title: alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
abstract: In a program to identify new anti-ulcer compounds, a series of N-acyl derivatives of alpha-amino acids were screened for their in vitro H(+)/K(+) ATPase inhibitory activity, and in vivo efficacy in Pylorus ligation model. 3D-QSAR studies were carried out and a representative compound 13 was studied for the nature of its proton pump inhibition.
authors.affiliation: Medicinal Chemistry Division, Central Drug Research Institute, Chattar Manzil Palace, Lucknow 226 001, India.
authors.forename: Preeti
authors.initials: P
authors.lastname: Sharma
authors.forename: Sangeeta
authors.initials: S
authors.lastname: Singh
authors.forename: Tanveer I
authors.initials: TI
authors.lastname: Siddiqui
authors.forename: Vishnu S
authors.initials: VS
authors.lastname: Singh
authors.forename: Bijoy
authors.initials: B
authors.lastname: Kundu
authors.forename: Philip
authors.initials: P
authors.lastname: Prathipati
authors.forename: Anil K
authors.initials: AK
authors.lastname: Saxena
authors.forename: Dinesh K
authors.initials: DK
authors.lastname: Dikshit
authors.forename: Leena
authors.initials: L
authors.lastname: Rastogi
authors.forename: Chetna
authors.initials: C
authors.lastname: Dixit
authors.forename: M B
authors.initials: MB
authors.lastname: Gupta
authors.forename: G K
authors.initials: GK
authors.lastname: Patnaik
authors.forename: Madhu
authors.initials: M
authors.lastname: Dikshit
mesh_terms: D009597:4-Nitrophenylphosphatase / Q000378:metabolism; D000255:Adenosine Triphosphate / Q000494:pharmacology; D000596:Amino Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005745:Gastric Acidity Determination; D005753:Gastric Mucosa / Q000187:drug effects / Q000201:enzymology; D066298:In Vitro Techniques; D008026:Ligation; D008297:Male; D008861:Microsomes / Q000187:drug effects / Q000201:enzymology; D008958:Models, Molecular; D009853:Omeprazole / Q000494:pharmacology; D054328:Proton Pump Inhibitors; D011708:Pylorus / Q000502:physiology; D021281:Quantitative Structure-Activity Relationship; D051381:Rats; D017207:Rats, Sprague-Dawley; D033921:Vesicular Transport Proteins / Q000378:metabolism
chemical_list: D000596:Amino Acids; D000897:Anti-Ulcer Agents; D004791:Enzyme Inhibitors; D054328:Proton Pump Inhibitors; D033921:Vesicular Transport Proteins; D000255:Adenosine Triphosphate; D009597:4-Nitrophenylphosphatase; D009853:Omeprazole