Title:
HALOGENATED ANTITUBERCULOSIS AGENTS
Document Type and Number:
WIPO Patent Application WO2002092019
Kind Code:
A3
Abstract:
Halogenated derivatives of two synthetic anti-tuberculosis agents, thioacetazone and p-aminosalicylic acid, have been synthesized. In general, the halogenated compound has the structure of Structure (I), wherein X1 is a halogen and X2 is a second halogen or hydrogen, and Y is sulfur or oxygen;or, has the structure of Structure (IV), wherein X1 is a halogen and X2 is a second halogen or hydrogen. Alternatively, the halogenated compounds may be pharmaceutically acceptable salts of these compounds. These halogenated derivates possess anti-mycobacterial activity and are particularly useful for the treatment of Mycobacterium tuberculosis infections. In particular, fluorinated analogs of thioacetazone and p-aminosalicylic acid have been synthesized for use as anti-tuberculosis therapeutic agents either alone or in combination with other conventional anti-tuberculosis therapeutic agents.
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Inventors:
KOBARFARD FARZAD
KAUFFMAN JOEL M
KAUFFMAN JOEL M
Application Number:
PCT/US2002/022071
Publication Date:
March 27, 2003
Filing Date:
March 07, 2002
Export Citation:
Assignee:
UNIV THE SCIENCES IN PHILADELP (US)
International Classes:
C07C281/14; C07C337/08; (IPC1-7): C07C337/06; C07C337/08
Foreign References:
| US2672463A | 1954-03-16 |
Other References:
DATABASE CAPLUS [online] (COLUMBUS OHIO, USA); SARIPINAR ET AL.: "Electron-topological investigation of the structure-antitubercular activity relationship of thiosemicarbazone derivative", XP002958705, accession no. STN Database accession no. 125:184913
GHEORGHIU ET AL.: "Antituberculous substances", REV. CHIM. ACAD. REP. POPULAIRE ROUMAINE 1, no. 1, 1956, (AMERICAN CHEMICAL SOCIETY ABSTRACT NO. 17509D), pages 97 - 125, XP002958704
GHEORGHIU ET AL.: "Antituberculous substances", REV. CHIM. ACAD. REP. POPULAIRE ROUMAINE 1, no. 1, 1956, (AMERICAN CHEMICAL SOCIETY ABSTRACT NO. 17509D), pages 97 - 125, XP002958704
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