5205-39-0Relevant articles and documents
COMPOSITION COMPRISING BISTHIOLACTONES AND PROCESS FOR TREATING KERATIN MATERIALS USING SAME
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Page/Page column 26; 28, (2018/07/29)
The present invention relates to i) a process for treating keratin materials, in particular human keratin fibres, comprising the application of a composition comprising at least one bisthiolactone of formula (I), in particular for shaping keratin fibres and/or straightening/relaxing, ii) a composition comprising the bisthiolactone(s) of formula (I), iii) novel bisthiolactones of formula (I), iv) a process for preparing the novel bisthiolactones of formula (I), and v) the use of said bisthiolactones in cosmetics. In which formula (I), R1, R2, R3, R4, X, X', Y, Y', A, A', B, a, b, c, and d are as defined in the description.
Discovery of LFF571: An investigational agent for Clostridium difficile infection
Lamarche, Matthew J.,Leeds, Jennifer A.,Amaral, Adam,Brewer, Jason T.,Bushell, Simon M.,Deng, Gejing,Dewhurst, Janetta M.,Ding, Jian,Dzink-Fox, Joanne,Gamber, Gabriel,Jain, Akash,Lee, Kwangho,Lee, Lac,Lister, Troy,McKenney, David,Mullin, Steve,Osborne, Colin,Palestrant, Deborah,Patane, Michael A.,Rann, Elin M.,Sachdeva, Meena,Shao, Jian,Tiamfook, Stacey,Trzasko, Anna,Whitehead, Lewis,Yifru, Aregahegn,Yu, Donghui,Yan, Wanlin,Zhu, Qingming
supporting information; experimental part, p. 2376 - 2387 (2012/06/01)
Clostridium difficile (C. difficile) is a Gram positive, anaerobic bacterium that infects the lumen of the large intestine and produces toxins. This results in a range of syndromes from mild diarrhea to severe toxic megacolon and death. Alarmingly, the prevalence and severity of C. difficile infection are increasing; thus, associated morbidity and mortality rates are rising. 4-Aminothiazolyl analogues of the antibiotic natural product GE2270 A (1) were designed, synthesized, and optimized for the treatment of C. difficile infection. The medicinal chemistry effort focused on enhancing aqueous solubility relative to that of the natural product and previous development candidates (2, 3) and improving antibacterial activity. Structure-activity relationships, cocrystallographic interactions, pharmacokinetics, and efficacy in animal models of infection were characterized. These studies identified a series of dicarboxylic acid derivatives, which enhanced solubility/efficacy profile by several orders of magnitude compared to previously studied compounds and led to the selection of LFF571 (4) as an investigational new drug for treating C. difficile infection.
Trimethylsilyldiazomethane as a versatile stitching agent for the introduction of aziridines into functionalized organic molecules
Ren, Hong,Wulff, William D.
supporting information; experimental part, p. 4908 - 4911 (2011/02/21)
A highly enantioselective route for the introduction of aziridines into functionalized organic molecules was developed via a tandem acylation and aziridination of TMSCHN2.
2,3,4,5-TETRAHYDRO-1H-1,5-BENZODIAZEPINE DERIVATIVE AND MEDICINAL COMPOSITION
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, (2008/06/13)
The present invention has its object to provide a 2,3,4,5-tetrahydro-1H-1,5-benzodiazepine derivative represented with the Formula (1) , or the pharmaceutically acceptable salt, which is effective as a therapeutic and prophylactic agent for diabetes, diabetic nephropathy, or glomerulosclerosis.
A New Class of Linear Tetrapyrroles: Acetylenic 10,10a-Didehydro-10a-homobilirubins
Tu, Bin,Ghosh, Brahmananda,Lightner, David A.
