Infection caused
by Mycobacterium tuberculosis
Infection by
inhalation of the bacteria
Pulmonary TB most
common, but all organs, include. CNS, may be attaced
Until ca. 1959;
50% of all infected died
First effective
drug: Streptomycin 1946
First line drugs
today: Isoniacid, Pyridazinamide, Ethambutol, Rifampicin
During the 1980Õs
TB cases began to increase again even in the industrialized world (AIDS, drug
resistance, increased migration, porr health care in inner cities)
8 Million new
cases each year
30 Million will
die in 10 years
No new drugs on
the marked for ca 30 years
References (see also Natural products)
¯ Selective Anti-tubercular Purines.
Synthesis and Chemotherapeutic Properties of 6-Aryl- and
6-Heteroaryl-9-benzylpurines. Br¾ndvang, M.; Gundersen, L.-L. Bioorg. Med.
Chem. 2005, 13, 6360-6373
¯ Synthesis, Biological Activity and SAR
of Antimycobacterial 9-Aryl-, 9-Arylsulfonyl- and
9-Benzyl-6-(2-furyl)purinesÓBakkestuen, A. K.; Gundersen, L.-L; Utenova, B. T.
J. Med. Chem. 2005,
48, 2710-2723.
¯ Antimycobacterial Activity of
1-Substituted Indolizines" Gundersen. L.-L.; Negussie, A. H.; Rise, F.;
¯stby, O. B. Arch. Pharm. Pharm. Med. Chem. 2003, 336, 191-195.
¯ Cytotoxic and Antibacterial Effects of
2-Oxopurine derivatives." Andresen, G.; Gundersen, L.-L.; Nissen-Meyer,
J.; Rise, F.; Spilsberg, B. Bioorg. Med. Chem. Lett 2002, 12, 567-569.
¯ Synthesis and Antimycobacterial Activity
of 6-Arylpurines; the Requirements for the N-9 Substituent in Active
Antimycobacterial Purines." Gundersen, L.-L.; Nissen-Meyer, J.; Spilsberg,
B. J. Med. Chem.
2002, 45,
1383-1386.
¯ 9-Benzylpurines with Inhibitory Activity
Against Mycobacterium Tuberculosis. Bakkestuen, A. K.; Gundersen, L.-L.;
Langli, G.; Liu, F.; Nols¿e, J. M. J. Bioorg. Med. Chem. Lett. 2000, 10, 1207-1210
