68874-23-7Relevant academic research and scientific papers
Synthesis of axially chiral N-aryl benzimidazoles via chiral phosphoric acid catalyzed enantioselective oxidative aromatization
Chen, Jin-Fang,Cui, Xin,Li, Guang-Xun,Shi, Jin-Yi,Tang, Zhuo,Yin, Cong-Cong,Zhao, Jin-Zhong
, p. 6398 - 6402 (2022/04/19)
Given the great importance of N-substituted benzimidazoles in pharmaceutics, here N-aryl benzimidazoline produced in situ was used as a H2 donor, which was converted to C-N axially chiral N-aryl benzimidazole by CPA-catalyzed enantioselective transfer hydrogenation of the in situ produced imine.
Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-Aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3 H)-yl]-1-(methylamino)butan-2- ols (WYE-103231)
O'Neill, David J.,Adedoyin, Adedayo,Alfinito, Peter D.,Bray, Jenifer A.,Cosmi, Scott,Deecher, Darlene C.,Fensome, Andrew,Harrison, Jim,Leventhal, Liza,Mann, Charles,McComas, Casey C.,Sullivan, Nicole R.,Spangler, Taylor B.,Uveges, Albert J.,Trybulski, Eugene J.,Whiteside, Garth T.,Zhang, Puwen
experimental part, p. 4511 - 4521 (2010/08/20)
Structural modification of a virtual screening hit led to the identification of a new series of 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol- 1(3H)-yl]-1-(methylamino)butan-2-ols which are potent and selective inhibitors of the norepinephrine transporter over both the serotonin and dopamine transporters. One representative compound S-17b (WYE-103231) had low nanomolar hNET potency (IC50 = 1.2 nM) and excellent selectivity for hNET over hSERT (>1600-fold) and hDAT (>600-fold). S-17b additionally had a good pharmacokinetic profile and demonstrated oral efficacy in rat models of ovariectomized-induced thermoregulatory dysfunction and morphine dependent flush as well as the hot plate and spinal nerve ligation (SNL) models of acute and neuropathic pain.
ARYL SULFAMIDE DERIVATIVES AND METHODS OF THEIR USE
-
Page/Page column 103, (2008/12/06)
The present invention is directed to aryl sulfamide derivatives of formula (I): or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.
