CAS: 3572-60-9; Amidinomycin

该化合物是属于米地类的化学化合物,其特点是存在一个氨基功能组,该功能组由碳原子双柱组成,该物质组由氮原子组成,单柱体结为另一个氮原子组成;该结构赋予分子独特的特性,包括其作为抗微生物剂的潜力;对氨二氮素的生物活动进行了研究,特别是其对某些细菌菌株的功效;该化合物一般为室温固态,可能表现出极地溶剂溶解性;其化学行为受功能组的影响,这些功能组可参与各种化学反应,包括核肺病袭击和与金属离子的协调;由于其生物意义,氨二氮素及其衍生物对医药化学和药物研究,特别是开发新抗生素具有兴趣;但是,在与任何化学物质合作时,应遵循具体的安全和处理准则.

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      专利信息


      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.

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      主要参考文献


      1: Sapse AM, Feng W, Fugler-Domenico L, Kabir S, Joseph T, Lown JW. Quantum chemical and molecular mechanics studies on the binding of stereoisomers of the oligopeptide antibiotics amidinomycin and noformycin to the minor groove of B-DNA. J Biomol Struct Dyn. 1993 Feb;10(4):709-26. doi: 10.1016/j.bmcl.2013.02.053. Epub 2013 Feb 22. German. German.

      合成参考文献


      摘要:Index of Antibiotics from Actinomycetes, Umezawa, H. et al., eds., Tokyo, Univ. of Tokyo Press, 1967, -(444), 1967
      摘要:Index of Antibiotics from Actinomycetes, Umezawa, H. et al., eds., Tokyo, Univ. of Tokyo Press, 1967, -(127), 1967
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