1. Pharmacophore Based Synthesis of 3-Chloroquinoxaline-2-carboxamides as Serotonin3 (5-HT3) Receptor Antagonist
- Author
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Ramachandran Venkatesha Perumal, Pandi Vijaya Pandi, and Radhakrishnan Mahesh
- Subjects
Male ,Agonist ,Serotonin ,medicine.drug_class ,Stereochemistry ,Guinea Pigs ,Myenteric Plexus ,Pharmaceutical Science ,Mannich base ,In Vitro Techniques ,Pharmacology ,Structure-Activity Relationship ,chemistry.chemical_compound ,5-HT3 Receptor Antagonist ,Ileum ,Quinoxalines ,Animals ,Serotonin 5-HT3 Receptor Antagonists ,Medicine ,Structure–activity relationship ,Receptor ,Molecular Structure ,business.industry ,Antagonist ,Muscle, Smooth ,General Medicine ,chemistry ,Serotonin Antagonists ,Pharmacophore ,business ,Muscle Contraction - Abstract
A series of 3-chloroquinoxaline-2-carboxamides were designed and prepared by the condensation of 3-chloro-2-quinoxaloylchloride with appropriate Mannich bases of the p-aminophenol in the microwave environment. The synthesized compounds were evaluated for serotonin(3) (5-HT(3)) receptor antagonistic activities in longitudinal muscle-myenteric plexus (LMMP) preparation from guinea pig ileum against the 5-HT(3) agonist, 2-methyl-5-HT. Compound 3g exhibited comparable 5-HT(3) antagonistic activity (pA(2) 6.4) to that of standard antagonist Ondansetron (pA(2) 6.9), while the other compounds exhibited mild to moderate 5-HT(3) antagonistic activities.
- Published
- 2004