FTR1335 Is a Novel Synthetic Inhibitor of Candida albicans N(-)Myristoyltransferase with Fungicidal Activity

Abstract

Fungal infections range in severity from common superficial problems affecting the skin and nails, to deeply invasive and disseminated infections, such as systemic candidiasis and pulmonary aspergillosis.1,2) These illnesses reduce the quality of life of patients and can progress to become life threatening. Four classes of antifungal drugs are available at present: polyene macrolides, azoles, flucytosine and candins. However, their use is restricted by their limited activity spectra, toxicity, hazardous interactions and non-optimal pharmacokinetics.

Pharmacologically targeting the myristoylation of the scaffold protein FRS2α inhibits FGF/FGFR-mediated oncogenic signaling and tumor progression

“…Numerous NMT inhibitors have been reported to inhibit fungal growth due to low amino acid sequence similarity of the NMT protein between fungi or parasites and humans (54,55). However, only a limited number of agents have been identified so far as anti-cancer agents (15,22).…”

Design, Synthesis and Antifungal Activity of Novel Benzofuran-Triazole Hybrids

“…Therefore, NMT would be a promising target for the development of novel fungicidal drugs. Up to now, various types of NMT inhibitors such as peptidomimetic [10][11][12], myristic acid analogues [13] and different kinds of heterocycles [14][15][16] have been reported. Among them, benzofuran inhibitors showed high selectivity and powerful antifungal activity [16][17][18][19] (Figure 1).…”

Synthesis and antimicrobial activity of pyrazolinones and pyrazoles having benzothiazole moiety

“…A large range of benzothiazole derivatives were reported having anticancer (Brantley et al, 2006), anticonvulsant (Rana et al, 2008), antiinflammatory (Naik et al, 1996), and antimicrobial activities (Amir et al, 2009;Bondock et al, 2010;Franchini et al, 2009;Soni et al, 2010;Ebara et al, 2005) (Fig. 1).…”