41167-60-6Relevant articles and documents
Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a]pyrimidine-5-carboxamide and Thieno[3,2- b]pyridine-5-carboxamide Cores
Childress, Elizabeth S.,Wieting, Joshua M.,Felts, Andrew S.,Breiner, Megan M.,Long, Madeline F.,Luscombe, Vincent B.,Rodriguez, Alice L.,Cho, Hyekyung P.,Blobaum, Anna L.,Niswender, Colleen M.,Emmitte, Kyle A.,Conn, P. Jeffrey,Lindsley, Craig W.
supporting information, p. 378 - 384 (2019/01/15)
A scaffold hopping exercise from a monocyclic mGlu2 NAM with poor rodent PK led to two novel heterobicyclic series of mGlu2 NAMs based on either a functionalized pyrazolo[1,5-a]pyrimidine-5-carboxamide core or a thieno[3,2-b]pyridine-5-carboxamide core. These novel analogues possess enhanced rodent PK, while also maintaining good mGlu2 NAM potency, selectivity (versus mGlu3 and the remaining six mGlu receptors), and high CNS penetration. Interestingly, SAR was divergent between the new 5,6-heterobicyclic systems.
Synthesis of novel hybrids of pyrazole and coumarin as dual inhibitors of COX-2 and 5-LOX
Shen, Fa-Qian,Wang, Zhong-Chang,Wu, Song-Yu,Ren, Shen-Zhen,Man, Ruo-Jun,Wang, Bao-Zhong,Zhu, Hai-Liang
supporting information, p. 3653 - 3660 (2017/07/27)
In our previous study, we designed a series of pyrazole derivatives as novel COX-2 inhibitors. In order to obtain novel dual inhibitors of COX-2 and 5-LOX, herein we designed and synthesized 20 compounds by hybridizing pyrazole with substituted coumarin w
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis
Lu, Xiao-Yuan,Wang, Zhong-Chang,Ren, Shen-Zhen,Shen, Fa-Qian,Man, Ruo-Jun,Zhu, Hai-Liang
supporting information, p. 3491 - 3498 (2016/07/21)
Cyclooxygenase-2 is frequently overexpression in malignant tumors and the product PGE2promotes cancer cell progression and metastasis. We designed novel series of coumarin sulfonamides derivatives to improve biological activities of COX-2 inhib