Publications by authors named "Gabor Varro"
The development of a dual V1a/V2 antagonist compound is a complex and challenging task. Conivaptan is up to now the only known V1a/V2 antagonist which was approved for the treatment of euvolemic hyponatremia. Previously, we reported RGH-122, a novel selective V1a antagonist compound.
View Article and Find Full Text PDFThe discovery and characterization of novel naphthyridine derivatives with selective α5-GABAR negative allosteric modulator (NAM) activity are disclosed. Utilizing a scaffold-hopping strategy, fused [6 + 6] bicyclic scaffolds were designed and synthesized. Among these, 1,6-naphthyridinones were identified as potent and selective α5-GABAR NAMs with metabolic stability, cardiac safety, and beneficial intellectual property (IP) issues.
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- A series of synthesized derivatives of (±)-trans-dihydronarciclasine and (±)-trans-dihydrolycoricidine, focusing on variations in ring A, were tested against 60 human tumor cell lines to evaluate their anti-cancer effects.
- Among the 13 tested alkaloids, (±)-trans-dihydronarciclasine demonstrated the strongest ability to kill cancer cells.
- A structure-activity relationship analysis revealed that a hydroxy group at position 7 and a rigid 1,3-benzodioxole structure are crucial for the antiproliferative effectiveness of these compounds.
Abstract: Some new -dihydronarciclasine derivatives containing a 1,4-benzodioxane moiety were stereoselectively synthesised using our feasible and efficient method developed recently. These new phenanthridone alkaloid analogues were obtained in both racemic and optically active forms. High enantioselectivities (up to 99% ) were achieved by applying (8,9)-9-amino(9-deoxy)epiquinine as an organocatalyst.
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- A new method for synthesizing the biologically active alkaloid (-)-trans-dihydronarciclasine was developed starting from vanillin.
- The synthesis features a key step involving an asymmetric, organocatalytic Michael addition that produces an optically active nitropentanone with over 99% enantioselectivity.
- The process is efficient, achieving the target molecule in 13 steps and providing access to a form of a potent cytostatic alkaloid that was previously difficult to obtain.