Cavalleri B, Turconi M, Tamborini G, Occelli E, Cietto G, Pallanza R, Scotti R, Berti M, Romanó G, Parenti F
Merrell Dow Research Institute--Lepetit Research Center, Gerenzano, Italy.
J Med Chem. 1990 May;33(5):1470-6. doi: 10.1021/jm00167a029.
A series of derivatives of rifamycin P, an antibiotic produced by fermentation of a mutant strain of Nocardia mediterranea or by chemical modification of rifamycin S, have been prepared. The structures of these compounds were determined by 1H NMR, IR, UV, and LC/MS. Their in vitro and in vivo antibacterial activities in comparison with rifampicin and two other rifamycins under investigation were evaluated. The derivatives were more active than rifamycin P against Mycobacterium avium complex and other slowly and rapidly growing nontuberculous mycobacteria which frequently cause systemic infection in patients with AIDS. 2'-(Diethylamino)rifamycin P (P/DEA) appears suitable for further investigation.
已制备了利福霉素P的一系列衍生物，利福霉素P可通过地中海诺卡氏菌突变株发酵产生，也可通过利福霉素S的化学修饰得到。这些化合物的结构通过1H NMR、IR、UV和LC/MS确定。评估了它们与利福平及另外两种正在研究的利福霉素相比的体外和体内抗菌活性。这些衍生物对鸟分枝杆菌复合体以及其他经常在艾滋病患者中引起全身感染的缓慢和快速生长的非结核分枝杆菌的活性比利福霉素P更强。2'-(二乙氨基)利福霉素P（P/DEA）似乎适合进一步研究。
