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Datacija u buli pape Nikole V. o samostanu na Košljunu (28. veljače 1448.)

Authors
Publisher
The catholic faculty of theology
Publication Date
Disciplines
  • Biology
  • Chemistry
  • Medicine
  • Pharmacology

Abstract

Mohareb.vp The continuing interest in the chemistry of b-amino-a,g-dicyanocrotononitrile (1) (1-6) forms a part of the systematic efforts to obtain pyridines, pyrimidines, pyridazines, thio- phenes, thiazoles and their analogs. The importance of such compounds is due to their diverse pharmaceutical activities in neurological disorders (7), as receptor antagonists (8, 9), tubulin inhibitors (10), kinase inhibitors (11) and for anticancer activity (12). More- over, annulated nitrogen heterocycles, bearing pyridine and benzene, constitute a class of biologically active compounds that are potent anti-inflammatory agents (13), anti-bac- terial agents (14), inhibitors of gastric acid secretion (15) and calcium channel blockers (16). Such biological and pharmaceutical importance of the different classes of hetero- cyclic derivatives prompted us to study the chemical reactivity of 2-amino-4-phenyl- penta-1,3-diene-1,1,3-tricarbonitrile 2 towards some chemical reagents with the aim of forming biologically active heterocyclic derivatives. 429 Acta Pharm. 58 (2008) 429–444 Original research papers 10.2478/v10007-008-0030-3 The reaction of �-amino-�,�-dicyanocrotononitrile with acetophenone: Synthesis of pyridine, pyridazine and thiophene derivatives with antimicrobial activities RAFAT M. MOHAREB1* KARAM A. El-SHARKAWY2 SHERIF M. SHERIF1 1Department of Chemistry Faculty of Science, Cairo University Giza, Egypt 2Department of Organic Chemistry Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), October, Egypt Accepted November 11, 2008 Condensation of b-amino-a,g-dicyanocrotononitrile (1) with acetophenone gave 2-amino-4-phenylpenta-1,3-di- ene-1,1,3-tricarbonitrile (2). The latter product was used in a series of heterocyclization reactions with different reagents such as diazonium salts, hydrazines, hydroxyl- amines and elemental sulfur to give pyridazine, pyrazo- le, isoxazole and thiophene derivatives, respectively. On the other hand, it gave pyridine der

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