Averrhoa bilimbi Linn. fruit and its extracts were screened for antihypercholesterolemic activity using Triton-induced hypercholesterolemia in rats as a model. The fruit and its water extract, but not alcohol and hexane extracts, showed remarkable antihypercholesterolemic activity. An active fraction, which showed activity at a low dose of 0.8 mg/kg, was purified from the water extract. An active component was isolated from the active fraction, which showed optimum activity at a dose of 0.3 mg/kg. The efficacy of the fruit was tested in chronic high-fat diet fed hyperlipidemic rats. The fruit (125 mg/kg) as well as its water extract (50 mg/kg) were found to be effective in lowering lipids in the high-fat diet fed rats. The fruit was subjected to preliminary general toxicity evaluation in mice. Oral administration of the fruit homogenate daily for 15 days did not result in any toxic symptoms up to a dose of 1 g/kg studied. Thus, this fruit can be used as a dietary ingredient to prevent as well as treat hyperlipidemia.
One‐pot synthesis of heterocycle fused‐triazole analogs from the corresponding aldehydes and heteroarylhydrazines is demonstrated. Transformation of hydrazones to the desired systems was achieved by employing the oxidative cyclization with catalytic CuBr2 and oxone. This reaction condition is mild and selective, and a wide range of functional groups were able to sustain. An array of biologically important triazolopyridines, triazolopyridazines, triazolopyrimidines, and triazoloquinolines were obtained in fairly good yield.
Palladium catalyzed oxidative C-H arylation of heterocycle embedded thiophenes with aryl boronic acids is described. This method is found to display high C5-selectivity and thus enabled rapid access to 2,5disubstituted thiophenes. Furan analogs also exhibited a similar selectivity.
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