Synthesis and in vitro anti-Mycobacterium activity of N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary toxicity and pharmacokinetic evaluation
G. Pagani et al., Synthesis and in vitro anti-Mycobacterium activity of N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary toxicity and pharmacokinetic evaluation, J MED CHEM, 43(2), 2000, pp. 199-204
Disseminated infections with Mycobacterium tuberculosis (MT) and Mycobacter
ium avium complex (MAC) are increasingly opportunistic diseases in patients
with advanced acquired human immunodeficiency syndrome (AIDS). A series of
N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides has been synthesize
d, and MICs for MT and MAC strains, either standard or isolated from infect
ed patients, have been determined. Preliminary tests show a good activity a
nd a very low toxicity for some derivatives. Pharmacokinetic studies in the
rat show a very rapid elimination from the body after intravenous administ
ration and a poor absorption after oral administration.