33533-81-2Relevant academic research and scientific papers
Expedient chemoselective and catalyst-free synthesis of 3,3-difluorochroman-4-ones from o-hydroxyarylenaminones and Selectfluor
Xu, Jian,Kuang, Zhijie,Song, Qiuling
supporting information, p. 963 - 966 (2017/11/27)
An expedient and mild strategy for the synthesis of unconventional 2-(dimethylamino)-3,3-difluorochroman-4-one derivatives from o-hydroxyarylenaminones and Selectfluor was developed at room temperature under catalyst-free conditions. This method showed excellent chemoselectivity and great functional groups tolerance.
Analogues of Dehydroacetic Acid as Selective and Potent Agonists of an Ectopic Odorant Receptor through a Combination of Hydrophilic and Hydrophobic Interactions
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
, p. 477 - 482 (2017/04/10)
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.
Ultrasonicated synthesis of 1-(2-hydroxyaryl)-3-(pyrrolidin-1-yl)propenones and their antimicrobial screening
Shelke, Sharad N.,Pawar, Yogesh J.,Pawar, Sheshrao B.,Gholap, Somanth S.,Gill, Charnshing H.
experimental part, p. 461 - 463 (2012/03/11)
A facile synthesis of title compounds has been carried out under ultrasound irradiation. The main advantages of the present procedure are shorter reaction time and higher yield. Products have been characterized by IR, PMR, CMR, GC-MS study and screened for their antimicrobial activity.
