Early Research on Cell-Wall Active Agents

Early Research on Cell-Wall Active Agents 

In the 1970s two structural classes of fungal fermentation products were discovered in screening programs for antifungal agents (1) the 

1974 Echinocandin B Sandoz Ciba-Geigy Lilly OH OH OH ch3 ch3 Linoleic acid 

Cilofungin Limited Spectrum and Solubility Problems Ended Development, Leading to Reduced Interest in the Entire Class 

In the 1970s scientists at Eli Lilly Co. determined that echinocan-din B had potent antifungal activity against C. albicans and Candida trop-icalis and in vivo activity in animal models of candidiasis. Its limitations for human therapeutics were lack of oral bioavailability and poor water solubility. There was also concern because it produced in vitro lysis of red blood cells. Early chemical modifications focused on reducing the lytic potential of echinocandin B and showed that the fatty acyl tail 

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III. Early Research On Cell Wall Active Agents. 430... 

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