361456-52-2Relevant academic research and scientific papers
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.
Bent-core mesogens with an aromatic unit at the terminal position
Bajzíková, Kvetoslava,Svoboda, Ji?í,Novotná, Vladimíra,Pociecha, Damian,Gorecka, Ewa
, p. 4672 - 4679 (2017/07/10)
Bent-core liquid crystals with a naphthalene central unit and an aromatic ring at the terminal position of molecular tails were synthesised with the aim of enhancing nanosegregation. It was found that the length of the spacer between the rigid core and the terminal aromatic moiety had a profound influence on the liquid crystal polymorphism. The homologues with short spacers exhibited nematic and columnar phases, whereas the homologue with long spacers exhibited a tilted lamellar phase with a liquid-like in-plane order, indicating an unusual morphology of the densely packed toroidal objects. The morphology can be changed to twisted ribbons by small additives adsorbed on the membrane surface. This is the first example of twisted ribbons constructed by a lamellar system with no long-range in-plane order.
Removable phosphine reagents for the Mitsunobu reaction
Yoakim, Christiane,Guse,O'Meara,Thavonekham
, p. 473 - 476 (2007/10/03)
We have developed a novel triphenylphosphine replacement for the Mitsunobu reaction. We have demonstrated that 4-diphenylphosphanyl-benzoic acid 2-trimethylsilanyl-ethyl ester (DPPBE) is an efficient reagent and greatly facilitates the isolation of the desired product.
Carboxylic acid derivatives as IP antagonists
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, (2008/06/13)
This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 are each independently in each occurrence aryl or heteroaryl; R4 is
