Details

Autor(en) / Beteiligte

• Pagani, Giuseppe
• Pregnolato, Massimo
• Ubiali, Daniela
• Terreni, Marco
• Piersimoni, Claudio
• Scaglione, Francesco
• Fraschini, Franco
• Gascón, Alicia Rodríguez
• Pedraz Muñoz, José Luis

Titel

Synthesis and in Vitro Anti-Mycobacterium Activity of N-Alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary Toxicity and Pharmacokinetic Evaluation

Ist Teil von

• Journal of medicinal chemistry, 2000-01, Vol.43 (2), p.199-204

Ort / Verlag

Washington, DC: American Chemical Society

Erscheinungsjahr

2000

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.