期刊
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
卷 30, 期 1, 页码 26-35出版社
ELSEVIER
DOI: 10.1016/j.ejps.2006.09.006
关键词
indolizine; antimicrobial; tuberculosis
1-Substituted indolizines with activity against Mycobacterium tuberculosis have been synthesized. The most active compounds carry an hydroxyphenylmethyl- or hydroxyalkyl substituent in the indolizine 1-position. The alkyl chain should be moderately long (C-5 or C-6). Aryl groups in the 2- and 3-position of the indolizine are also required. Removal of the 3-substituent resulted in significant loss of activity. A nitrile substituent in the 7-position is beneficial for both chemical stability and bioactivity. The compounds studied display a narrow antibacterial spectrum and appear to be quite selective antimycobacterial compounds. Moderate activity against certain pathogenic protozoa was also observed. (c) 2006 Elsevier B.V. All rights reserved.
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