Synthesis and Activity against Mycobacterium tuberculosis of Olivacine and Oxygenated Derivatives

被引：13

作者：

Schmidt, Ulrike ^{[1
]}

Theumer, Gabriele ^{[1
]}

Jaeger, Anne ^{[1
]}

Kataeva, Olga ^{[2
]}

Wan, Baojie ^{[3
]}

Franzblau, Scott G. ^{[3
]}

Knoelker, Hans-Joachim ^{[1
]}

机构：

[1] Tech Univ Dresden, Fac Chem, Bergstr 66, D-01069 Dresden, Germany

[2] Kazan Fed Univ, AM Butlerov Chem Inst, Kremlevskaya Str 18, Kazan 420008, Russia

[3] Univ Illinois, Coll Pharm, Inst TB Res, 833 S Wood St,MC 964, Chicago, IL 60612 USA

来源：

MOLECULES | 2018年 / 23卷 / 06期

关键词：

inhibitory activity; catalysis; cyclization; olivacine; palladium; pyrido[4,3-b]carbazoles; CARBAZOLE ALKALOIDS; ORGANIC-SYNTHESIS; IN-VITRO; ELLIPTICINE; ARYLATION;

D O I：

10.3390/molecules23061402

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The tetracyclic pyrido[4,3-b]carbazole olivacine and four of its oxygenated derivatives have been synthesized by a late-stage palladium-catalyzed Heck-type cyclization of the pyrrole ring as a key step. In a test for the inhibition of the growth of Mycobacterium tuberculosis, 9-methoxyolivacine showed the most significant inhibitory activity against Mycobacterium tuberculosis, with an MIC90 value of 1.5 mu M.

引用

页数：16

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