Amberlyst-15 catalyzed Povarov reaction of N-arylidene-1H-indazol-6-amines and indoles: a greener approach to the synthesis of exo-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinolines as potential sirtuin inhibitors

Autor: Jakeer Pasha, Srinivas Oruganti, Saikat Sen, Sushmitha Bujji, Devyani Haldar, Bhaskar Kandagatla, Guru Pavan Kumar Seerapu, Srinivas Nanduri
Rok vydání: 2015
Předmět:
Zdroj: Tetrahedron Letters. 56:2289-2292
ISSN: 0040-4039
Popis: Amberlyst® 15(H) has been shown for the first time to be effective as a greener catalyst in promoting the Povarov reaction between an imine, derived from the aryl/heteroaryl aldehydes and 1H-indazol-6-amine, and indole/5-bromo-1H-indole. Representative candidates from the library of exo-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinolines, thus synthesized, were tested for their sirtuin (Sir-2) inhibitory activity using a yeast based assay. Among the ten compounds investigated in the assay, those derived from 5-bromoindole exhibited a higher degree of Sir-2 inhibition as compared to their analogs, derived from indole.
Databáze: OpenAIRE