alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
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.
Sharma
Preeti
P
Medicinal Chemistry Division, Central Drug Research Institute, Chattar Manzil Palace, Lucknow 226 001, India.
Singh
Sangeeta
S
Siddiqui
Tanveer I
TI
Singh
Vishnu S
VS
Kundu
Bijoy
B
Prathipati
Philip
P
Saxena
Anil K
AK
Dikshit
Dinesh K
DK
Rastogi
Leena
L
Dixit
Chetna
C
Gupta
M B
MB
Patnaik
G K
GK
Dikshit
Madhu
M
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
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