The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
A series of new carbocyclic uracil derivatives were synthesized and evaluated as potential antituberculosis agents. Racemic 1-[4'-hydroxy-2'-cyclopenten-1'-yl]-5-tetradecynyluracil completely inhibited the growth of Mycobacterium tuberculosis H37Rv in vitro at a concentration of 10 μg/ml. Individual (+) and (-) isomers of the above uracil derivative were isolated and showed the same level of activity against two strains of Mycobacterium tuberculosis: laboratory sensitive (H37Rv) and clinical resistant to five top antituberculosis drugs (MS-115).
Engelhardt Institute of Molecular Biology RAS, Vavilova 32, Moscow, Russia.
Elena
E
Matyugina
Anastasia
A
Khandazhinskaya
Larisa
L
Chernousova
Sofia
S
Andreevskaya
Tatiana
T
Smirnova
Alexander
A
Chizhov
Inna
I
Karpenko
Sergey
S
Kochetkov
Ludmila
L
Alexandrova
D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects / Q000302:isolation & purification; D013237:Stereoisomerism; D014498:Uracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000633:toxicity; D014709:Vero Cells
D000995:Antitubercular Agents; D014498:Uracil