923243-45-2Relevant academic research and scientific papers
Boronic acid-containing aminopyridine- and aminopyrimidinecarboxamide CXCR1/2 antagonists: Optimization of aqueous solubility and oral bioavailability
Schuler, Aaron D.,Engles, Courtney A.,Maeda, Dean Y.,Quinn, Mark T.,Kirpotina, Liliya N.,Wicomb, Winston N.,Mason, S. Nicholas,Auten, Richard L.,Zebala, John A.
, p. 3793 - 3797 (2015/08/24)
Abstract The chemokine receptors CXCR1 and CXCR2 are important pharmaceutical targets due to their key roles in inflammatory diseases and cancer progression. We have previously identified 2-[5-(4-fluoro-phenylcarbamoyl)-pyridin-2-ylsulfanylmethyl]-phenylboronic acid (SX-517) and 6-(2-boronic acid-5-trifluoromethoxy-benzylsulfanyl)-N-(4-fluoro-phenyl)-nicotinamide (SX-576) as potent non-competitive boronic acid-containing CXCR1/2 antagonists. Herein we report the synthesis and evaluation of aminopyridine and aminopyrimidine analogs of SX-517 and SX-576, identifying (2-{(benzyl)[(5-boronic acid-2-pyridyl)methyl]amino}-5-pyrimidinyl)(4-fluorophenylamino)formaldehyde as a potent chemokine antagonist with improved aqueous solubility and oral bioavailability.
Design of novel N-phenylnicotinamides as selective cyclooxygenase-1 inhibitors
Shi, Lei,Li, Zi-Lin,Yang, Ying,Zhu, Zhen-Wei,Zhu, Hai-Liang
supporting information; experimental part, p. 121 - 124 (2011/02/25)
A series of N-phenylnicotinamides (1-40) were designed and evaluated in vitro for their COX inhibitory activities. Most of the synthesized compounds were proved to be potent and selective inhibitors of COX-1. Compound 28 showed the most potent COX-1 inhib
