volume 30 issue 12 pages 2270-2277

2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties

Arthur A. Santilli 1
1
 
Research Division, Wyeth Laboratories, Inc., Radnor, Pennsylvania 19087.
Publication typeJournal Article
Publication date1987-12-01
scimago Q1
wos Q1
SJR1.801
CiteScore11.5
Impact factor6.8
ISSN00222623, 15204804
PubMed ID:  3681897
Drug Discovery
Molecular Medicine
Abstract
The syntheses of 2-oxo-1,8-naphthyridine-3-carboxylic acid derivatives having potent gastric antisecretory properties in the pyloric-ligated (Shay) rat model are described. Two of the more potent compounds tested that were selected for more detailed dose-response evaluation were 4-amino-1-ethyl-1,2-dihydro-2-oxonaphthyridine-3-carboxylic acid ethyl ester (35) and 1-ethyl-1,2-dihydro-7-methyl-4-(4-methyl-1-piperazinyl)-2- oxo-1,8-naphthyridine-3-carboxylic acid ethyl ester (77). These compounds lowered total acid output in the rat in a dose-related fashion. Both compounds were more potent than cimetidine when tested in the rat. Both 35 and 77 showed inhibitory activity in food-stimulated acid secretion in the Pavlov-pouch, conscious dog. The mechanism of action for this series is not known. Details of structure-activity relationships are described.
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GOST |
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GOST Copy
Santilli A. A. et al. 2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties // Journal of Medicinal Chemistry. 1987. Vol. 30. No. 12. pp. 2270-2277.
GOST all authors (up to 50) Copy
Santilli A. A. 2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties // Journal of Medicinal Chemistry. 1987. Vol. 30. No. 12. pp. 2270-2277.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1021/jm00395a015
UR - https://doi.org/10.1021/jm00395a015
TI - 2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties
T2 - Journal of Medicinal Chemistry
AU - Santilli, Arthur A.
PY - 1987
DA - 1987/12/01
PB - American Chemical Society (ACS)
SP - 2270-2277
IS - 12
VL - 30
PMID - 3681897
SN - 0022-2623
SN - 1520-4804
ER -
BibTex |
Cite this
BibTex (up to 50 authors) Copy
@article{1987_Santilli,
author = {Arthur A. Santilli},
title = {2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties},
journal = {Journal of Medicinal Chemistry},
year = {1987},
volume = {30},
publisher = {American Chemical Society (ACS)},
month = {dec},
url = {https://doi.org/10.1021/jm00395a015},
number = {12},
pages = {2270--2277},
doi = {10.1021/jm00395a015}
}
MLA
Cite this
MLA Copy
Santilli, Arthur A., et al. “2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties.” Journal of Medicinal Chemistry, vol. 30, no. 12, Dec. 1987, pp. 2270-2277. https://doi.org/10.1021/jm00395a015.