Gage J.L.,Omeros Corporation |
Onrust R.,Omeros Corporation |
Johnston D.,Scottish Biomedical |
Osnowski A.,Scottish Biomedical |
And 10 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2011
Cyclic nucleotide phosphodiesterases (PDEs) are represented by a large superfamily of enzymes. A series of hydrazone-based inhibitors was synthesized and shown to be novel, potent, and selective against PDE10A. Optimized compounds of this class were efficacious in animal models of schizophrenia and may be useful for the treatment of this disease. © 2011 Elsevier Ltd. All rights reserved.
Szommer T.,AMRI Hungary Zrt. |
Lukacs A.,AMRI Hungary Zrt. |
Kovacs J.,AMRI Hungary Zrt. |
Szabo M.J.,AMRI Hungary Zrt. |
And 3 more authors.
Molecular Diversity | Year: 2012
An efficient and convenient solution-phase synthesis of a 1H-1,2,4-triazole library with potential agrochemical activity is reported employing microwave-assisted organic synthesis (MAOS) and continuous-flow microfluidic synthetic methods starting from commercially available 3,5-dibromo-1H-1,2,4- triazole (1). MAOS was used for the synthesis of 5-amino-3-bromo-1,2,4-triazole analogs 3 and for their 3-aryl derivatives 4 via Suzuki-Miyaura coupling with polymer-supported catalyst. A microfluidic hydrogenation reactor integrated into an automated parallel synthesis platform was built and utilized for the reductive dehalogenation reactions providing 5-aminotriazoles (5). © 2012 Springer Science+Business Media B.V.