title: Identification of quinoline-chalcone hybrids as potential antiulcer agents.
abstract: Antiulcer activity of novel quinoline-chalcone hybrids (13-37) was investigated. Among them, eight compounds (14, 16, 17, 23, 29, 31, 32 and 35) were found to be active in various ulcer models in Sprague-Dawley (SD) rats. To understand the mechanism of action of these hybrids, the effects of the compounds on antisecretory and cytoprotective activities were studied. All these active hybrids improved the depleted levels of mucin and consequently inhibited the formation of erosions in a pyloric ligated ulcer model. In addition, they also significantly increased the gastric PGE2 content in an aspirin induced ulcer model. The additional experiments including the in vitro metabolic stability and in vivo pharmacokinetics led to the identification of compound 17 as an orally active and safe candidate that is worthy of further investigation to be developed as an antiulcer agent.
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India. Electronic address: sashidhar123@gmail.com.
authors.forename: Koneni V
authors.initials: KV
authors.lastname: Sashidhara
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Srinivasa Rao
authors.initials: SR
authors.lastname: Avula
authors.affiliation: Pharmacology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Vaibhav
authors.initials: V
authors.lastname: Mishra
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Gopal Reddy
authors.initials: GR
authors.lastname: Palnati
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: L Ravithej
authors.initials: LR
authors.lastname: Singh
authors.affiliation: Pharmacology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Neetu
authors.initials: N
authors.lastname: Singh
authors.affiliation: Pharmacokinetics and Metabolism Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Yashpal S
authors.initials: YS
authors.lastname: Chhonker
authors.affiliation: Medicinal Chemistry Division, National Institute of Pharmaceutical Education and Research (NIPER), Raebareli 229 010, India.
authors.forename: Priyanka
authors.initials: P
authors.lastname: Swami
authors.affiliation: Pharmacokinetics and Metabolism Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: R S
authors.initials: RS
authors.lastname: Bhatta
authors.affiliation: Pharmacology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Gautam
authors.initials: G
authors.lastname: Palit
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000897:Anti-Ulcer Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D001241:Aspirin; D002599:Chalcone / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D015394:Molecular Structure; D015363:Quinolones / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013276:Stomach Ulcer / Q000139:chemically induced / Q000188:drug therapy*
chemical_list: D000897:Anti-Ulcer Agents; D015363:Quinolones; D002599:Chalcone; D001241:Aspirin
keywords: Antiulcer activity; Chalcone; Pharmacokinetic studies; Quinoline