Morpholine antifungals

Morpholine antifungals inhibit ergosterol biosynthesis by acting on the enzymes A -reductase and A ,A -isomerase (Fig. 40.1, Site 3 and 4) (45). Inhibition of these enzymes results in incorporation into fungal cell membranes of sterols retaining either a... 

Antifungal drugs are classified according to their mode of action and/or their chemical class. Four chemical classes have mainly contributed to the actual armentory of antifungal drugs the broadest class is the one of azoles (imidazoles and triazoles), followed by polyenes, allylamines and morpholines. Some individual compounds are used in dermatology. 

Amorolfine is a morpholine derivative, used topically as an antifungal, with a broad spectrum of activity against dermatophytes, other fungi and yeasts. 

Aryl and morpholine substituted analogs of rocagiamide were synthesized and tested for insecticidal and antifungal activity [153]. The Pd-catalyzed amination of bromophenyl derivative 90 with morpholine gave moderate yield of 91. 

Eswaran et al. [4] reported synthesis and antimicrobial activity of new 1,2,4-triazole carrying quinoline derivatives using multistep reactions. The biological results revealed that cyclopropylamine, cychlohexylamine and morpholine at position 4 of quinoline enhanced antibacterial and antifungal activity. 

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