NOVEL ANALOGS OF 3-O-ACETYL-11-KETO-BETA-BOSWELLIC ACID

摘要

This invention relates to novel AKBA analogs of the formula I given below: Where in R1, R2, R3, R4 and R5 in each of the said analogs are: 1. R1-OCHO, R2-H, R3-COOH, R4 & R5-O 2. R1-OCOCH2Cl, R2-H, R3-COOH, R4 & R5-O 3. R1-5'-O-methylgalloyloxy, R2-H, R3-COOH, R4 & R5-O 4. R1-OCOCH2CH2COOH, R2-H, R3-COOH, R4 & R5-O 5. R1-8',9'-Dihydro-4'-hydroxycinnamoyloxy, R2-H, R3-COOH, R4 & R5-O 6. R1-4'-Hydroxycinnamoyloxy, R2-H, R3-COOH, R4 & R5-O 7. R1-3',4'-Dimethoxycinnamoyloxy, R2-H, R3-COOH, R4 & R5-O 8. R1-3',4'-Dihydroxy-5'-methoxycinnamoyloxy, R2-H, R3-COOH, R4 & R5-O 9. R1-OCOCH2NH(tert-BOC), R2-H, R3-COOCH3, R4 & R5-O 10. R1-OCOCH2NH2HCl, R2-H, R3-COOH, R4 & R5-O 11. R1-OCOCH(CH3)NH2HCl, R2-H, R3-COOH, R4 & R5-O 12. R1-H, R2-OH, R3-COOCH3, R4 & R5-O 13. R1-H, R2-Br, R3 COOCH3, R4 & R5-O 14. R1-CN, R2-H, R3-COOCH3, R4 & R5-O 15. R1-SH, R2-H, R3-COOCH3, R4& R5-O 16. R1 & R2-N(OH), R3-COOCH3, R4 & R5-O 17. R1 & R2-H & OCOCH3 R3-H, R4 & R5-O 18. R1-OCOCH3, R2-H R3-COOCH2CH2N(CH3)2, R4 & R5-O 19. R1-OCOCH3, R2-H R3-CONH2, R4 & R5-O 20. R1-OCOCH3, R2-H, R3-CONHNH2, R4 & R5-O 21. R1-OCOCH3, R2-H, R3-CONHCH2CH2NH2, R4 & R5-O 22. R1-OCOCH3, R2-H, R3-CONHCH2CH2OH, R4 & R5-O 23. R1-OCOCH3, R2-H, R3-CON(CH2CH2)2NH, R4 & R5-O 24. R1-OCOCH3, R2-H R3-NCO, R4 & R5-O 25. R1-OCOCH3, R2-H R3-NH2, R4 & R5-O 26. R1-OCOCH3, R2-H R3-CN, R4 & R5-O 27. R1-OH, R2-H R3-COOH, R4 & R5-OH & H These compounds exhibited 5-Lipoxigenase inhibitory properties and these compounds may be used in pharmaceutical compositions for therapeutic applications against a variety of inflammations and hypersensitivity-based human diseases including asthma, arthritis, bowel diseases such as ulcerative colitis and circulatory disorders such as shock and ischaemia. These compounds also inhibited the growth of Brine Shrimp in cultures, which may be considered as a positive indication for cytotoxicity and antitumor activity.