880495-84-1Relevant articles and documents
PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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Page/Page column 179, (2021/12/08)
The present invention relates to pyrazolopyrimidine derivatives having dual pharmacological activity towards both the α2δ subunit of the voltage-gated calcium channel and the sigma-1 (σ1) receptor, to processes of preparation of such compounds,
Meta-Selective C-H Borylation of Benzamides and Pyridines by an Iridium-Lewis Acid Bifunctional Catalyst
Yang, Lichen,Uemura, Nao,Nakao, Yoshiaki
supporting information, p. 7972 - 7979 (2019/05/22)
We report herein the iridium-catalyzed meta-selective C-H borylation of benzamides by using a newly designed 2,2′-bipyridine (bpy) ligand bearing an alkylaluminum biphenoxide moiety. We also demonstrate the iridium-catalyzed C3-selective C-H borylation of pyridine with a 1,10-phenanthroline (Phen) ligand bearing an alkylborane moiety. It is proposed that the Lewis acid-base interaction between the Lewis acid moiety and the aminocarbonyl group or the sp2-hybridized nitrogen atom accelerates the reaction and controls the site-selectivity.
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus
Wiles, Jason A.,Song, Yongsheng,Wang, Qiuping,Lucien, Edlaine,Hashimoto, Akihiro,Cheng, Jijun,Marlor, Christopher W.,Ou, Yangsi,Podos, Steven D.,Thanassi, Jane A.,Thoma, Christy L.,Deshpande, Milind,Pucci, Michael J.,Bradbury, Barton J.
, p. 1277 - 1281 (2007/10/03)
We synthesized a diverse series of 9H-isothiazolo[5,4-b]quinoline-3,4- diones containing heteroaromatic groups at the 7-position via palladium-catalyzed cross-coupling. Many of these compounds demonstrated potent antistaphylococcal activity (MICs ≤2 μg/mL) against a multi-drug-resistant strain (ATCC 700699) and low cytotoxic activity (CC50 > 100 μM) against the human cell line Hep2 (laryngeal carcinoma).