116748-53-9Relevant academic research and scientific papers
Thiazole amide compound and preparation method, pharmaceutical composition and application thereof
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Paragraph 0207; 0231; 0256; 0257; 0258, (2019/01/08)
The invention discloses a thiazole amide compound and a preparation method thereof, a pharmaceutical composition and application thereof. The thiazole amide compound as shown in a formula I and a pharmaceutically acceptable salt thereof are provided, and
Synthesis and antiproliferative evaluation of 2'-arenesulfonyloxy-5- benzylidene-thiazolidine-2,4-diones
Chen, Emily M.,Lu, Pei-Jung,Shaw, Arthur Y.
, p. 792 - 798 (2012/10/29)
A series of 2'-arenesulfonyloxy-5-benzylidene-thiazolidine-2,4-diones (TZDs) were synthesized and examined for their antiproliferative effects on a panel of carcinoma cell lines. Our results indicated that initial synthesis of 5-[2'-hydroxybenzylidene]-2,
Design and synthesis of novel N-benzylidenesulfonohydrazide inhibitors of murC and murD as potential antibacterial agents
Frlan, Rok,Kovac, Andreja,Blanot, Didier,Gobec, Stanislav,Pecar, Slavko,Obreza, Ales
, p. 11 - 30 (2008/09/16)
A series of novel N-benzylidenesulfonohydrazide compounds were designed and synthesized as inhibitors of UDP-N-acetylmuramic acid:L-alanine ligase (MurC) and UDP-N-acetylmuramoyl-L-alanine:D-glutamate ligase (MurD) from E. coli, involved in the biosynthes
New arylsulfonohydrazide inhibitors of enzymes MurC and MurD
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Page/Page column 29, (2008/06/13)
This invention belongs to the field of pharmaceutical chemistry and relates to new arylsulfonohydrazides as inhibitors of UDP-N-acetylmuramyl:L-alanine ligaze (MurC) and UDP-N-acetylmuramyl-L-alanine:D-glutamate ligaze (MurD), to procedures for their preparation and pharmaceutical preparations containing the same. The enzymes MurC and MurD are the key enzymes involved in the synthesis of bacterial peptidoglycan, so arylsulfonohydrazide inhibitors possess antibacterial activity. Compounds of general formula I and the pharmaceutically acceptable salts are described. The appropriate substituents are clearly presented in the body of the text and in claims.
A concise approach to the preparation of 2-hydroxydiarylketones by an intramolecular acyl radical ipso substitution
Motherwell,Vazquez
, p. 9667 - 9671 (2007/10/03)
Substituted 2-hydroxydiarylketones have been simply prepared using an intramolecular acyl radical [1,6] ipso substitution reaction. (C) 2000 Elsevier Science Ltd.
Studies on the Conformation of 5,15-Diarylporphyrins with (Arylsulfonyl)oxy Substituents
Sanders, Georgine M.,Dijk, Marinus van,Veldhuizen, Albertus van,Plas, Henk C. van der,Hofstra, Ulbert,Schaafsma, Tjeerd J.
, p. 5272 - 5281 (2007/10/02)
Dimeso-substituted octaalkylporphyrins, carrying an (arylsulfonyl)oxy group at the ortho position of the two (meso) phenyl groups, were synthesized from dipyrrolylmethanes and aldehydes.On account of a 1H NMR upfield shift in CDCl3 solution of 2-5 ppm for the aryl protons, a folded conformation is assumed in which the substituted aryl groups lie right above and below the porphyrin plane.In CDCl3/CF3COOH solution the upfield shifts are absent.The results of low-temperature 1H NMR measurements and ring-current calculations agreed with our assumptions.The sulfonyloxy group promotes folding of the molecule more than the ester, sulfonyl, sulfinyl, thio, or methylene group.In zinc porphyrins carrying anthraquinone substituents, intramolecular coordination was observed. ΔG, ΔH, and ΔS values for the various conformational equilibria were calculated from the NMR data.We suggest van der Waals interactions with a contribution of charge transfer as the driving force for the folding of the molecule.
