Synthesis and in vitro anti-mycobacterium activity of N-alkyl-1, 2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary toxicity and pharmacokinetic evaluation.
Disseminated infections with Mycobacterium tuberculosis (MT) and Mycobacterium 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 synthesized, and MICs for MT and MAC strains, either standard or isolated from infected patients, have been determined. Preliminary tests show a good activity and a very low toxicity for some derivatives. Pharmacokinetic studies in the rat show a very rapid elimination from the body after intravenous administration and a poor absorption after oral administration.
Pagani
G
G
Dipartimento di Chimica Farmaceutica, Università degli Studi, I-27100 Pavia, Italy.
Pregnolato
M
M
Ubiali
D
D
Terreni
M
M
Piersimoni
C
C
Scaglione
F
F
Fraschini
F
F
Gascón
A R
AR
Pedraz Muñoz
J L
JL
D000818:Animals; D005260:Female; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D051379:Mice; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar; D013854:Thioamides / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity
D011725:Pyridines; D013854:Thioamides