Reduction in post-prandial hyperglycemic excursion through alpha-glucosidase inhibition by beta-acetamido carbonyl compounds.
A series of beta-acetamido carbonyl compounds (S(1)-S(7)) were prepared using Dakin-West reaction from different substituted aldehyde and acetophenone in the presence of lanthanum triflate as a solid catalyst. All the compounds were tested for their alpha-glucosidase inhibitory potential against rat intestinal alpha-glucosidase. The most potent rat intestinal alpha-glucosidase inhibitors S(5) and S(7) were tested for their antihyperglycemic activity following carbohydrate tolerance test. Both the compounds displayed antihyperglycemic activity equivalent to the standard drug acarbose.
Pharmacology Division, Taranaka, Indian Institute of Chemical Technology, Hyderabad 500607, India. astiwari@yahoo.com,
Ashok K
AK
Tiwari
Ravindra M
RM
Kumbhare
Sachin B
SB
Agawane
Amtul Z
AZ
Ali
K Vijay
KV
Kumar
D020909:Acarbose / Q000737:chemistry; D000081:Acetamides / Q000737:chemistry*; D000818:Animals; D002241:Carbohydrates / Q000737:chemistry; D002244:Carbon / Q000737:chemistry*; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy; D015195:Drug Design; D065089:Glycoside Hydrolase Inhibitors; D006943:Hyperglycemia / Q000188:drug therapy / Q000378:metabolism*; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D007422:Intestines / Q000201:enzymology*; D008956:Models, Chemical; D019518:Postprandial Period; D051381:Rats; D000520:alpha-Glucosidases / Q000737:chemistry*
D000081:Acetamides; D002241:Carbohydrates; D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents; D002244:Carbon; D000520:alpha-Glucosidases; D020909:Acarbose