Bioorganic and Medicinal Chemistry Letters p. 3559 - 3563 (2009)
Update date:2022-09-26
Topics: Esterification Purification In vitro Testing In Vivo Testing Formulation Metabolism Bioactivation Enhancement Strategies Publication Search Contacting Authors
Kagoshima, Yoshiko
Mori, Makoto
Suzuki, Eiko
Shibayama, Takahiro
Iida, Tamako
Kamai, Yasuki
Konosu, Toshiyuki
In this study, the synthesis and evaluation of a number of esters of CS-758 as injectable prodrugs are described. Phosphoryl ester 1a was soluble in water (>30 mg/mL) and was converted to CS-758 in human liver microsome. It was also converted to CS-758 in rats after iv administration, wherein the bioavailability of CS-758 was 53%. Compound 1a (iv) reduced the viable cell counts in kidneys in a murine systemic Candida albicans infection model, wherein the effect was comparable to or slightly superior to that of CS-758 (po). The prodrug 1a proved to be a promising injectable antifungal agent whose further evaluation is warranted.
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Doi:10.1002/1099-0682(200102)2001:2<381::AID-EJIC381>3.0.CO;2-A
(2001)Doi:10.1055/s-1971-35040
(1971)Doi:10.1039/j39710002696
(1971)Doi:10.1002/jhet.5570370634
(2000)Doi:10.1016/j.jorganchem.2006.05.065
(2007)Doi:10.1007/BF00473074
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