| 摘要 |
The present invention relates to novel fusidic acid derivatives of general formula [I] wherein X represents halogen trifluoromethyl, cyano, azido, alkyl, alkenyl or aryl, wherein, said alkyl, alkenyl or aryl are optionally substituted by one or more, same or different substituents selected from the group consisting of alkyl alkenyl, aryl, alkoxy, nitro, alkylthio, halogen, azido, trifluoromethy and cyano; Y and Z both represent hydrogen, or together with the C-17/C-20 bond form a double bond between C-17 and C-20, or together are methylene and form a cyclopropane ring in combination with С-17 and C-20; A represents a bond,. O, S or S(O); В represents Calkyl Calkenyl, Cacyl, Ccycloalkylcarbonyl or benzoyl, all of which are optionally substituted with one or more substituents selected from the group consisting of halogen, hydroxy, alkoxy, aryl, heteroaryl am azido, or, if A represents a bond, В may also represent hydrogen; Q1 and ‘Q2 independently represent. -CH2-, -C(O)-, -(CHOR)-, -(CHOR)--(CHSH)-, - (NH)-, -(CHNH2)- or -(CHW)-, wherein R represent: Calkyl and W represents halogen, cyano, azido or trifluoromethyl; Q3 represents -CH2-, -C(O)- or -CHOH-; G represents hydrogen, OH or O-CO-CHtwo bonds in the pentacyclic ring being depicted with full and dotted lines to indicate that either of the two bonds may be a double bond, in which case Y is absent and Z represents hydrogen; the bond between C-l and C-2 being either a single or a double bond; and pharmaceutically acceptable salts and easily hydrolysable esters thereof, to pharmaceutical compositions comprising said derivatives, as well as to their use in therapy.(I) |
