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-steroidalaryl 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 14thday, 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.