Events The 11th International Electronic Conference on Synthetic Organic Chemistry

Event submissions

Published

This submission belongs to the session b. Solid Phase Chemistry and Combinatorial Synthesis of the event The 11th International Electronic Conference on Synthetic Organic Chemistry

Published date

30 Nov, 2007

Citation

Bert U.W. Maes, Ernesto Cano, Reyes Laguna, Nuria Fraiz, Matilde Yáñez, Guy L. F. Lemière, Tom Verhelst, Caroline Meyers, Alberto Coelho,, Abdelaziz Elmaatougi, Eddy Sotelo, 2-Substituted 4-, 5- and 6-[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones and 2-Substituted 4,5-bis[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones as Potent Platelet Aggregation Inhibitors: Design, Synthesis and SAR Studies, in Proceedings of The 11th International Electronic Conference on Synthetic Organic Chemistry, 1 November–30 November 2007, MDPI: Basel, Switzerland, doi: 10.3390/ecsoc-11-01334

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2-Substituted 4-, 5- and 6-[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones and 2-Substituted 4,5-bis[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones as Potent Platelet Aggregation Inhibitors: Design, Synthesis and SAR Studies

Bert U.W. Maes ¹

Ernesto Cano ²

Reyes Laguna ²

Nuria Fraiz ²

Matilde Yáñez ²

Guy L. F. Lemière ¹

Tom Verhelst ¹

Caroline Meyers ¹

Alberto Coelho, ³

Abdelaziz Elmaatougi ⁴

Eddy Sotelo ^3,4

1. Organic Synthesis, Department of Chemistry, University of Antwerp, Groenenborgerlaan 171, B-2020 Antwerpen, Belgium

2. Departamento de Farmacología, Universidad de Santiago de Compostela, 15782-Santiago de Compostela, spain

3. Unidad de Química Combinatoria, Instituto de Farmacia Industrial (IFI), Spain

4. Departamento de Química Orgánica, Spain

Abstract

A set of regioisomeric 2-substituted pyridazin-3(2H)-ones containing a 3-oxo-3- phenylprop-1-en-1-yl fragment at either position 4, 5 or 6 and 2-substituted pyridazin-3(2H)-ones containing the same fragment both at positions 4 and 5 have been synthesized and evaluated as antiplatelet agents. The study allows the identification of a new highly potent platelet aggregation inhibitor (4c) as well as the formulation of preliminary structure-activity relationships in this series.

Keywords

Platelets

pyridazin-3(2H)-ones

chalcones

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