Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry


Synthesis of novel (1-substituted benzenesulfonyl-1H-indol-5-yl)-(4- substituted piperazin-1-yl)-methanone derivatives as 5-HT6R ligands

Author(s): Ramakrishna V. S. Nirogi1, Prabhakar Kothmirkar1, 2, Anil K. Shinde1*, Jagadish Babu K1, K. R. Sastry1 and P. K. Dubey2

(1H-Indol-5-yl)-(4-substituted piperazin-1-yl)-methanone derivatives, 6a and 6b were synthesized following the method given in Scheme - 1. Intermediates 6a & 6b were further reacted with substituted benzene sulfonyl chlorides to obtain the targeted compounds, (1- substituted benzenesulfonyl-1H-indol-5-yl)-(4-substitutedpiperazin-1-yl)-methanone derivatives 7a-m (Scheme - 2). All the synthesized compounds 7a-m were well characterized with spectral data and checked the in-vitro binding affinity towards 5-HT6 receptors. These compounds have shown mild to moderate potency towards serotonin 5-HT6 receptors and are considered as initial hits to do further modifications.