Identification of novel alpha-glucosidase inhibitors by screening libraries based on N- [4-(benzyloxy) benzoyl] alanine derivatives.
A library of 72 compounds related to N- [4-(benzyloxy) benzoyl]alanine (I) was synthesized, prepared and screened for alpha-glucosidase inhibitory activity. Four compounds showed potent inhibition, six compounds moderate inhibition, and 16 were weak inhibitors. One compound, N- [4-(benzyloxy) benzoyl] serine, was found to be a potent inhibitor of alpha-glucosidase with 100% inhibition at 1 micro M. This inhibitor was at least five times more potent than the lead compound I.
Kundu
B
B
Divisions of Medicinal Chemistry and Biochemistry, Central Drug Research Institute, Lucknow, 226 001, India. bijoy_kundu@yahoo.com
Rastogi
S K
SK
Ahmad
R
R
Srivastava
A K
AK
D000409:Alanine; D020650:Combinatorial Chemistry Techniques; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology; D065089:Glycoside Hydrolase Inhibitors
D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D000409:Alanine