41) were screened against human malarial parasite Plasmodium falciparum in vitro for their schizontocidal activity. Compounds (19, 24, 26, 28, 40 and 41) exhibited good activity at 2 microg/mL concentrations.
Mishra
R C
RC
Division of Medicinal Chemistry, Central Drug Research Institute, Lucknow-226001, India.
Tripathi
Renu
R
Katiyar
Diksha
D
Tewari
Neetu
N
Singh
Deepti
D
Tripathi
R P
RP
D000596:Amino Acids; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D004912:Erythrocytes / Q000469:parasitology; D006031:Glycosylation; D006801:Humans; D019811:Hydroxylamine / Q000138:chemical synthesis* / Q000494:pharmacology; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects / Q000378:metabolism
D000596:Amino Acids; D000962:Antimalarials; D019811:Hydroxylamine