ABSTRACT
Griseofulvin (MW 352.5 daltons) is a metabolite of Penicillium griseofulvum and P. janczewskii that disrupts the fungal mitotic spindle and inhibits cell wall synthesis. The structure is shown in Figure 167.1. This compound was discovered in 1939 (Oxford et al., 1939), but was not initially developed because of the absence of antibacterial activity. Griseofulvin was developed as systemic therapy for Botrytis infection in lettuce and Alternaria blight of tomatoes, but was too expensive for widespread horticultural use (Davies, 1980). The clinical potential of this agent was not realized until 1958, when griseofulvin was demonstrated to be effective in laboratory animal models of Microsporum canis and Trichophyton mentagrophytes infection. Subsequently, griseofulvin was demonstrated to be effective for human dermatophyte infections (Williams et al., 1958; Blank et al., 1959). The advent of modern antifungal agents that exhibit more favorable pharmacokinetic and toxicity profiles has largely relegated griseofulvin to a second-line agent. Chemical structure of griseofulvin. https://s3-euw1-ap-pe-df-pch-content-public-p.s3.eu-west-1.amazonaws.com/9781315152110/08d8042d-9481-4a8d-8c27-9bd589f6de6b/content/fig167_1.tif" xmlns:xlink="https://www.w3.org/1999/xlink"/>
