Development of a stereoselective and chemoselective approach to <i>trans</i>‐2,3‐disubstituted‐4‐chromanones

Chambers, Robert; Marfat, Anthony

doi:10.1002/jhet.5570310617

Cited by 4 publications

(1 citation statement)

References 14 publications

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“…The synthetic pathways employed are shown in Scheme . The designed sequences involved the use of key precursors ( 15 , 16 , 101 ) and transformations described previously . All members of the library were structurally characterized by a combination of NMR spectroscopy, mass spectrometry and/or elemental analysis.…”

Section: Introductionmentioning

confidence: 99%

3-Oxopyridazin-5-yl-Chalcone Hybrids: Potent Antiplatelet Agents That Prevent Glycoprotein IIb/IIIa Activation

et al. 2017

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A novel family of potent and broad‐spectrum antiplatelet agents has been discovered by exploration of a library of 3‐oxopyridazin‐5‐yl‐chalcone hybrids. The pharmacological evaluation of the collection established the most salient features of the SAR in this series and allowed the identification of lead compounds that exhibit antiplatelet activity that is substantially superior to drugs in clinical use and 3,4‐methylenedioxy‐β‐nitrostyrene (MNS). The derivatives reported herein act on GPIIb/IIIa, but in a different manner to classical antagonists (e. g., tirofiban), by preventing GPIIb/IIIa activation. Given their mechanism of action, these compounds might avoid the adverse effects of antagonists (paradoxical GPIIb/IIIa activation) and constitute attractive pharmacological tools for the development of tailored agents for the treatment of platelet‐dependent thrombosis.

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Section: Introductionmentioning

confidence: 99%