15070-88-9Relevant articles and documents
First selective CYP11B1 inhibitors for the treatment of cortisol-dependent diseases
Hille, Ulrike E.,Zimmer, Christina,Vock, Carsten A.,Hartmann, Rolf W.
supporting information; experimental part, 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
DUTPASE INHIBITORS
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Page/Page column 51, (2008/06/13)
Deoxyuridine derivatives of the formula (I) where R1 is H or various substituents; D is -NHCO-, -CONH-, -0-, -C(=O)-, -CH=CH, -CΞC-, -NR5-; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl or a stable monocyclic, bicyclic or tricyclic ring system; G is -O-, -S-, -CHR10-, -C(=O)-; J is -CH2-, or when G is CHR10 may also be -O- or -NH-; R10 is H, F, -CH3, -CH2NH2, -CH2OH; -OH R11 is H, F, -CH3, -CH2 NH2, -CH2OH, CH(OH)CH3, CH(NH3)CH3; or R10 and R11 together define an olefinic bond, or together form a -CH2-group, thereby defining a cis or trans cyclopropyl group; have utility in the prophylaxis or treatment of protozoal diseases such as malaria.
Synthesis and structure-activity relationships of cetiedil analogues as blockers of the Ca2+-activated K+ permeability of erythrocytes
Roxburgh,Ganellin,Athmani,Bisi,Quaglia,Benton,Shiner,Malik-Hall,Haylett,Jenkinson
, p. 3244 - 3253 (2007/10/03)
Cetiedil, [2-cyclohexyl-2-(3-thienyl)ethanoic acid 2-(hexahydro-1H-azepin-1-yl)ethyl ester], which blocks the intermediate calcium-activated potassium ion permeability (IKCa) in red blood cells, was used as a lead for investigating structure-ac
Aromatic hydroxamix acid compounds, their production and use
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, (2008/06/13)
A compound represented by the formula: STR1 wherein Ar1 and Ar2 independently represent an optionally substituted aromatic group; Q represents an optionally substituted divalent aliphatic hydrocarbon group optionally containing O or
Studies of Primary Alkyl and Aralkyl Radicals Using Electron Spin Resonance Spectroscopy and Intermediate Neglect of Differential Overlap Calculations
Brumby, Steven
, p. 1917 - 1924 (2007/10/02)
It is argued that a published ESR spectrum due to n-propyl radicals in solution does not, as has been claimed, exhibit selective broadening of the lines with M = 0 for the α protons, but, rather, a broadening of the lines with M = +/- 1 for the β protons.Based on INDO calculations for the n-propyl radical, and an analysis of the restricted internal rotation, the reported variations in aγ with temperature are rationalized.ESR spectra of 2-hydroxyethyl radicals in solution have been analyzed, and no line width alternation was detected at temperatures of -50 deg C and above.The well-known line width alternation in the ESR spectrum on n-butyl radicals is discussed and it is suggested, partly on the basis of INDO calculations, that the preferred orientations about the Cα-Cβ bond are dependent, to some extent, on the configuration with respect to the Cβ-Cγ bond.The ESR spectra of the species Me3CCH2CH2., Me3CCH2CH2CH2., and Ph3CCH2CH2. are reported and discussed.The spectrum of the former species shows no line width alternation, but the spectrum of the latter species shows a pronounced alternation, which is attributed to the chiral nature of the trityl group.ESR spectra of the species Me(CH2)nCH2. and Ph(CH2)nCH2., with n = 2,3, and 4, display particularly marked line width alternation in the latter series when n = 3 and 4.This observation, together with the results of INDO calculations, may possibly indicate that these radicals prefer conformations with the plane of the trigonal carbon atom parallel to the phenyl-group plane.
