Studies on anti-hypercholesterolemic activity of Indanyl tetrazoles

Abstract

Introduction: Clinically useful non-steroidal antihyperlipidemic drugs are now in the market for the treatment of patients suffering from hypercholesterolemia. Indan acids, which belong to non-steroidal aryl alkanoic acids class acids have been reported to possess varying degrees of cholesterol lowering activity. Keeping the above points in view exploration for better anti-hypercholesterolemic activity of indanyl tetrazole derivatives was undertaken.

Methods: Five-week-old male albino Charles Foster rats (120± 10 g) for normocholesterolemic and seven-week-old rats (130±10g) for hypercholesterolemic studies were used. On the 0-day and 14th day, tail vein blood was drawn from the overnight fasted animals respectively. Biochemical measurements were carried out using biochemical kits (Span, India) and an automated biochemical analyzer (Vitros-250, Johnson and Johnson Co. USA).

Results: The compound - V and VI exhibited almost same significant level of cholesterol lowering (p<0.01) activity. On closer look its reveal that the compound-VI exhibit triglyceride lowering (p<0.01) activity among the groups around 14 days of treatment on normocholesterolemic rats. Test compound- V (p<0.05) and compound-VI (p<0.001) have significant anti-hyper-cholesterolemic activity while clofibrate has no such activity on hypercholesterolemic rats.

Conclusions: Indanyl tetrazole derivatives, 5-(62 -methoxyindan-12 -yl) methyltetrazole (V) and 5- (52 , 62 -dimethoxyindan-12 -yl) methyltetrazole (VI) were more promising than their analogs in respect to their anti-hypercholesterolemic activity.

DOI: http://dx.doi.org/10.3126/joim.v32i3.4956

Journal of Institute of Medicine, December, 2010; 32:3 24-29