Mixture-based heterocyclic combinatorial positional scanning libraries: Discovery of bicyclic guanidines having potent antifungal activities against Candida albicans and Cryptococcus neoformans Article

Blondelle, SE, Crooks, E, Ostresh, JM et al. (1999). Mixture-based heterocyclic combinatorial positional scanning libraries: Discovery of bicyclic guanidines having potent antifungal activities against Candida albicans and Cryptococcus neoformans . ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 43(1), 106-114. 10.1128/aac.43.1.106

cited authors

  • Blondelle, SE; Crooks, E; Ostresh, JM; Houghten, RA

abstract

  • A mixture-based synthetic combinatorial library of more than 100,000 bicyclic guanidines was generated in a positional scanning format and assayed for activity against Candida albicans. Potent individual bicyclic guanidines were directly identified following the screening of the library. Time-kill curve studies indicated bactericidal activities for the individual bicyclic guanidines. These compounds also showed potent activity against Cryptococcus neoformans. These studies demonstrate the value of using mixture-based combinatorial positional scanning libraries made up of heterocyclic compounds for the rapid identification of novel classes of antifungal compounds.

publication date

  • January 1, 1999

published in

Digital Object Identifier (DOI)

start page

  • 106

end page

  • 114

volume

  • 43

issue

  • 1