Synthesis and biological activity of some derivatives of rifamycin P.
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.
Cavalleri
B
B
Merrell Dow Research Institute--Lepetit Research Center, Gerenzano, Italy.
Turconi
M
M
Tamborini
G
G
Occelli
E
E
Cietto
G
G
Pallanza
R
R
Scotti
R
R
Berti
M
M
Romanó
G
G
Parenti
F
F
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D005260:Female; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects; D051381:Rats; D012294:Rifamycins / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D012294:Rifamycins; C027407:rifamycin P; C063797:rifamexil