| 摘要 |
<p>9-Alkyl-beta -carboline compounds (I) and their salts, solvates, hydrates, complex compounds, enantiomers, diastereomers and racemates, are new. 9-Alkyl-beta -carboline compounds of formula (I) and their salts, solvates, hydrates, complex compounds, enantiomers, diastereomers and racemates, are new. R 1>-R 16>, -CR 4>R 5>R 6>, -X-CR 4>R 5>R 6>, -X-R 4>, -CO-NH-R 16>, -CO-O-R 16>; R 2>, R 3>-H, -R 7>, -R 8>, -CR 9>R 10>R 11>, -CR 12>R 13>R 14>, -Y 1>-CR 9>R 10>R 11>, -Z-CR 12>R 13>R 14>, -Y 1>-R 15>, -Z-R 15>, -O-R 17>, -S-R 18>, -NH-R 19>, -CO-NH-R 20> or -CO-O-R 21>; X : -(CH 2) n-, -CH=CH-, -C?=C-, -CH 2-CO-, -CO- or -CO-CH 2-; Y 1>, Z : -(CH 2) m-, -CH=CH-, -C?=C-, -O-(CH 2) p-, -NH-(CH 2) q-, -NH-CO-, -CO- or -O-CO-; R 4>-R 15>e.g. -H, -OH, -OCH 3, -OC 2H 5, -OC 3H 7, -O-cyclo-C 3H 5, -OCH(CH 3)2, -OC(CH 3) 3, -OC 4H 9, -OPh, -OCH 2-Ph, -OCPh 3, -SH, -SCH 3, -SC 2H 5, -SC 3H 7, -S-cyclo-C 3H 5, -SCH(CH 3) 2, -SC(CH 3) 3, -NO 2, -F, -Cl, -Br, -I, -N 3, -CN, -OCN, -NCO, -SCN, -NCS, -CHO, -COCH 3, -COC 2H 5 or -COC 3H 7; R 4>-R 21>-CH 2F, -CHF 2, -CF 3, -CH 2Cl, -CH 2Br, -CH 2I, -CH 2-CH 2F, -CH 2-CHF 2, -CH 2-CF 3, -CH 2-CH 2Cl, -CH 2-CH 2Br, -CH 2-CH 2I, cyclo-C 3H 5, cyclo-C 4H 7, cyclo-C 5H 9, cyclo-C 6H 11, cyclo-C 7H 13 or cyclo-C 8H 15; m, p, q : 1-4; and n : 1-6. Full Definitions are given in the Definitions (Full Definitions) section. An independent claim is included for a pharmaceutical composition comprising (I) and/or its salt, a carrier, an auxiliary material and/or a solvent. [Image] ACTIVITY : Antiparkinsonian; Neuroprotective; Nootropic; Antimicrobial; Antithyroid; Endocrine-Gen; Cytostatic; Cerebroprotective; Cardiant; Anticonvulsant; Muscular-Gen; Gastrointestinal-gen.; CNS-gen. The neuroprotective effect of (I) was tested in central brain cells. The results showed that after 48 hours, in a control culture about 20% of the cells were killed and in a culture with 9-alkyl-beta -carboline only about 10% of the cells were killed. MECHANISM OF ACTION : Dopamine receptor stimulator.</p> |
