4-(4-Cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as Selective Cyclooxygenase-2 Inhibitors:  Enhancement of the Selectivity by Introduction of a Fluorine Atom and Identification of a Potent, Highly Selective, and Orally Active COX-2 Inhibitor JTE-5221

2002 ◽  
Vol 45 (7) ◽  
pp. 1511-1517 ◽  
Author(s):  
Hiromasa Hashimoto ◽  
Katsuaki Imamura ◽  
Jun-ichi Haruta ◽  
Korekiyo Wakitani
2020 ◽  
Vol 7 (11) ◽  
pp. 1349-1357 ◽  
Author(s):  
Shuangshuang Xie ◽  
Changxing Qi ◽  
Yulin Duan ◽  
Qianqian Xu ◽  
Yaping Liu ◽  
...  

Cyclooxygenase-2 (COX-2) is a significant therapeutic target of chronic inflammatory diseases.


2021 ◽  
pp. 135965352110640
Author(s):  
D Andouard ◽  
R Gueye ◽  
S Hantz ◽  
C Fagnère ◽  
B Liagre ◽  
...  

Background Human cytomegalovirus (HCMV) is involved in complications on immunocompromised patients. Current therapeutics are associated with several drawbacks, such as nephrotoxicity. Purpose: As HCMV infection affects inflammation pathways, especially prostaglandin E2 (PGE2) production via cyclooxygenase 2 enzyme (COX-2), we designed 2'-hydroxychalcone compounds to inhibit human cytomegalovirus. Study design We first selected the most efficient new synthetic chalcones for their effect against COX-2-catalyzed PGE2. Study sample Among the selected compounds, we assessed the antiviral efficacy against different HCMV strains, such as the laboratory strain AD169 and clinical strains (naïve or multi-resistant to conventional drugs) and toxicity on human cells. Results The most efficient and less toxic compound (chalcone 7) was tested against HCMV in combination with other antiviral molecules: artesunate (ART), baicalein (BAI), maribavir (MBV), ganciclovir (GCV), and quercetin (QUER) using Compusyn software. Association of chalcone 7 with MBV and BAI is synergistic, antagonistic with QUER, and additive with GCV and ART. Conclusion These results provide a promising search path for potential bitherapies against HCMV.


1999 ◽  
Vol 42 (7) ◽  
pp. 1274-1281 ◽  
Author(s):  
W. Cameron Black ◽  
Christine Brideau ◽  
Chi-Chung Chan ◽  
Stella Charleson ◽  
Nathalie Chauret ◽  
...  

2000 ◽  
Vol 43 (16) ◽  
pp. 3168-3185 ◽  
Author(s):  
Ish K. Khanna ◽  
Yi Yu ◽  
Renee M. Huff ◽  
Richard M. Weier ◽  
Xiangdong Xu ◽  
...  

Cephalalgia ◽  
2004 ◽  
Vol 24 (5) ◽  
pp. 414-415 ◽  
Author(s):  
HC Siow

Chronic paroxysmal hemicrania (CPH) was first described by Sjaastad who also described a remitting form of this condition (1, 2). This new entity was named episodic paroxysmal hemicrania (EPH) in 1987 by Kudrow (3). It is characterized by brief, frequent attacks of unilateral orbital or temporal pain with associated autonomic symptoms. Most cases respond to indomethacin. A seasonal variant of EPH has been described (4), but never a response to treatment with cyclooxygenase (COX)-2 inhibitors.


1996 ◽  
Vol 6 (6) ◽  
pp. 725-730 ◽  
Author(s):  
W.C. Black ◽  
C. Bayly ◽  
M. Belley ◽  
C.-C. Chan ◽  
S. Charleson ◽  
...  

2000 ◽  
Vol 43 (2) ◽  
pp. 214-223 ◽  
Author(s):  
Carles Puig ◽  
María I. Crespo ◽  
Núria Godessart ◽  
Joan Feixas ◽  
Javier Ibarzo ◽  
...  

1996 ◽  
Vol 39 (9) ◽  
pp. 1846-1856 ◽  
Author(s):  
James J. Li ◽  
Monica B. Norton ◽  
Emily J. Reinhard ◽  
Gary D. Anderson ◽  
Susan A. Gregory ◽  
...  

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