- Synthesis of 1-(2-hydroxy-phenyl)-3-piperidin-1-yl-propenone by ultrasonic irradiation
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Different 1-(2-hydroxy-phenyl)-3-piperidin-1-yl-propenones have been synthesized by ultrasonic activation from differently substituted 3-formyl chromones and piperidine. Copyright Taylor & Francis Group, LLC.
- Dalvi,Shelke,Karale,Gill
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- Analogues of Dehydroacetic Acid as Selective and Potent Agonists of an Ectopic Odorant Receptor through a Combination of Hydrophilic and Hydrophobic Interactions
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Identification of potent agonists of odorant receptors (ORs), a major class of G protein-coupled receptors, remains challenging due to complex receptor–ligand interactions. ORs are present in both olfactory and non-chemosensory tissues, indicating roles beyond odor detection that may include modulating physiological functions in non-olfactory tissues. Selective and potent agonists specific for particular ORs can be used to investigate physiological functions of ORs in non-chemosensory tissues. In this study, we designed and synthesized novel synthetic dehydroacetic acid analogues as agonists of odorant receptor 895 (Olfr895) expressed in bladder. Among the synthesized analogues, (E)-3-((E)-1-hydroxy-3-(piperidin-1-yl)allylidene)-6-methyl-2H-pyran-2,4(3H)-dione (10) exhibited extremely high agonistic activity for Olfr895 in Dual-Glo luciferase reporter (EC50=9 nm), Ca2+ imaging, and chemotactic migration assays. Molecular docking and site-directed mutagenesis studies suggested that a combination of hydrophilic and hydrophobic interactions is central to the selective and specific binding of 10 to Olfr895. The design of agonists armed with both hydrophilic and hydrophobic portions could therefore lead to highly potent and selective ligands for ectopic ORs.
- Park, Bernie Byunghoon,Lee, NaHye,Kim, YunHye,Jae, YoonGyu,Choi, Seunghyun,Kang, NaNa,Hong, Yu Ri,Ok, Kiwon,Cho, Jeonghee,Jeon, Young Ho,Lee, Eun Hee,Byun, Youngjoo,Koo, JaeHyung
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p. 477 - 482
(2017/04/10)
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- Reaction of 3-iodochromone with nucleophiles 3. Formation of 2-aminomethylene-3(2h)-benzofuranones by the reaction with secondary amines
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3-Iodochromone (4a) easily reacted with secondary amines in the presence of potassium carbonate to give 2-aminomethylene-3(2H)-benzofuranones in good yields. Under similar conditions without potassium carbonate, 4a was reacted with piperidine to give the
- Sugita, Yoshiaki,Iwaki, Takako,Okamoto, Misaki,Yokoe, Ichiro
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p. 881 - 888
(2007/10/03)
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