Synthesis and evaluation of novel sulfonamide derivatives as thromboxane A2 receptor antagonists I

DOI: 10.1016/0223-5234(94)90036-1

Source and publish data:

European Journal of Medicinal Chemistry p. 185 - 190 (1994)

Update date:2022-09-26

Topics:

Authors:

Sato, M.

Kawashima, Y.

Goto, J.

Yamane, Y.

Chiba, Y.

et al. et al.

Read Full Text PDF DownLoad Join now for total 90,000,000 free articles

Article abstract of DOI:10.1016/0223-5234(94)90036-1

A series of 4-<2-(arylsulfonylamino)ethylthio>phenoxyacetic acids and related compounds were synthesized.The compounds were tested for their thromboxane A₂ (TXA₂) receptor antagonizing effects on (15S)-15-hydroxy-11a,9a-(epoxymethano)prosta-5(Z),13(E)-dienoic acid (U-46619)-induced aggregation of rabbit platelet-rich plasma (PRP).Among the compounds synthesized, 3-<4-<2-(arylsulfonylamino)ethylthio>phenyl>propionic acids 26a-e,g showed potent TXA₂ receptor antagonist activity.The most potent compound, 3-<4-<2-(4-chlorophenylsulfonylamino)ethylthio>phenyl>propionic acid 26c was more than 10-fold more potent in TXA₂ receptor antagonizing activity (IC50 = 1.1*10⁶ M) than sulotroban (BM-13177) on rabbit platelets.Compound 26c was also more than 10-fold more potent in TXA₂-inhibitory activity than sulotroban on rat aorta smooth muscle (pA₂ 7.7) thromboxane A₂ / TXA₂ / receptor antagonist / sulfonamide derivative / sulotroban

Full text of DOI:10.1016/0223-5234(94)90036-1

Products guided by the article

Product name:N-phenylsulfonylcysteamine

Cas No:28196-75-0

R&D Labs maybe for 28196-75-0

Anhui Jiatiansen Agrochemical Co.,Ltd

Contact:15366811918

Address:chemical industrial park,xiangyu town,dongzhi county,anhui,china
Huayi Isotopes Co.

Contact:+ 86 512 52491118

Address:1 Fuyu Road, Haiyu TownChangshu, Jiangsu, China
Hunan Haili Chemical Industry Co.,Ltd.

Contact:+86-731-85521860

Address:No.251, 2nd Section, Furong Road, Changsha,Hunan,China
Kraeber & Co GmbH

Contact:+49-4101-3053-0

Address:Waldhofstrasse 14 ,25474 Ellerbek Germany
Phantom-pharma

Contact:

Address:

Relevant to this article

A facile and effective synthesis of α-(1→6)-linked mannose di-, tri-, tetra-, hexa-, octa-, and dodecasaccharides, and β-(1→6)-linked glucose di-, tri-, tetra-, hexa-, and octasaccharides using sugar trichloroacetimidates as the donors and unprotected or partially protected glycosides as the acceptors

Doi:10.1016/S0008-6215(01)00070-2
(2001)
Concise preparation of 1,8-diazaanthracene-2,7,9,10-tetraones. Two alternative syntheses of the natural antifolate diazaquinomycin A

Doi:10.1016/S0040-4020(00)00371-9
(2000)
Doi:10.1007/BF00470541
()
2-Aryl indole NK₁ receptor antagonists: Optimisation of the 2-aryl ring and the indole nitrogen substituent

Doi:10.1016/S0960-894X(01)00183-4
(2001)
Brightening up Circularly Polarized Luminescence of Monosubstituted Polyacetylene by Conformation Control: Mechanism, Switching, and Sensing

Doi:10.1002/anie.202108010
(2021)
Palladium-catalysed heteroannulation with terminal alkynes: A highly regio- and stereoselective synthesis of (Z)-3-aryl(alkyl)idene isoindolin-1- ones

Doi:10.1016/S0040-4020(00)00359-8
(2000)

Article Doi