Identification of 3-phenylaminoquinolinium and 3-phenylaminopyridinium salts as new agents against opportunistic fungal pathogens.
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.
Florida A&M University, College of Pharmacy and Pharmaceutical Sciences, Tallahassee, FL 32307, United States.
Tryphon K
TK
Mazu
Jagan R
JR
Etukala
Xue Y
XY
Zhu
Melissa R
MR
Jacob
Shabana I
SI
Khan
Larry A
LA
Walker
Seth Y
SY
Ablordeppey
D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D001232:Aspergillus fumigatus / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D003455:Cryptococcus neoformans / Q000187:drug effects; D003500:Cyclization; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D011725:Pyridines; D011804:Quinolines