title: Synthesis and biological activity of some derivatives of rifamycin P.
abstract: 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.
authors.affiliation: Merrell Dow Research Institute--Lepetit Research Center, Gerenzano, Italy.
authors.forename: B
authors.initials: B
authors.lastname: Cavalleri
authors.forename: M
authors.initials: M
authors.lastname: Turconi
authors.forename: G
authors.initials: G
authors.lastname: Tamborini
authors.forename: E
authors.initials: E
authors.lastname: Occelli
authors.forename: G
authors.initials: G
authors.lastname: Cietto
authors.forename: R
authors.initials: R
authors.lastname: Pallanza
authors.forename: R
authors.initials: R
authors.lastname: Scotti
authors.forename: M
authors.initials: M
authors.lastname: Berti
authors.forename: G
authors.initials: G
authors.lastname: Romanó
authors.forename: F
authors.initials: F
authors.lastname: Parenti
mesh_terms: 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
chemical_list: D012294:Rifamycins; C027407:rifamycin P; C063797:rifamexil