136450-05-0Relevant articles and documents
Preparation method of 4-(4-phenylbutoxy) benzoic acid
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Paragraph 0047-0050, (2020/09/08)
The invention relates to a preparation method of 4-(4-phenylbutoxy) benzoic acid, which specifically comprises the following steps: a, performing a reaction on gamma-chlorobutanone with p-hydroxybenzoate under the catalysis of alkali to generate a compoun
Selective Optimization of Pranlukast to Farnesoid X Receptor Modulators
Schierle, Simone,Schmidt, Jurema,Kaiser, Astrid,Merk, Daniel
, p. 2530 - 2545 (2018/11/25)
Selective optimization of side activities (SOSA) offers an alternative entry to early drug discovery and may provide rapid access to bioactive new chemical entities with desirable properties. SOSA aims to reverse a drug's side activities through structural modification and to design out the drug's original main action. We identified a moderate side activity for the cysteinyl leukotriene receptor 1 (CysLT1R) antagonist pranlukast on the farnesoid X receptor (FXR). Systematic structural modification of the drug allowed remarkable optimization of its partial FXR agonism to sub-nanonmolar potency. The resulting FXR modulators lack any activity on CysLT1R and are characterized by high selectivity, high metabolic stability, and low toxicity. With their favorable in vitro profile, these SOSA-derived FXR modulators constitute a new FXR ligand chemotype that appears suitable for further preclinical evaluation.
A 4-( benzene butoxy) benzoic acid synthesis method
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, (2017/01/23)
The invention relates to a method for chemically synthetizing 4-(benzene butoxy) benzoic acid. The method comprises the following steps: causing benzene butanol as shown in a formula (II) to carry out thermal reaction in the presence of alkali, and then i