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


Synthesis and biological screening of 3-chloro-2-piperazinylmethyl-N-aryl sulfonamide indole derivatives as 5-HT6 receptor ligands: Part III

Author(s): Ramakrishna V. S. Nirogi, Amol D. Deshpande, Anil K. Chindhe, Ramasastri Kambhampati, Anil K. Shinde, P. K. Dubey

In continuation to our earlier work and to improve upon the potentency of 2-piperazinylmethyl-N-aryl sulfonamide indole derivatives, a new series of compounds were taken up for synthesis by inserting halo group at 3rd position of indole. The critical intermediate 3-halo-2-formyl indole was achieved through the Vilsmerier reaction, which on further reductive amination followed by sulfonylation gave 3-chloro-2-piperazinylmethyl-N-aryl sulfonamide indole derivatives as a targeted series of compounds. The design, synthesis and their in-vitro affinity towards the 5-HT6 receptor is discussed in this communication.