SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists

Current status of pyrazole and its biological activities

“…Gomez et al .,[ 43 ] have reported the synthesis and structure-activity relationship studies of 1,5-diarylpyrazoles analogs with various structural modifications of the alkane side chain of the molecule and concluded that compound showed good oral bioavailability and could be used for the potential treatments of irritable bowel syndrome and other gastrointestinal disorders. Compound 19 showed good results [ Figure 41 ].…”

Screening a Plant Extract Library for Inhibitors of Cholecystokinin Receptor CCK1 Pathways

“…Compounds that target cholecystokinin receptors have been pursued by a number of groups. These studies used both high-throughput screening and rational design approaches, 7,13,14 typically guided by receptor binding assays. To the best of our knowledge, β-lactamase-based gene reporter screens have not been used to search for inhibitors of CCK-induced pathways.…”

An Economical Access to 3,4‐Diaryl‐2(5H)‐furanones and 4‐Aryl‐6‐methyl‐2(2H)‐pyranones by Pd‐Catalyzed Suzuki‐Type Arylation of 3‐Aryl‐4‐tosyloxy‐2(5H)‐furanones and 6‐Methyl‐4‐tosyloxy‐2(2H)‐pyranones, Respectively

“…Five-membered heterocycles with two aryl groups on adjacent positions include a very large number of biologically active compounds [1] such as cyclooxygenase-2 (COX-2) inhibitors, [2] anticoccidial agents, [3] cannabinoid CB 1 receptor antagonists, [4] ligands for the Niemann Pick C1 Like 1 (NPC1L1) protein, [5] antagonists for the human CCK 1 receptor, [6] inhibitors of transforming growth factor-beta, [7] p38α MAP kinase, [8] and HMG-CoA reductase, [9] and substances with potent cytotoxic activity against human cancer cell lines. [10] Among these heterocycles, unsymmetrical 3,4-diaryl-substituted 2(5H)-furanones 1 represent a class of compounds that has received considerable attention because of their biological properties.…”