First-in-class, dual-action, 3, 5-disubstituted indole derivatives having human nitric oxide synthase (nNOS) and norepinephrine reuptake inhibitory (NERI) activity for …
…, J Ramnauth, SP Maddaford, S Rakhit…
文献索引：Mladenova, Gabriela; Annedi, Subhash C.; Ramnauth, Jailall; Maddaford, Shawn P.; Rakhit, Suman; Andrews, John S.; Zhang, Dongqin; Porreca, Frank Journal of Medicinal Chemistry, 2012 , vol. 55, # 7 p. 3488 - 3501
A family of different 3, 5-disubstituted indole derivatives having 6-membered rings were designed, synthesized, and demonstrated inhibition of human nitric oxide synthase (NOS) with norepinephrine reuptake inhibitory activity (NERI). The structure–activity relationship (SAR) within the cyclohexane ring showed the cis-isomers to be more potent for neuronal NOS and selective over endothelial NOS compared to their trans-counterparts. ...
