Design , Synthesis, Molecular Docking, QSAR Studies and Anti Histaminic Activity of Novel Tetrahydro Carbazole Drivatives

The heterocyclic rings are having varied biological activities and prone to have significant importance in drug discovery. Present scheme of study was to develop novel antihistaminic agents from heterocyclic ring tetrahydrocarbazole. In the first scheme substituted N- tetrahydrocarbazoles were prepared from fischer- indole synthesis. In the second step N- substituted aromatic benzoyl derivatives were prepared , all the compounds were showed characteristic IR, NMR, MASS peaks in their corresponding regions. All the compounds were subjected to molecular docking studies by using VLife MDS software , version 4.5, receptor code 3RZE, the compounds were showed good negative dock scores. Antihistaminic activity was performed by using guinea pig ileum , the ligands TH3, TH6, TH8, TH10, TH11, TH14 were showed good percent inhibition remaining were showed moderate activity. The data was analysed by 3D QSAR studies, PLSR method was showed good result, the values of r2 = 0.9977, q2 = 0.0882, F- test-1709.37, Pred_ r2 = 3.3755, Pred_ r2 se=1.6625. The data was analysed by ANNOVA studies, the results were showed less variance. The compounds TH6,TH8,TH14 were taken as lead compounds for further studies.