Synthesis and biological evaluation of a novel structural type of serotonin 5-HT3 receptor antagonists.
A series of novel 3-substituted quinoxalin-2-carboxamides were designed as per the pharmacophoric requirement for 5-HT(3) receptor antagonists and prepared by microwave irradiation and also by conventional method. The compounds were characterized by spectral data (IR, (1)H NMR, and MS) and the purity was ascertained by microanalysis. The synthesized compounds were evaluated for 5-HT(3) antagonisms in longitudinal muscle-myenteric plexus preparation from guinea pig ileum against 5-HT(3) agonist, 2-methyl-5-HT. Among the test compounds, N-{3-[(4-methylpiperazin-1-yl)methyl]-4-hydroxyphenyl}-3-methoxyquinoxalin-2-carboxamide 4e showed most favorable 5-HT(3) receptor antagonism.
Venkatesha Perumal
Ramachandran
R
Department of Pharmaceutical Chemistry, Periyar College of Pharmaceutical Sciences for Girls, Trichirappalli-620 021, Tamil Nadu, India.
Mahesh
Radhakrishnan
R
D000818:Animals; D006168:Guinea Pigs; D008297:Male; D058831:Serotonin 5-HT3 Receptor Antagonists; D012702:Serotonin Antagonists / Q000737:chemistry / Q000494:pharmacology*; D013057:Spectrum Analysis / Q000379:methods
D058831:Serotonin 5-HT3 Receptor Antagonists; D012702:Serotonin Antagonists