Design and synthesis of substituted 2-naphthyloxyethylamines as potential 5-HT 1A antagonists
Department of Pharmaceutical Chemistry, Prin. K. M. Kundnani College of Pharmacy, Cuffe Parade, Mumbai - 400 005, India
Urmila J Joshi Department of Pharmaceutical Chemistry, Prin. K. M. Kundnani College of Pharmacy, Mumbai - 400 005 India E-mail: [email protected]
Although 5-HT 1A antagonists are known to be useful in the treatment of depression, no specific 5-HT 1A antagonist is available clinically. Propranolol is one of the important ligands acting at the presynaptic 5-HT 1A receptor. This article deals with the design of 5-HT 1A antagonists based on propranolol using the pharmacophoric requirements of the receptor and the other SAR data, synthesis of these compounds and their preliminary evaluation for the 5-HT 1A antagonistic activity against a specific partial agonist. This was done by measuring the reversal of agonist-induced hypothermia in mice. The synthesized compounds showed a promising 5-HT 1A antagonistic activity.