Brufani M, Cellai L, Marchi E, Segre A
J Antibiot (Tokyo). 1984 Dec;37(12):1611-22. doi: 10.7164/antibiotics.37.1611.
Two series of new semisynthetic rifamycin SV derivatives have been prepared. One of them bears a quaternary ammonium salt at C3 (1-5), and the other a pyridoimidazo system condensed at C3 and C4 (6-11). While compounds 1-5 had poor antibacterial activity in vitro, compounds 6-11 were found to be highly active in vitro but poorly absorbed in vivo. They could thus have potential as agents in the therapy of intestinal infections. The synthesis and the 1H NMR structure determination of these new compounds are reported.
已经制备了两系列新的半合成利福霉素SV衍生物。其中一系列在C3位带有季铵盐（1-5），另一系列在C3和C4位稠合有吡啶并咪唑体系（6-11）。虽然化合物1-5在体外具有较差的抗菌活性，但发现化合物6-11在体外具有高活性，但在体内吸收较差。因此，它们可能有潜力作为肠道感染治疗药物。报道了这些新化合物的合成及1H NMR结构测定。
