PMID: 8980782Jan 1, 1997Paper

Efficacies of two novel azole derivatives each containing a morpholine ring, UR-9746 and UR-9751, against systemic murine coccidioidomycosis

Antimicrobial Agents and Chemotherapy
K V Clemons, D A Stevens

Abstract

UR-9746 and UR-9751 are novel azole derivatives each containing a morpholine ring. They were examined for both in vitro and in vivo activities against Coccidioides immitis. In vitro, UR-9746 and UR-9751 were active, with MICs of 25 and 3.1 micrograms/ml, respectively, against C. immitis Silveira; minimum fungicidal concentrations were > 100 micrograms/ml, the highest concentration tested, for both compounds. Antifungal activity in serum showed the desirable characteristic of remaining severalfold above the MIC at all times. Against systemic murine coccidioidomycosis, UR-9746 and UR-9751 prolonged survival at dosages of > or = 10 mg/kg/day and showed increased reduction of infectious burden in the spleens, livers, and lungs of treated mice with escalating dosage. Both compounds lacked observable toxicity and on a milligram-per-kilogram of body weight basis were > or = 10-fold superior to fluconazole in prolonging survival and clearing infection with C. immitis.

References

May 1, 1990·Antimicrobial Agents and Chemotherapy·K V ClemonsD A Stevens
May 1, 1995·Antimicrobial Agents and Chemotherapy·K V ClemonsD A Stevens
Jan 1, 1994·Journal of Medical and Veterinary Mycology : Bi-monthly Publication of the International Society for Human and Animal Mycology·K V Clemons, D A Stevens

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Citations

Mar 9, 2007·Annals of the New York Academy of Sciences·Karl V ClemonsDavid A Stevens
Nov 17, 2015·SAR and QSAR in Environmental Research·R Medina MarreroF Pérez-Giménez
Aug 26, 2000·Scandinavian Journal of Infectious Diseases·J FohlmanB Petrini
Nov 30, 2000·Current Infectious Disease Reports·A V Jacobs, H L Leaf
Mar 31, 2021·Antimicrobial Agents and Chemotherapy·Laura L KovandaDavid A Stevens
Jan 9, 1999·Clinical Microbiology Reviews·D J SheehanC M Sibley
Aug 15, 2006·Drug Resistance Updates : Reviews and Commentaries in Antimicrobial and Anticancer Chemotherapy·D SanglardJ Bille
Jul 17, 2021·The Journal of Antimicrobial Chemotherapy·Gabriele SassDavid A Stevens
Jul 13, 2021·Antimicrobial Agents and Chemotherapy·Gabriele SassDavid A Stevens

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