Experimental and Clinical Studies of 5-Fluorocytosine Activity in <i>Candida </i>Ocular Infections

Abstract

In vitro sensitivity to 5-Fluorocytosine (5-FC) of 35 Candida strains (14 C. albicans, 10 C. tropicalis, 5 C. parapsilosis, 2 C. guilliermondii, 2 C. krusei, 2 C. pseudotropicalis), isolated from the eyes of patients suffering from various external ocular inflammations who had not been treated with 5-FC, was tested and compared to that of standard Candida species. The minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC) of 5-FC for the strains isolated from ocular infections ranged from 0.06 to 1.95 μg/mland from 0.24 to 7.81 μg/ml, respectively, indicating that no primary resistant strains to 5-FC were found in this series.

Recent advances in antimicrobial nucleoside antibiotics targeting cell wall biosynthesis

“…The MIC of 5-FC for the strains isolated from ocular infections ranged from 0.06 to 1.95 µg mL Ϫ1 . 82 It is converted into the nucleotide triphosphate and incorporated into RNA, thereby causing miscoding, and is converted to its deoxynucleoside which inhibits thymidylate synthase and thereby DNA synthesis.…”

“…Analogues lacking either the N-methyl group (81) or the diaminobutyric acid C4 methyl group (82) were reported to have no activity. 98 Bozzoli et al have also reported the solid phase synthesis of MRD analogues (83) lacking the enamide group, and lacking the N-methyl group and diaminobutyric acid C-4 methyl group.…”