Identification of 3-phenylaminoquinolinium and 3-phenylaminopyridinium salts as new agents against opportunistic fungal pathogens |
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| Authors: | Mazu Tryphon K Etukala Jagan R Zhu Xue Y Jacob Melissa R Khan Shabana I Walker Larry A Ablordeppey Seth Y |
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| Institution: | a Florida A&M University, College of Pharmacy and Pharmaceutical Sciences, Tallahassee, FL 32307, United States
b The National Center for the Development of Natural Products, Research Institute of Pharmaceutical Sciences, University of Mississippi, MS 38677, United States |
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| Abstract: | Previous studies on the indoloquinoline alkaloid, cryptolepine (2), revealed that it has antii-nfective properties among other activities. Using Structure-activity relationship (SAR) techniques, several ring-opened analogs of cryptolepine (3-phenylaminopyridinium and 3-phenylaminoquinolinium derivatives) were designed to improve the potency and lower the cytotoxicity shown by several of the precursor agents. Results indicate that these ring-opened analogs constitute new anti-infective agents with over a 100-fold potency and several fold lower cytotoxicity than cryptolepine from which they are derived. |
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| Keywords: | Cryptolepine analogs Ring-opened analogs Antifungal agents Anti-opportunistic infection agents Anti-bacterial agents Agents against AIDS-related opportunistic pathogens |
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