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Azole Antifungals and DMI Fungicides: History, Activity, Synthesis, Resistance, MoA , and SAR

Clemens Lamberth

2026

Abstract

This chapter provides a comprehensive overview of the chemistry, biochemistry, and biology of azoles and DMIs which are, because of their potent fungicidal and antifungal activity and broad spectrum, the biggest-selling antimycotic class on both pharmaceutical and agrochemical markets. Since the appearance of the first azole antifungal in 1969 and the first DMI fungicide in 1973, a whole arsenal of 84 products has entered the application in medicine and agriculture. Discovery, mode of action, pharmacological activity and spectrum, resistance, synthesis, and structure–activity relationships of these active ingredients as well as several of their analogs are shared.

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