184898-80-4Relevant academic research and scientific papers
Design, synthesis, biological evaluation, and computational studies of novel thiazolo-pyrazole hybrids as promising selective COX-2 inhibitors: Implementation of apoptotic genes expression for ulcerogenic liability assessment
Marzouk, Adel A.,Taher, Ehab S.,Shaykoon, Montaser Sh. A.,Lan, Ping,Abd-Allah, Walaa Hamada,Aboregela, Adel M.,El-Behairy, Mohammed Farrag
, (2021/04/19)
A novel series of thiazolo-pyrazole hybrids has been prepared and assessed for their in vitro COX-1/COX-2 inhibitory activity. Compound 6c exhibited the most selective COX-2 inhibition profile (SI of 264) not far of Celecoxib (2 9 4). In-vivo anti-inflamm
2-(1H-Pyrazol-1-yl)acetic acids as chemoattractant receptor-homologous molecule expressed on Th2 lymphocytes (CRTh2) antagonists
Andrés, Miriam,Bravo, Mónica,Buil, Maria Antonia,Calbet, Marta,Castillo, Marcos,Castro, Jordi,Eichhorn, Peter,Ferrer, Manel,Lehner, Martin D.,Moreno, Imma,Roberts, Richard S.,Sevilla, Sara
, p. 168 - 184 (2014/01/06)
In this manuscript, the synthesis and biological activity of a series of pyrazole acetic acid derivatives as CRTh2 antagonists is presented. Biological evaluation in vitro revealed that the pyrazole core showed in several cases a different structure-activity relationship (SAR) to that of related indole acetic acid. A potent series of ortho-sulfonyl benzyl substituents was found, from which compounds 27 and 63 were advanced to in vivo profiling.
