title: Synthesis and in vitro anti-mycobacterium activity of N-alkyl-1, 2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary toxicity and pharmacokinetic evaluation.
abstract: 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.
authors.affiliation: Dipartimento di Chimica Farmaceutica, Università degli Studi, I-27100 Pavia, Italy.
authors.forename: G
authors.initials: G
authors.lastname: Pagani
authors.forename: M
authors.initials: M
authors.lastname: Pregnolato
authors.forename: D
authors.initials: D
authors.lastname: Ubiali
authors.forename: M
authors.initials: M
authors.lastname: Terreni
authors.forename: C
authors.initials: C
authors.lastname: Piersimoni
authors.forename: F
authors.initials: F
authors.lastname: Scaglione
authors.forename: F
authors.initials: F
authors.lastname: Fraschini
authors.forename: A R
authors.initials: AR
authors.lastname: Gascón
authors.forename: J L
authors.initials: JL
authors.lastname: Pedraz Muñoz
mesh_terms: 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
chemical_list: D011725:Pyridines; D013854:Thioamides