Synthesis and antihyperlipaemic activity of some novel N-cyanovinylformamidines.
Potent antihyperlipaemic activity has been observed in a series of novel N-cyanovinylformamidines when tested in hyperlipaemic rats. Two of the compounds (11 and 15) were found more potent than gemfibrozil at 50 mg/kg/d dose level in reducing serum cholesterol and triglyceride levels and also in elevating serum HDL level. A good three-dimensional structural similarity has been observed between these two compounds and clofibrate and gemfibrozil, respectively. Acute toxicity studies carried out in mice indicated compound 11 to be safe even at a dose level of 4.5 g/kg. The title compounds were synthesized by the reaction of alpha-cyanoketene S,N-acetals with formamidineacetate under controlled reaction conditions.
Shishoo
C J
CJ
Department of Pharmaceutical Chemistry, L.M. College of Pharmacy, Ahmedabad, India.
Chhabria
M T
MT
Gandhi
T P
TP
Bangaru
R A
RA
D000818:Animals; D002784:Cholesterol / Q000097:blood; D005260:Female; D005559:Formamides / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D015248:Gemfibrozil / Q000494:pharmacology; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D008958:Models, Molecular; D051381:Rats; D017208:Rats, Wistar; D013055:Spectrophotometry, Infrared; D014280:Triglycerides / Q000097:blood
D005559:Formamides; D000960:Hypolipidemic Agents; D014280:Triglycerides; D002784:Cholesterol; D015248:Gemfibrozil