- Discovery and SAR study of hydroxyacetophenone derivatives as potent, non-steroidal farnesoid X receptor (FXR) antagonists
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Compound 1 (IC50 = 35.2 ± 7.2 μM), a moderate FXR antagonist was discovered via high-throughput screening. Structure-activity relationship studies indicated that the shape and the lipophilicity of the substituents of the aromatic ring affect the activity dramatically, increasing the shape and the lipophilicity of the substituents of the aromatic ring enhances the potency of FXR antagonists. Especially, when the OH at C2 position of the aromatic ring was replaced by the OBn substituent (analog 2b), its activity could be improved to IC50 = 1.1 ± 0.1 μM. Besides, the length of the linker and the tetrazole structure are essential for retaining the activity.
- Liu, Peng,Xu, Xing,Chen, Lili,Ma, Lei,Shen, Xu,Hu, Lihong
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p. 1596 - 1607
(2014/03/21)
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- Antifungal Activity of 2,4-Dihydroxyacylophenones and Related Compounds
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The antifungal activity of 2,4-dihydroxyacylophenones and related compounds against Trichophyton spp. and other fungi were investigated to determine their structure-activity relationships.The activity of these compounds was found to be closely related to the length of the acyl and alkyl substituents attached to the 1,3-dihydroxybenzene moiety.In addition, differences in activity were observed depending on the position of the alkyl substituents and on the number of substituents attached to the 1,3-dihydroxybenzene moiety.Some compounds tested showed potent antifungal activity against Trichophyton spp. and other fungi that was more active than amphotericin B.
- Mizobuchi, Shigeyuki,Sato, Yuko
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p. 1327 - 1334
(2007/10/02)
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