CAS: 110588-57-3; Saperconazole

该化合物是一种主要用于治疗各种真菌感染的抗风素剂,属于被称为"阿佐莱斯"的化合物类别,其功能是抑制合成真菌细胞膜膜的有机成分-- egosterol;这一机制扰乱细胞膜膜的完整,导致细胞死亡;萨佩尔康拿索尔展示了广泛频谱抗风素活动,使其对一系列皮肤素和酵母感染有效;该化合物通常以主题方式管理,其配方可包括各种外源,以提高皮肤渗透性和稳定性;就物理特性而言,萨佩尔康诺通常具有有机溶性,水溶性有限,这是阿祖衍生物中常见的.安全性和功效简介是通过临床研究建立的,与其他抗风素剂一样,它可能具有潜在的副作用,包括皮肤刺激或过敏反应.

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      专利号:WO-2009056955-A1
      优先权日:2007-10-30
      标题 :Amine-bearing phospholipids (abps), their synthesis and use
      发明人:ZUMBUEHL ANDREAS
      权利人:UNIV BASEL; ZUMBUEHL ANDREAS
      摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.

      专利号:US-7199128-B2
      优先权日:2005-02-02
      标题 :8-N-substituted-2H-isothiazolo[5,4-b]quinolizine-3,4-diones and related compounds as antiinfective agents
      发明人:BRADBURY BARTON J; WILES JASON ALLAN; DESHPANDE MILIND; WANG QIUPING; HASHIMOTO AKIHIRO; LUCIEN EDLAINE
      权利人:ACHILLION PHARMACEUTICALS INC
      摘要:The invention provides compounds and salts of Formula I and Formula II: n nwhich possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A 1 , A 8 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 9 are defined herein.n n Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of compounds of Formula I and/or Formula II and one or more other active agents. The invention also provides methods for treating microbial and protozoal infections in animals.

      专利号:RU-2156764-C2
      优先权日:1994-01-24
      标题:Azole compounds, methods of their synthesis, antifungal composition, method of composition preparing, method of inhibition of development and proliferation of fungi in warm-blooded animals, intermediate compounds

      专利号:US-2014315720-A1
      优先权日:2012-10-24
      标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
      发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
      权利人:CELANESE ACETATE LLC
      摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.

      专利号:RU-2189982-C2
      优先权日:1997-03-31
      标题:Azole compounds, method of their synthesis, antifungal pharmaceutical composition and method of treatment of fungal infection

      专利号:RU-94045798-A
      优先权日:1992-03-18
      标题:Stereoisomers of itraconazole or saperconazole, method of their synthesis, their complexes and method of preparing, pharmaceutical composition on their base and its preparing, method of preparing aqueous solutions at increased concentration of itraconazole or saperconazole

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      主要参考文献


      1: Meerpoel L, Heeres J, Backx LJ, Van der Veken LJ, Hendrickx R, Corens D, De Groot A, Leurs S, Van der Eycken L, Weerts J, Luyts P, Van Gerven F, Woestenborghs FA, Van Breda A, Oris M, van Dorsselaer P, Willemsens GH, Bellens D, Marichal PJ, Vanden Bossche HF, Odds FC. Synthesis and in vitro and in vivo antifungal activity of the hydroxy metabolites of saperconazole. ChemMedChem. 2010 May 3;5(5):757-69. doi: 10.1002/cmdc.201000040. Review. Review.
      13: Lynch ME, Sobel JD. Comparative in vitro activity of antimycotic agents against pathogenic vaginal yeast isolates. J Med Vet Mycol. 1994;32(4):267-74. Review. French.
      19: Franco L, Gomez I, Restrepo A. Saperconazole in the treatment of systemic and subcutaneous mycoses. Int J Dermatol. 1992 Oct;31(10):725-9.

      合成参考文献


      参考文献:10.1159/000238959
      摘要:Fu KP, Isaacson D, Foleno B, LoCoco J. Saperconazole: in vitro and in vivo anticandidal activity. Chemotherapy. 1992;38(3):174–8. doi: 10.1159/000238959.
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