Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-[3-(3-pyridinyl)propyl]octanoic acid and analogs
1
Research Department Pharmaceuticals Division CIBA-GEIGY Corporation Summit, New Jersey 07901
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Publication type: Journal Article
Publication date: 1992-11-01
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
1447738
Drug Discovery
Molecular Medicine
Abstract
The title compound (10a) and its analogs were synthesized and found to possess two activities, the inhibition of the biosynthesis of thromboxane A2 and antagonism of its receptors. The in vitro and in vivo profile of these compounds as thromboxane receptor antagonists (TxRAs) and thromboxane synthase inhibitors (TxSIs) is described. 10a and its analogs displayed very potent TxRA activity in human washed platelets (IC50 approximately 10(-7)-10(-9) M) and dog saphenous vein (pA2 approximately 9) and also potent TxSI activity (IC50 approximately 10(-9) M). The good bioavailability and the long duration of action of some of these compounds was demonstrated using ex vivo measurement of the TxRA activity upon oral administration to guinea pigs. Compounds 10a, 20, and 33 potently inhibited arachidonic acid induced bronchoconstriction in guinea pigs.
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15
Total citations:
15
Citations from 2024:
1
(6.67%)
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Bhagwat S. S. et al. Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-[3-(3-pyridinyl)propyl]octanoic acid and analogs // Journal of Medicinal Chemistry. 1992. Vol. 35. No. 23. pp. 4373-4383.
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Bhagwat S. S. Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-[3-(3-pyridinyl)propyl]octanoic acid and analogs // Journal of Medicinal Chemistry. 1992. Vol. 35. No. 23. pp. 4373-4383.
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RIS
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TY - JOUR
DO - 10.1021/jm00101a015
UR - https://doi.org/10.1021/jm00101a015
TI - Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-[3-(3-pyridinyl)propyl]octanoic acid and analogs
T2 - Journal of Medicinal Chemistry
AU - Bhagwat, Shripad S.
PY - 1992
DA - 1992/11/01
PB - American Chemical Society (ACS)
SP - 4373-4383
IS - 23
VL - 35
PMID - 1447738
SN - 0022-2623
SN - 1520-4804
ER -
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BibTex (up to 50 authors)
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@article{1992_Bhagwat,
author = {Shripad S. Bhagwat},
title = {Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-[3-(3-pyridinyl)propyl]octanoic acid and analogs},
journal = {Journal of Medicinal Chemistry},
year = {1992},
volume = {35},
publisher = {American Chemical Society (ACS)},
month = {nov},
url = {https://doi.org/10.1021/jm00101a015},
number = {23},
pages = {4373--4383},
doi = {10.1021/jm00101a015}
}
Cite this
MLA
Copy
Bhagwat, Shripad S., et al. “Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-[3-(3-pyridinyl)propyl]octanoic acid and analogs.” Journal of Medicinal Chemistry, vol. 35, no. 23, Nov. 1992, pp. 4373-4383. https://doi.org/10.1021/jm00101a015.