Polyprenylated phloroglucinol compounds as potent p-glycoprotein inducers
AssigneeCouncil of Scientific and Industrial Research
InventorsSandip BHARATE, Ajay KUMAR, Jaideep BHARATE, Prashant JOSHI, Abubakar WANI, Ramesh MUDUDUDDLA, Rohit SHARMA, Ram VISHWAKARMA
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Abstract
The present invention relates to the polyprenylated phloroglucinol compounds of formulae I and II. The present invention also provides synthesis and p-glycoprotein induction activity of the alkyl- and acyl-polyprenylated phloroglucinol compounds. Further, use of the compounds as p-glycoprotein inducers and methods of treatment of Alzheimer's disease using compounds of the invention are also provided.
Claims14
A compound of general formula I or II
- wherein R1 and R2 are individually selected from hydrogen, substituted or un-substituted alkyl group and substituted or un-substituted acyl group;
- alkyl group is selected from the group comprising of methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, isovaleryl, propargyl, allyl, prenyl, geranyl, and other long aliphatic chains with chain length from C5-C20;
- and
- acyl group is selected from the group comprising of acetyl, benzyl, benzoyl and butanoyl.
The compound as claimed in 1, wherein compound 1 b, 1g and 2b displayed EC50 of 8.9, 6.8 and 2.9 nM respectively.
A pharmaceutical composition for the treatment of Alzheimer's disease comprising;
- an effective amount of the compound of general formulae I or II optionally along with the pharmaceutically acceptable excipients.
Dependencies are inferred from the claim text.