103195-35-3Relevant articles and documents
Malonic acid receptors with decarboxylative activity
Raposo, Cesar,Luengo, Alicia,Almaraz, Marta,Martin, Mercedes,Mussons, M. Luisa,Caballero, M. Cruz,Moran, Joaquin R.
, p. 12323 - 12332 (1996)
The geometry and electronic properties of several malonic acids receptors are studied with a view to optimizing their decarboxylative activity.
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.
PROCESS FOR PRODUCING CHROMONE COMPOUND
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Page 24, 25, (2008/06/13)
A process for producing a dicarboxylic acid compound represented by the formula (4): wherein R1 and R2 are the same or different and each represents lower alkyl and the wavy line indicates that this compound is the E- or Z-isomer or