Bioorganic and Medicinal Chemistry Letters p. 2031 - 2036 (1996)
Update date:2022-08-05
Topics:
Dickinson, Roger P.
Bell, Andrew S.
Hitchcock, Christopher A.
Narayanaswami, Subramaniyan
Ray, Stephen J.
Richardson, Kenneth
Troke, Peter F.
Replacement of one triazole ring of fluconazole with 4-pyridinyl leads to an increase in activity against Aspergillus fumigatus. Introduction of an α-methyl group has a marked additional beneficial effect. Investigation of pyridinyl and pyrimidinyl analogues resulted in the identification of 30 (UK-109,496), voriconazole) which has excellent potency against a broad range of fungal pathogens including A. fumigatus and Candida krusei.
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