Development of New MDR-Tuberculosis Drugs (Pharmacology - by Jarmila Vinsova, Martin Kratky

By Jarmila Vinsova, Martin Kratky

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013 µg/mL. N´-Acetylrifabutinol and N´(undec-10´-enoyl)-rifabutin (17) exhibiting the highest activity against MDR- Research of Novel MDR Potential Drugs 17 TB clinical isolates (except RIF- and INH- resistant to STM or EMB, additionally) having a MIC value of 8 and 6 µg/mL, respectively. Both the luciferase and CFU endpoints indicated that all of the rifabutin derivatives were more active against non-replicating persistent mycobacteria than RIF, especially rifabutin and N´-(undec-10´-enoyl)-rifabutin, but this derivative appears to be more cytotoxic (Vero cells) than rifabutin.

All isoprenoids are derived from the repetitive condensation of two important precursors, isopentenyl diphosphate (IPP) and dimethylallyl diphosphate (DMAPP), catalyzed by prenyl diphosphate synthetases. In M. , IPP and DMAPP are biosynthesized only through the 2C-methyl-D- Research of Novel MDR Potential Drugs 39 erythrol 4-phosphate pathway [141]. A number of isoprenoids have been observed and characterized in M. tbc. including polyprenyl phosphate (Pol-P), the prenyl side-chain of menaquinone and various forms of carotenoids.

Tbc. strains and does not show crossresistance to any current first-line drugs [96]. The long half-life of OPC67683, the lack of metabolization by CYP enzymes and its efficacy in immunocompromised mice suggest that this drug may be useful for the treatment of co-infected TB/HIV patients [74]. The cell wall is the target of Research of Novel MDR Potential Drugs 25 the action. It inhibits like INH methoxymycolic and ketomycolic acid synthesis at significantly lower concentrations, but does not inhibit α-mycolic acid biosynthesis.

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