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.
Tiwari
Ashok K
AK
Pharmacology Division, Taranaka, Indian Institute of Chemical Technology, Hyderabad 500607, India. astiwari@yahoo.com,
Kumbhare
Ravindra M
RM
Agawane
Sachin B
SB
Ali
Amtul Z
AZ
Kumar
K Vijay
KV
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