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Antimicrobial Agents and Chemotherapy, January 1999, p. 106-114, Vol. 43, No. 1
0066-4804/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.

Mixture-Based Heterocyclic Combinatorial Positional Scanning Libraries: Discovery of Bicyclic Guanidines Having Potent Antifungal Activities against Candida albicans and Cryptococcus neoformans

Sylvie E. Blondelle,* Ema Crooks, John M. Ostresh, and Richard A. Houghten*

Torrey Pines Institute for Molecular Studies, San Diego, California 92121

Received 18 June 1998/Returned for modification 14 September 1998/Accepted 19 October 1998

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.

* Corresponding author. Mailing address: Torrey Pines Institute for Molecular Studies, 3550 General Atomics Ct., San Diego, CA 92121. Fax: (619) 455-3804. Phone for Sylvie E. Blondelle: (619) 455-3843. E-mail: blondell{at}tpims.org. Phone for Richard A. Houghten: (619) 455-3803. E-mail: houghten{at}tpims.org.

Antimicrobial Agents and Chemotherapy, January 1999, p. 106-114, Vol. 43, No. 1
0066-4804/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.




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