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.
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