, p. 8950 - 8963 (2007/10/03)
Novel bilirubin analogues with dipyrrinones conjoined to an acetylene rather than a methylene group were synthesized and examined spectroscopically. Despite the increased separation of the dipyrrinones forced by replacing a -CH2- by a -C≡C- unit, molecular dynamics calculations show that, like bilirubin, they may still engage in intramolecular hydrogen bonding to carboxylic acid groups when the propionic acid chains are slightly lengthened, e.g., butanoic acids. Unlike bilirubin, however, which is bent in the middle and has a ridge-tile shape, the acetylene orients the attached dipyrrinones along a linear path, and intramolecular hydrogen bonding preserves a twisted linear molecular shape. The extended planes of the dipyrrinones intersect along the -C≡C- axis at an angle of 136° for the conformation stabilized by intramolecular hydrogen bonding in the bis-butyric acid rubin (lb). With shorter acid chains (propionic), only one CO2H can engage an opposing dipyrrinone in intramolecular hydrogen bonding, and in this energy-minimum conformation of the linear pigment 1a, the intersection of the extended planes of the dipyrrinones has an angle of 171°. Spectroscopic evidence for such linearized and twisted structures was found in the pigments' NMR spectral data and their exciton UV-vis and induced circular dichroism spectra.
Hydrogen-bonded dimers in dipyrrinones and acyldipyrrinones
Huggins,Lightner
, p. 203 - 221 (2007/10/03)
A crystal structure determination of the 9-acyl-dipyrrinone 9-butanoyl-2,3,7,8-tetramethyl-(10H)-dipyrrin-1-one indicates the presence of intermolecularly hydrogen-bonded dimers; however, in CHCl3 solution the pigment is monomeric as determined by vapor pressure osmometry measurements. Lacking an alkyl group at C(8), the 9-acyl-dipyrrinone exhibits only a weak tendency to form dimers in CHCl3 (KA ～ 60 M-1) as determined by analysis of variable temperature 1H NMR data. In contrast, when the 9-acyl group is replaced by formyl or when the acyl group is fixed in a syn orientation to the pyrrole NH, the dipyrrinone is strongly prone to dimerization in CHCl3.
Mild hydrolysis or alcoholysis of amides. Ti(IV) catalyzed conversion of primary carboxamides to carboxylic acids or esters
Fisher,Caroon,Stabler,Lundberg,Zaidi,Sorensen,Sparacino,Muchowski
, p. 142 - 145 (2007/10/02)
Reaction of primary amides (e.g., 1a or 6-13) or O-methylhydroxamates (1b and 1c) with a catalytic amount of TiCI4 and one equivalent of aqueous HCI converts these compounds in good yields to carboxylic esters (when an alcohol is used as solvent) or to carboxylic acids (when 9:1 dioxane:H2O is used as solvent). These conversions are chemoselective for primary amides: mono- and dialkyl amides are not affected by the reaction conditions. The hydrolysis conditions described do not compromise the stereochemical integrity of an adjacent chiral center. This is exemplified by the hydrolysis of naproxen amide (34) to naproxen (33) without detectable racemization as determined by chiral HPLC.
SYNTHESE DANS LA CHIMIE DES PHENANTHRIDINES. II. PREPARATION D'UNE NOUVELLE SERIE D'ω-(PHENANTHRIDINYL-6) ALCANOATES DE METHYLE OU D'ETHYLE
Lion, C.,Boukou-Poba, J. P.,Charvy, C.
, p. 567 - 574 (2007/10/02)
A new series of methyl and ethyl ω-(6-phenanthridinyl) alkanoates is easily synthesised from the acid chloride - esters ROCO(CH2)nCOCl (n=0, 3 to 8; R=Me or Et).Reaction of these with o-aminobiphenyl leads to the expected amide-esters which are cyclised to phenanthridines quaternised to the corresponding phenanthridinium salts.
ENZYMATIC REACTIONS IN ORGANIC SYNTHESIS 4- HYDROLYSES OF DIESTERS
Jeso, B. De,Drouillard, S.,Degueil-Castaing, M.,Saux, A.,Maillard, B.
, p. 1691 - 1698 (2007/10/02)
Enzymatic hydrolyses allowed discriminations of esters functions present in the same molecule.
