Stereoselective synthesis of 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as PIM kinase inhibitors inspired from marine alkaloids.
Sign Up to like & getrecommendations! Published in 2022 at "Chirality"
DOI: 10.1002/chir.23501
Abstract: We previously demonstrated that natural product-inspired 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones derivatives delivered potent and selective PIM kinases inhibitors however with non-optimal ADME/PK properties and modest oral bioavailability. Herein, we describe a structure-based scaffold decoration and a stereoselective approach… read more here.
Keywords: synthesis dihydropyrrolo; dihydropyrrolo pyrazin; pyrazin one; synthesis ... See more keywords
Design, synthesis, anticancer evaluation and molecular docking studies of chalcone linked pyrido[4,3-b]pyrazin-5(6H)-one derivatives
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DOI: 10.1016/j.molstruc.2020.129851
Abstract: Abstract A series of novel chalcone derivatives pyrido[4,3-b]pyrazin-5(6H)-one (10a-j) were designed, synthesized and their structures were confirmed by 1H NMR, 13C NMR and mass spectral data. Further, all derivatives were tested for their anticancer activities… read more here.
Keywords: pyrazin one; pyrido pyrazin; cancer; anticancer ... See more keywords
Discovery of 6,7-Dihydropyrazolo[1,5-a]pyrazin-4(5H)-one Derivatives as mGluR2 Negative Allosteric Modulators with In Vivo Activity in a Rodent's Model of Cognition.
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DOI: 10.1021/acs.jmedchem.4c01227
Abstract: Allosteric modulators of the metabotropic group II receptors, mGluR2 and mGluR3, have been widely explored due to their ability to modulate cognitive and neurological functions in mood disorders, although none have been approved yet. In… read more here.
Keywords: allosteric modulators; negative allosteric; dihydropyrazolo pyrazin; mglur2 negative ... See more keywords
Novel 2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one derivatives as potent and selective aldose reductase inhibitors with antioxidant activity
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2019.1643336
Abstract: Abstract To develop multifunctional aldose reductase (AKR1B1) inhibitors for anti-diabetic complications, a novel series of 2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one derivatives were designed and synthesised. Most of the derivatives were found to be potent and selective against AKR1B1, and… read more here.
Keywords: pyrazin one; antioxidant activity; potent selective; aldose reductase ... See more keywords