Brajendra K. Tripathi

Synthesis and antihyperglycemic activity of suitably functionalized 3H-quinazolin-4-ones

A series of 2-sec-amino-3H-quinazolin-4-ones (4a-p) and 4-sec-amino-2-chloroquinazolines (5a-b) have been synthesized by nucleophilic substitution reaction of 2-chloro-4(3H)-quinazolones (3) and 2,4-dichloroquinazolines (2) with amines, respectively. Most of the synthesized compounds were evaluated for antihyperglycemic activity but only 4a,b,d,j,o displayed significant reduction in blood glucose level in streptozotocin and sucrose loaded rat models.

Reductive amination of glycosyl aldoses: synthesis of n-glycosylated β-glycosyl amino alcohols and their enzyme inhibitory effect.

Abstract Reductive amination of glycosyl aldehydes (1a–c, 2) with glycosyl amino esters (3a–c, 4) in the presence of sodium borohydride gave diglycosylated amino esters (5–15) in good yield. N‐Glycosyl‐glycosylated amino esters were reduced to the respective diglycosyl amino alcohols (16–26) with LiAlH4 in good yield. All the synthesized compounds were studied for their inhibitory effect, if any, against hepatic glucose‐6‐phosphatase, glycogen phosphorylase, and intestinal brush border membrane α‐glucosidase; among these compounds 7, 21, and 25 have shown marked inhibition on these enzymes, respectively. #CDRI Communication No. 6605.

HEPATOPROTECTIVE EFFECTS OF PICROLIV IN ALCOHOL-FED ALBINO RATS

Alcohol abuse is thought to be a risk factor for the cause of liver damage, hyperlipidemia and insulin resistance. An alcohol-fed rat model was developed by chronic administration of ethanol to rats which caused significant alteration in liver function as revealed by elevated serum transaminases, alkaline phosphatase, acid phosphatase, sorbitol dehydrogenase, glutamate dehydrogenase, lactate dehydrogenase and bilirubin and decline in total serum protein content over the control group after 25 days of feeding in both male and female rats. Hepatic glutathione, lipid peroxides, glutathione peroxidase, alcohol dehydrogenase, aldehyde dehydrogenase, glycogen and total protein in liver were also significantly altered. A slightly elevated fasting blood glucose profile, 1.5 fold higher serum insulin levels and impaired glucose tolerance was prevalent in ethanol treated rats. In the present study, the effect of picroliv, an irridoid glycosidic fraction of Picrorhiza kurroa, on the above said parameters of these alcoholic rats was studied. Picroliv significantly reverted most of the above said altered blood and hepatic parameters in the alcohol-fed male and female rats to almost normal levels.