Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 46, Issue 6, Pages 2378-2385Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.03.021
Keywords
delta-carboline; Anti-fungal; Anti-bacterial; Opportunistic; Synthesis; Quaternary
Categories
Funding
- National Institutes of Health, National Institute of Allergy and Infectious Diseases [R15 A137976-01]
- Research Centers at Minority Institutions (RCMI) [G12 RR 03020]
- Title III
- Pharmaceutical Research Center NIH/NCRR [1 C06-RR12512-01]
- NIH, NIAID, Division of AIDS [AI 27094]
- USDA Agricultural Research Service [58-6408-2-0009]
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Previous studies have indicated that the delta-carboline (2) ring system derived from the natural product cryptolepine (1) may represent a pharmacophore for anti-infective activity. This paper describes the design and synthesis of a small library of substituted delta-carbolines and the evaluation of the anti-fungal and anti-bacterial activities. An evaluation of the anti-bacterial activity of a previously reported library of ring-opened analogs was also conducted to provide an opportunity to test the hypothesis that both group of compounds may have the same biological target. Results indicate that against a selected group of fungal pathogens, substituted delta-carbolinium analogs displayed higher potency and several fold lower cytotoxicity than cryptolepine the parent natural product. Both the delta-carbolinium compounds and their ring-opened analogs, exhibited equally high anti-bacterial activity against the selected pathogens and especially against the gram positive bacteria evaluated. Published by Elsevier Masson SAS.
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