Aids-057176

Aids-057176 - Names and Identifiers

Name	4-[2-[(2R,3R)-3-(2,4-difluorophenyl)-3-hydroxy-4-(1,2,4-triazol-1-yl)b utan-2-yl]-1,3-thiazol-4-yl]benzonitrile
Synonyms	Er-30346 Bms-207147 ER-30346) Aids057176 Bms-207,147 Aids-057176 Ravuconazole (BMS-207147 4-[2-[(2R,3R)-3-(2,4-difluorophenyl)-3-hydroxy-4-(1,2,4-triazol-1-yl)b utan-2-yl]-1,3-thiazol-4-yl]benzonitrile Benzonitrile, 4-[2-[(1R,2R)-2-(2,4-difluro-phenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-4-thiazolyl]- [R-(R,R)]-4-{2-[2-(2,4-Difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)-propyl]-4-thiazolyl}-benzonitrile
CAS	182760-06-1

Aids-057176 - Physico-chemical Properties

Molecular Formula	C22H17F2N5OS
Molar Mass	437.47
Density	1.38±0.1 g/cm3(Predicted)
Melting Point	64-66°C
Boling Point	674.9±65.0 °C(Predicted)
Specific Rotation(α)	D24 -29.1° (c = 1.03 in methanol)
pKa	11.62±0.29(Predicted)
Storage Condition	-20°C Freezer
In vitro study	Ravuconazole shows a broad spectrum of activity against a wide range of fungi covering Candida spp. , Trichosporon beigelii , C. neoformans and A. fumigatus . The MIC 90 ranges from 0.025 to 0.39 mg/mL.Ravuconazoleshows relatively higher levels of activity against three strains of Candida krusei , with MICs ranging from 0.05 to 0.39 mg/mL.Ravuconazoleshows good activity against T. mentagrophytes , T. rubrum , M. gypseum and M. canis with MICs ranging from 0.05 to 0.39 mg/mL. Ravuconazoleis about two- to four fold more potent than itraconazole and about 40-fold more active than fluconazole against yeasts. Ravuconazoleand itraconazoleare inhibitory to most aspergilli, and against half of the isolates, the activity iscidal. Ravuconazoleand itraconazoleare active, though not cidal, against most hyaline Hyphomycetes , dermatophytes, and the dematiaceous fungi and inactive against Sporothrix schenckii and zygomycetes.
In vivo study	The maximum concentration of ravuconazole in plasma and the area under the concentration-time curve for ravuconazoleshow good linearity over a range of doses from 2 to 40 mg/kg of body weight. Ravuconazole at a dose of 2.5 mg/kg delays mortality significantly compared with the control treatment.Ravuconazole also shows a substantial therapeutic effect against systemic cryptococcosis. Ravuconazole reduces the numbers of CFU in the lungs significantly compared with the numbers of CFU in the lungs of the controls. In an experimental model of oral candidiasis in rats, ravuconazole reduces the numbers of CFU in oral swabs significantly compared with the numbers of CFU in oral swabs from the controls and is more effective than itraconazole and as effective as fluconazole..