452979-20-3Relevant academic research and scientific papers
AMIDE DERIVATIVE
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, (2012/06/01)
Provided are a compound having an excellent hypoglycemic action, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause an increase in the blood sugar level due to abnormal sugar metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.
Synthesis, cleavage, and antifungal activity of a number of novel, water-soluble ester prodrugs of antifungal triazole CS-758
Kagoshima, Yoshiko,Mori, Makoto,Suzuki, Eiko,Shibayama, Takahiro,Iida, Tamako,Kamai, Yasuki,Konosu, Toshiyuki
scheme or table, p. 3559 - 3563 (2010/03/31)
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.
WATER-SOLUBLE TRIAZOLE FUNGICIDE
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Page/Page column 183, (2010/02/07)
A triazole compound of the general formula (I) or a pharmacologically acceptable salt thereof: [wherein,X represents a group of formula X-OH which has antifungal activity,L represents a -(adjacently substituted C6-C10 aryl)-CH2-group and the like, andR represents a -P(=O) (OH)2 group and the like.
