79757-76-9Relevant academic research and scientific papers
Metal-Free Aerobic Oxidative Selective C-C Bond Cleavage in Heteroaryl-Containing Primary and Secondary Alcohols
Xia, Anjie,Qi, Xueyu,Mao, Xin,Wu, Xiaoai,Yang, Xin,Zhang, Rong,Xiang, Zhiyu,Lian, Zhong,Chen, Yingchun,Yang, Shengyong
, (2019/05/07)
A transition-metal-free aerobic oxidative selective C-C bond-cleavage reaction in primary and secondary heteroaryl alcohols is reported. This reaction was highly efficient and tolerated various heteroaryl alcohols, generating a carboxylic acid derivative and a neutral heteroaromatic compound. Experimental studies combined with density functional theory calculations revealed the mechanism underlying the selective C-C bond cleavage. This strategy also provides an alternative simple approach to carboxylation reaction.
First selective CYP11B1 inhibitors for the treatment of cortisol-dependent diseases
Hille, Ulrike E.,Zimmer, Christina,Vock, Carsten A.,Hartmann, Rolf W.
, p. 2 - 6 (2011/04/17)
Outgoing from an etomidate-based design concept, we succeeded in the development of a series of highly active and selective inhibitors of CYP11B1, the key enzyme of cortisol biosynthesis, as potential drugs for the treatment of Cushing's syndrome and rela
Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17α-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure
Jagusch, Carsten,Negri, Matthias,Hille, Ulrike E.,Hu, Qingzhong,Bartels, Marc,Jahn-Hoffmann, Kerstin,Mendieta, Mariano A.E. Pinto-Bazurco,Rodenwaldt, Barbara,Mueller-Vieira, Ursula,Schmidt, Dirk,Lauterbach, Thomas,Recanatini, Maurizio,Cavalli, Andrea,Hartmann, Rolf W.
, p. 1992 - 2010 (2008/09/20)
Novel chemical entities were prepared via Suzuki and SN reaction as AC-ring substrate mimetics of CYP17. The synthesised compounds 1-31 were tested for activity using human CYP17 expressed in Escherichia coli. Promising compounds were tested for selectivity against hepatic CYP enzymes (3A4, 2D6, 1A2, 2C9, 2C19, 2B6). Two potent inhibitors (27, IC50 = 373 nM/28, IC50 = 953 nM) were further examined in rats regarding their effects on plasma testosterone levels and their pharmacokinetic properties. Compound 28 was similarly active as abiraterone and showed better pharmacokinetic properties (higher bioavailability, t1/2 9.5 h vs 1.6 h). Docking studies revealed two new binding modes different from the one of the substrates and steroidal inhibitors.
Fused Heterocycles from Pyrrolethiols.Thienopyrroles,Thienopyroles and THiazolopyrroles from Pyrrol-2-yl Phenacyl Sulfides
Harris, Roger L.N.,McFadden, Helen G.
, p. 887 - 892 (2007/10/02)
A reinvestigation of the cyclization of pyrrol-2-yl phenacyl sulfides in polyphosphoric acid has shown that the major product is a thienopyrrole, where rearrangement of the sulfur substituent from position 2 to position 3 has preceded cyclization.W
