title: Syntheses, characterization and evaluation of novel 2,6-diarylpiperidin-4-ones as potential analgesic-antipyretic agents.
abstract: A novel series of N-(N-methylpiperazinoacetyl)-2,6-diarylpiperidin-4-one derivatives (1c-3c and 5c) were synthesized, via base catalyzed nucleophilic substitution of N-chloroacetyl-2,6-diarylpiperidin-4-ones (1b-6b) with N-methyl piperazine. The newly synthesized compounds were characterized by FTIR, Mass and NMR spectral studies. All the compounds were screened for their possible analgesic and antipyretic activities. The compound 2c exhibited promising antipyretic activity, comparable to that of paracetamol at 60 mg/kg dose. The compounds 2b and 2c showed significant analgesic profile at a dose of 60 mg/kg and were also found to be more potent than the reference drug, diclofenac sodium. Thus, it can be concluded that the synthesized 2,6-diarylpiperidin-4-ones exhibit promising antipyretic and analgesic activities and could be potential drug candidates.
authors.affiliation: Division of Pharmaceutical Chemistry, Faculty of Pharmacy, Babu Banarasi Das Northern India Institute of Technology, Lucknow 226028, Uttar Pradesh, India.
authors.forename: Purnima
authors.initials: P
authors.lastname: Tripathi
authors.affiliation: Division of Pharmaceutical Chemistry, Faculty of Pharmacy, Babu Banarasi Das Northern India Institute of Technology, Lucknow 226028, Uttar Pradesh, India.
authors.forename: Avinash C
authors.initials: AC
authors.lastname: Tripathi
authors.affiliation: Division of Pharmaceutical Chemistry, Faculty of Pharmacy, Babu Banarasi Das Northern India Institute of Technology, Lucknow 226028, Uttar Pradesh, India.
authors.forename: Viney
authors.initials: V
authors.lastname: Chawla
authors.affiliation: Division of Pharmaceutical Chemistry, Faculty of Pharmacy, Babu Banarasi Das Northern India Institute of Technology, Lucknow 226028, Uttar Pradesh, India. Electronic address: dirpharmniec@gmail.com.
authors.forename: Shailendra K
authors.initials: SK
authors.lastname: Saraf
mesh_terms: D019342:Acetic Acid; D000700:Analgesics / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D058633:Antipyretics / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D001831:Body Temperature / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D005334:Fever / Q000188:drug therapy*; D008297:Male; D051379:Mice; D010146:Pain / Q000139:chemically induced / Q000188:drug therapy*; D010147:Pain Measurement; D010879:Piperazines / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D010880:Piperidines / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D012007:Rectum / Q000503:physiopathology
chemical_list: D000700:Analgesics; D058633:Antipyretics; C000595841:N-(N-methylpiperazinoacetyl)-2,6-diarylpiperidin-4-one; D010879:Piperazines; D010880:Piperidines; D019342:Acetic Acid
keywords: 2,6-Diarylpiperidin-4-one; Analgesic; Antipyretic; Mannich reaction; N-methyl piperazine; Piperidin-4-one