- 1-[1-[2-[(3-Chlorobenzyl)oxy]phenyl]vinyl]-1H-imidazole hydrochloride, a new potent antifungal agent
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The synthesis and antifungal properties of 1-[1-[2-[(3-chlorobenzyl)oxy]phenyl]vinyl]-1H-imidazole hydrochloride (1-HCl) are described. Topical application of cream and gel formulation of 1-HCl showed high efficacy against guinea pig dermatophytosis.
- Ogata,Matsumoto,Hamada,Takehara,Tawara
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- Syntheses and NMR Spectroscopic Studies on the Conformations of 1--1H-Imidazoles
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The title compounds were synthesized from 2-phenol and their conformations were discussed on the basis of their 1H and 13C spectra.
- Yamamoto, Kazuko,Hamada, Yoshiki,Takeuchi, Isao,Suezawa, Hiroko,Hirota, Minoru
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- Synthesis and Antifungal Activity of New 1-Vinylimidazoles
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Carbonyl compounds I were subjected to an imidazole transfer reaction with N,N'-sulfinyldiimidazole or N,N'-carbonyldiimidazole to obtain the diimidazole II and the monoimidazole III.Various 1-vinylimidazoles IV, derived from o-hydroxyacetophenones by imi
- Ogata, Masaru,Matsumoto, Hiroshi,Shimizu, Sumio,Kida, Shiro,Shiro, Motoo,Tawara, Katsuya
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p. 1348 - 1354
(2007/10/02)
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- SYNTHESES OF PHENOLIC METABOLITES OF AN ANTIFUNGAL IMIDAZOLE DERIVATIVE (CLOCONAZOLE HYDROCHLORIDE)
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Syntheses of phenolic metabolites of antifungal vinylimidazole derivative 6*HCl (Cloconazole hydrochloride) are described.Phenolic compound 8 was prepared from 2 using selective mono THP protection, followed by imidazolation and deprotection. 10 was synth
- Takahashi, Kimio,Shimizu, Sumio,Ogata, Masaru
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p. 1483 - 1491
(2007/10/02)
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- Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1H-imidazoles and related compounds
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Various 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1H-azoles were synthesized and investigated for β-adrenoceptor-blocking and antiarrhythmic activities. Although no compounds showed more potent β-blocking effects than propranolol in the isolated guinea pig right atria, many compounds exhibited significant antiarrhythmic effects against aconitine or ischemic arrhythmia in mice or dogs. 1-[2,5-Dichloro-6-[1-(1H-imidazol-1-yl)ethenyl]phenoxy]-3-[(1-methylethyl) amino]-2-propanol hydrochloride (48) (711389-S) was selected as a candidate for clinical evaluation in man, since its antiarrhythmic effects were superior to those of quinidine, disopyramide, or propranolol. Asymmetric synthesis of (R)-(+)- and (S)-(-)-48 is described, and it is proven that there is no stereospecificity in the antiarrhythmic effect of 48.
- Ogata,Matsumoto,Takahashi,Shimizu,Kida,Ueda,Kimoto,Haruna
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p. 1142 - 1149
(2007/10/02)
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