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Your search keyword '"Radhakrishnan, Mahesh"' showing total 2 results
Start Over "Radhakrishnan, Mahesh" Topic medicine Journal bioorganicmedicinal chemistry letters
2 results on '"Radhakrishnan, Mahesh"'

1. Discovery of new anti-depressants from structurally novel 5-HT3 receptor antagonists: design, synthesis and pharmacological evaluation of 3-ethoxyquinoxalin-2-carboxamides

Author

Thangaraj Devadoss, Radhakrishnan Mahesh, Dilip Kumar Pandey, and Shvetank Bhatt

Subjects
Agonist, medicine.drug_class, Hydrochloride, Stereochemistry, Clinical Biochemistry, Guinea Pigs, Drug Evaluation, Preclinical, Pharmaceutical Science, Myenteric Plexus, Carboxamide, Pharmacology, Biochemistry, Chemical synthesis, 5-HT3 receptor, Piperazines, chemistry.chemical_compound, Structure-Activity Relationship, Quinoxalines, Drug Discovery, medicine, Animals, Serotonin 5-HT3 Receptor Antagonists, Molecular Biology, biology, Chemistry, Organic Chemistry, Antagonist, Ligand (biochemistry), Receptor antagonist, Amides, Antidepressive Agents, Drug Design, biology.protein, Molecular Medicine, Receptors, Serotonin, 5-HT3
Abstract

A novel series of 3-ethoxyquinoxalin-2-carboxamides were designed as per the pharmacophoric requirements of 5-HT(3) receptor antagonist using ligand-based approach. The desired carboxamides were synthesized from the key intermediate, 3-ethoxyquinoxalin-2-carboxylic acid by coupling with appropriate amines in the presence of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC·HCl) and 1-hydroxybenzotriazole (HOBt). The 5-HT(3) receptor antagonism was evaluated in longitudinal muscle myenteric plexus preparation from guinea pig ileum against 5-HT(3) agonist, 2-methy-5-HT, which was expressed in the form of pA(2) values. Compound 6h (3-ethoxyquinoxalin-2-yl)(4-methylpiperazin-1-yl)methanone was found to be the most active compound, which expressed a pA(2) value of 7.7. In forced swim test, the compounds with higher pA(2) value exhibited good anti-depressant-like activity and compounds with lower pA(2) value failed to show activity as compared to the vehicle-treated group.

Published
2010

2. Microwave assisted synthesis of 2-(4-substituted piperazin-1-yl)-1,8-naphthyridine-3-carbonitrile as a new class of serotonin 5-HT3 receptor antagonists

Author

Ramachandran Venkatesha Perumal, Radhakrishnan Mahesh, and Pandi Vijaya Pandi

Subjects
Agonist, Male, Nitrile, Stereochemistry, medicine.drug_class, Clinical Biochemistry, Guinea Pigs, Neuromuscular Junction, Pharmaceutical Science, Myenteric Plexus, In Vitro Techniques, Microwave assisted, Biochemistry, Chemical synthesis, Medicinal chemistry, 5-HT3 receptor, Piperazines, Guinea pig, chemistry.chemical_compound, Structure-Activity Relationship, Ileum, Drug Discovery, Nitriles, medicine, Animals, Serotonin 5-HT3 Receptor Antagonists, Naphthyridines, Receptor, Microwaves, Molecular Biology, biology, Chemistry, Organic Chemistry, Biological activity, Muscle, Smooth, General Medicine, Microwave irradiation, biology.protein, Molecular Medicine, Serotonin, Piperidine, Serotonin Antagonists, Receptors, Serotonin, 5-HT3, Antagonism, Muscle Contraction
Abstract

A series of novel 2-(4-substituted piperazin-1-yl)-1,8-naphthyridine-3-carbonitrile 6 were prepared by microwave irradiation and conventional heating. The intermediate, 2-oxo-1,2-dihydro-1,8-naphthyridine-3-carbonitrile 3, was prepared from 2-aminonicotinaldehyde 1 and ethyl cyanoacetate 2 in the presence of piperidine under solvent free condition. The synthesized compounds were evaluated for 5-HT3 antagonisms in longitudinal muscle-myenteric plexus (LMMP) preparation from Guinea pig ileum against 5-HT3 agonist, 2-methyl-5-HT. Among the compounds tested, 2-(4-allylpiperazin-1-yl)-1,8-naphthyridine-3-carbonitrile 6d showed most favorable 5-HT3 receptor antagonism in the Guinea pig ileum.

Published
2004

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