原创力文档synthesis and biological evaluation of quinazoline-4-thiones合成和生物评价quinazoline-4-thiones.pdfVIP
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synthesis and biological evaluation of quinazoline-4-thiones合成和生物评价quinazoline-4-thiones
Molecules 2003, 8, 756-769
molecules
ISSN 1420-3049
Synthesis and Biological Evaluation of Quinazoline-4-thiones
Lenka Kubicov· 1,*, Martin äustr 1, KatarÌna Kr·ľov· 2, VladimÌr Chobot 1, Jitka Vytlačilov· 1,
Luděk Jahod·ř 1, Pia Vuorela 3, Miloö Mach·ček 1, Jarmila Kaustov· 4
1 Faculty of Pharmacy in Hradec Kr·lovÈ, Charles University in Prague, HeyrovskÈho 1205, 500 05
Hradec Kr·lovÈ, Czech Republic. Tel. +420 49 5067339, Fax +420 49 5210002.
2 Institute of Chemistry, Faculty of Natural Sciences, Comenius University, Mlynsk· dolina CH-2, 842
15 Bratislava, Slovak Republic.
3 Department of Pharmacy, Division of Pharmacognosy, University of Helsinki, P.O. Box 56,
(Viikinkaari 5), Helsinki, Finland.
4 National Reference Laboratory for Mycobacterium Kansasii, Institute of Hygiene, 728 92 Ostrava,
Czech Republic.
*
Author to whom correspondence should be addressed; e-mail: kubicova@faf.cuni.cz
Received: 25 August 2004; in revised form: 30 September 2003 / Accepted: 30 September 2003 /
Published: 15 November 2003
Abstract: Several 2,2-dimethyl-3-phenyl-1,2-dihydroquinazoline-4(3H)-thiones and 2-
methyl-3-phenylquinazoline-4(3H)-thiones were synthesized and tested for their
antimycobacterial, photosynthesis-inhibiting, and antialgal activity. Antimycobacterially
active compounds were found among the 6-chloro substituted compounds. 6-Chloro-3-(4-
isopropylphenyl)-2-methylquinazoline-4(3H)-thione exhibited higher activity than the
isoniazid standard against Mycobacterium avium and M. kansasii . Most of the compounds
posse
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