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Sci. Pharm. 2013, 81(2), 329-338; doi:10.3797/scipharm.1303-03

7-Aza-des-A-steroids with Antimicrobial and Cytotoxic Activity

Department of Pharmacy – Center for Drug Research, Ludwig-Maximilians University, Butenandtstr. 5–13, 81377 Munich, Germany
Author to whom correspondence should be addressed.
Received: 2 March 2013 / Accepted: 14 April 2013 / Published: 14 April 2013
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This paper describes a convenient approach to the 7-aza-des-A-steroid (6,6a,7,8,9,9a-hexahydro-5H-cyclopenta[h]quinoline) scaffold starting from Grundmann's ketone using two different pyridine annulation protocols. The biological evaluation of the pyridine and pyridinium products revealed that these compounds unexpectedly do not interfere with ergosterol and cholesterol biosynthesis. The pyridinium compound 6 showed significant antimicrobial and cytotoxic activities which are most likely due to its detergent-like structure.
Keywords: Azasteroids; Pyridine; Annulation; Antimicrobial activity; Cytotoxic activity Azasteroids; Pyridine; Annulation; Antimicrobial activity; Cytotoxic activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

KROJER, M.; KELLER, M.; BRACHER, F. 7-Aza-des-A-steroids with Antimicrobial and Cytotoxic Activity. Sci. Pharm. 2013, 81, 329-338.

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