Isobenzofurans as conformationally constrained miconazole analogs with improved antifungal potency

…, AJ Elliott, JJ Kaminski, D Loebenberg…

Index: Lovey, Raymond G.; Elliott, Arthur J.; Kaminski, James J.; Loebenberg, David; Parmegiani, Raulo M.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 22 p. 4221 - 4229

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Citation Number: 22

Abstract

A series of halogen-substituted isobenzofuran analogues was synthesized, which represented conformationally constrained analogues of miconazole (I). In vitro and in vivo topical antifungal activity against both dermatophytes and Candida species varied widely, but 13c proved to be significantly superior to both 1 and clotrimazole against a vaginal Candida infection in hamsters, while 13b was significantly more active than 1 against aa ...