52700-25-1Relevant articles and documents
Palladium-Catalyzed Direct α-C(sp3) Heteroarylation of Ketones under Microwave Irradiation
Quillen, Andrew,Nguyen, Quynh,Neiser, Matthew,Lindsay, Kara,Rosen, Alexander,Ramirez, Stephen,Costan, Stefana,Johnson, Nathan,Do, Thuy Donna,Rodriguez, Oscar,Rivera, Diego,Atesin, Abdurrahman,Ate?in, Tülay Aygan,Ma, Lili
, p. 7652 - 7663 (2019/05/22)
Heteroaryl compounds are valuable building blocks in medicinal chemistry and chemical industry. A palladium-catalyzed direct α-C(sp3) heteroarylation of ketones under microwave irradiation is developed and reported in this study. Under optimized condition
Synthesis and biological activities of 4-phenyl-5-pyridyl-1,3-thiazole derivatives as p38 MAP kinase inhibitors
Miwatashi, Seiji,Arikawa, Yasuyoshi,Naruo, Ken-Ichi,Igaki, Keiko,Watanabe, Yasumasa,Kimura, Hiroyuki,Kawamoto, Tomohiro,Ohkawa, Shigenori
, p. 410 - 418 (2007/10/03)
A novel series of 4-phenyl-5-pyridyl-1,3-thiazole analogues possessing potent in vitro inhibitory activity against p38 mitogen-activated protein kinase and the release of tumor necrosis factor-α (TNF-α) from human monocytic THP-1 cells stimulated by lipopolysaccharide has been identified. Subsequent structure-activity relationship (SAR) studies and optimization for absorption, distribution, metabolism, and elimination (ADME) profiles led to the identification of compounds 7g and 10b as orally active lead candidates that block the in vivo production of proinflammatory cytokine (TNF-α). In pharmacokinetic studies, compound 10b showed good oral administration in mice and demonstrated significant in vivo anti-inflammatory activity in an anti-collagen monoclonal antibody-induced arthritis mouse model (minimum effective dose (MED)=30 mg/kg). Further elucidation of this class of compounds may provide novel anti-inflammatory agents, such as anti-rheumatoid arthritis drugs.
CONCOMITANT DRUGS
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, (2008/06/13)
The present invention relates to a pharmaceutical agent containing one or more kinds of a p38 MAP kinase inhibitor and/or a TNF-α production inhibitor and one or more kinds of drugs selected from the group consisting of (1) a non-steroidal antiinflammator