化学
利福霉素
抗菌活性
立体化学
抗菌剂
抗生素
吸收(声学)
细菌细胞结构
衍生工具(金融)
细菌
组合化学
生物化学
经济
物理
金融经济学
生物
遗传学
声学
作者
E. Marchi,L. Montecchi,Arianna Venturini,Giuseppe Mascellani,M. Brufani,Luciano Cellai
摘要
A series of 4-deoxypyrido[1',2':1,2]imidazo[5,4-c]rifamycin SV derivatives (6-11) were prepared that demonstrated high antibacterial activity suitable for an intestinal disinfectant. These compounds are zwitterionic in nature and are poorly absorbed through the gastroenteric tract but maintain the ability to cross the bacterial cell wall. X-ray crystallographic data are presented to demonstrate the zwitterionic nature of these compounds. The structure-activity relationship of this novel series of antibiotics is discussed and the derivative with the highest ratio between subcutaneous and oral activity (6) was selected for clinical development. At the outset of this work several 3-(quaternary ammonium bromides) (1-5) were prepared and tested for antibacterial activity. These compounds were demonstrated to be too polar to even cross the bacterial cell wall but led to the synthesis of 6-11.
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