150235-40-8Relevant academic research and scientific papers
Structural Basis for Developing Multitarget Compounds Acting on Cysteinyl Leukotriene Receptor 1 and G-Protein-Coupled Bile Acid Receptor 1
Fiorillo, Bianca,Sepe, Valentina,Conflitti, Paolo,Roselli, Rosalinda,Biagioli, Michele,Marchianò, Silvia,De Luca, Pasquale,Baronissi, Giuliana,Rapacciuolo, Pasquale,Cassiano, Chiara,Catalanotti, Bruno,Zampella, Angela,Limongelli, Vittorio,Fiorucci, Stefano
, p. 16512 - 16529 (2021/11/24)
G-protein-coupled receptors (GPCRs) are the molecular target of 40% of marketed drugs and the most investigated structures to develop novel therapeutics. Different members of the GPCRs superfamily can modulate the same cellular process acting on diverse pathways, thus representing an attractive opportunity to achieve multitarget drugs with synergic pharmacological effects. Here, we present a series of compounds with dual activity toward cysteinyl leukotriene receptor 1 (CysLT1R) and G-protein-coupled bile acid receptor 1 (GPBAR1). They are derivatives of REV5901-the first reported dual compound-with therapeutic potential in the treatment of colitis and other inflammatory processes. We report the binding mode of the most active compounds in the two GPCRs, revealing unprecedented structural basis for future drug design studies, including the presence of a polar group opportunely spaced from an aromatic ring in the ligand to interact with Arg792.60 of CysLT1R and achieve dual activity.
N-benzyl dihydroindole LTD4 antagonists
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, (2008/06/13)
This invention relates to pharmaceutical N-benzyl dihydroindole compounds having the general formula: STR1 and their use as LTD4 antagonists.
Development of a Novel Series of (2-quinolinylmethoxy)phenyl-Containing Compounds as High-Affinity Leukotriene D4 Receptor Antagonists. 2. Effects of an Additional Phenyl Ring on Receptor Affinity
Huang, Fu-Chih,Galemmo, Robert A.,Johnson, William H.,Poli, Gregory B.,Morrissette, Matthew M.,et al.
, p. 1194 - 1200 (2007/10/02)
This series of reports describe the development of orally active, highly potent, specific antagonists of the peptidoleukotrienes containing a (2-quinolinylmethoxy)phenyl moiety.The compounds reported in this paper contain an additional phenyl ring, which
