申请人:The Procter & Gamble Company
公开号:US05656623A1
公开(公告)日:1997-08-12
Antimicrobial lactam-quinolone compounds comprising a lactam-containing moiety linked to a quinolone moiety, of the formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.4 and R.sup.6 generally form any of a variety of quinolone, naphthyridine or related cyclic moieties known in the art to have antimicrobial activity; and (2) R.sup.1 or R.sup.3 contain a linking moiety, linking the quinolone moiety to a lactam-containing moiety having the formula: ##STR2## wherein (3) R.sup.10, R.sup.11, R.sup.12, R.sup.13, and R.sup.14, together with bonds "a" and "b", form any of a variety of lactam-containing moieties known in the art to have antimicrobial activity; and (4) the linking moiety includes (for example) carbamate, dithiocarbamate, urea, thiourea, isouronium, isothiouronium, guanidine, carbonate, trithiocarbonate, reversed carbamate, xanthate, reversed isouronium, reversed dithiocarbamate, reversed isothiouronium, amine, imine, ammonium, heteroarylium, ether, thioether, phosphono, phosphoramide, phosphate, sulfonamide, ester, thioester, amide, and hydrazide groups.
含有乳内酰胺-
喹诺酮化合物,包括连接到
喹诺酮基团的乳内酰胺基团,其
化学式为:##STR1## 其中(1)A.sup.1、A.sup.2、A.sup.3、R.sup.1、R.sup.4和R.sup.6通常形成一种在艺术上已知具有抗微
生物活性的
喹诺酮,
萘啶或相关环状基团; (2)R.sup.1或R.sup.3包含一个连接基团,将
喹诺酮基团连接到具有以下
化学式的乳内酰胺含基团:##STR2## 其中(3)R.sup.10、R.sup.11、R.sup.12、R.sup.13和R.sup.14与键“a”和“b”一起形成艺术上已知的各种含乳内酰胺的基团,具有抗微
生物活性; (4)连接基团包括(例如)
氨基甲酸酯,二
硫代
氨基甲酸酯,
脲,
硫脲,异
脲,异
硫脲,
胍,
碳酸酯,
三硫代碳酸酯,反向
氨基甲酸酯,黄原酸酯,反向异
脲,反向二
硫代
氨基甲酸酯,反向异
硫脲,胺,
亚胺,
铵,杂环芳基
铵,醚,
硫醚,
膦酸酯,膦酰胺,
磷酸酯,磺酰胺,酯,
硫酯,酰胺和
肼基团。