《Discovery of 6-Phenylhexanamide Derivatives as Potent Stereoselective Mitofusin Activators for the Treatment of Mitochondrial Diseases》 was written by Dang, Xiawei; Zhang, Lihong; Franco, Antonietta; Li, Jiajia; Rocha, Agostinho G.; Devanathan, Sriram; Dolle, Roland E.; Bernstein, Peter R.; Dorn, Gerald W.. Related Products of 27489-62-9 And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:
Mutations in the mitochondrial fusion protein mitofusin (MFN) 2 cause the chronic neurodegenerative condition Charcot-Marie-Tooth disease type 2A (CMT2A), for which there is currently no treatment. Small-mol. activators of MFN1 and MFN2 enhance mitochondrial fusion and offer promise as therapy for this condition, but prototype compounds have poor pharmacokinetic properties. Herein, we describe a rational design of a series of 6-phenylhexanamide derivatives whose pharmacokinetic optimization yielded a 4-hydroxycyclohexyl analog, 13, with the potency, selectivity, and oral bioavailability of a preclin. candidate. Studies of 13cis- and trans-4-hydroxycyclohexyl isostereomers unexpectedly revealed functionality and protein engagement exclusively for the trans form, 13B(I). Preclin. absorption, distribution, metabolism, and excretion (ADME) and in vivo target engagement studies of 13B support further development of 6-phenylhexanamide derivatives as therapeutic agents for human CMT2A. The experimental part of the paper was very detailed, including the reaction process of trans-4-Aminocyclohexanol(cas: 27489-62-9Related Products of 27489-62-9)
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Related Products of 27489-62-9
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