Rifamycin compounds of high antibiotic activity

Details Rifamycin compounds of high antibiotic activity Rifamycin compounds of high antibiotic activity

C - Chemistry, Metallurgy

07

D

260/235.82

C07D 498/12 (2006.01) C07D 498/08 (2006.01) C07D 498/20 (2006.01)

Patent

CA 1053667

ABSTRACT OF THE DISCLOSURE: Novel rifamycin derivatives selected from the group consisting of compounds having the general formula: (I) Image wherein X is hydrogen, carboxyl, alkyl with less than 10 atoms C, cycloalkyl with less than 7 atoms C, alkenyl with less than 4 atoms C, cycloalkenyl with less than 7 atoms C, aryl with less than 13 atoms C, arylalkenyl with less than 11 atoms C, or an heterocyclic radical selected from the group consisting of furan, thiophene, pyridine, thiazole, tetrazole, 1,3-benzodioxole and thianaphtene, the radical X being optionally substituted with at least one radical different therefrom and selected from the group consisting, in addition to the aforesaid radicals, of halogen, hydroxyl, alkoxyl, nitro, carboxyl, carbalkoxy and carboxyalkoxy, Y is -H or -COCH3, and their 16,17,18,19-tetra- hydroderivatives, their 16,17,18,19,28,29-hexahydroderivatives as well as the corresponding oxidized derivatives of the general formula: Image (II) wherein X and Y have the aforesaid meanings, have high anti- bacterial activity on Gram-positive and Gram-negative bacteria and particularly on Mycobacterium Tuberculosis.

252701

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