SYNTHESIS AND BIOLOGIC PROPERTIES OF SOME 1-(ALCHYL)PHENYL-3-(4-(3-(PYRIDIN-2-IL)ACRYLOYL)PHENYLTHIOUREA

Abstract

This paper describe the synthesis of some 1-(alchyl)aril-3-(4-(3-pyridin-2-il) acryloyl)phenylthiourea obtained by condensation of 2-pyridincarboxaldehide with some derivatives of 4-acetylphenilthioureas in basic medium or by addition of aliphatic and aromatic amines to the correspondingisothiocyanatopropenones. 12 new compounds were obtained and their biological properties were analysed. The substituted thioureas by pyridine radicals, morpholine and phenol show a maximum bacteriostatic activity for Gram positive microorganisms like: Staphylococcus Aureus and Enterococcus Faecalis at the minimum inhibitory concentration 9.37-37.5 μM. Antifungal activity for Candida Albicans, Aspergillus Niger, AspergillusFumigatus, Penicillium is weak, in minimum inhibitory concentration 600->600 μM. The leukemia activity like inhibitor (HL-60), is 84-96.9% at the concentration 10-5mol/l and 15- 20% and at the concentrations 10-6, 10-7mol/l.

Keywords

• chalcones
• isothiocyanatopropenones
• thioureas
• antibacterial activity
• antifungal activity
• antiproliferative activity