ABSTRACT
Thienyl-triazine-sulphonamide conjugates were prepared from their precursor amines using triethyl orthoformate or ethyl chloroformate as cross coupling reagents. The progress of these reactions was investigated by spectral (IR, NMR, MS) and microanalytical techniques. The synthesized compounds were in vitro screened for antibacterial, antifungal, antioxidant, and anticancer activity. 4-[({[3-Mercapto-5-oxo-6-[2-(2-thienyl)yinyl]-1,2,4-triazin- 4(5H)-yl]imino}methyl)amino]-benzenesulfonamide turned out to be a powerful antibacterial agent, while all the compounds prepared were inactive against fungal species tested. 4-{[({8-Cyano-4-oxo-3-[2-(2-thienyl)vinyl- 4H,8H-[1,2,4]triazino[3,4-b][1,3,4]thiadiazin-7-yl}amino)(ethoxy)methyl]amino}benzenesulfonamide displayed in vitro promising cytotoxicity against Ehrlich ascites carcinoma cell line with concurrent attenuation of malonodinitrile and it was unique among other compounds being unable to increase glutathione S-transferase and reduced glutathione S-transferase activities. This compound exhibited also good antioxidant properties that together with its cytotoxicity nominated it for further investigation in cancer research.
Subject(s)
Anti-Bacterial Agents , Antifungal Agents , Antineoplastic Agents , Antioxidants , Triazines , Animals , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Antioxidants/chemical synthesis , Antioxidants/chemistry , Antioxidants/pharmacology , Bacteria/growth & development , Carcinoma, Ehrlich Tumor/drug therapy , Carcinoma, Ehrlich Tumor/metabolism , Carcinoma, Ehrlich Tumor/pathology , Cell Line, Tumor , Female , Fungi/growth & development , Mice , Triazines/chemical synthesis , Triazines/chemistry , Triazines/pharmacologyABSTRACT
Synthesis of benzofuran-1,3-thiazolidinone derivatives is described herein. These compounds were prepared via a concise and short route by condensation reaction of khellinone with aromatic/aliphatic amines followed by cyclization using thioglycolic acid. The newly synthesized compounds were characterized using the well known spectroscopic tools (IR, 1H NMR, and mass spectroscopy), as well as microanalysis. In frames of biological screening of the compounds, antioxidant activity was assessed in vitro.
Subject(s)
Antioxidants/chemistry , Benzofurans/chemistry , Free Radicals/chemistry , Thiazoles/chemistry , Antioxidants/chemical synthesis , Benzofurans/chemical synthesis , Benzofurans/pharmacology , Free Radicals/metabolism , Khellin/chemistry , Oxidation-Reduction , Thiazoles/pharmacologyABSTRACT
Synthesis of selenium-containing amino acid analogues is described. These compounds were prepared in a concise and short synthetic route in good yields by nucleophilic substitution reaction of pyridineselenol and quinolineselenol derivatives with N-phthaloylglycyl chloride followed by hydrazinolysis. The newly synthesized compounds were screened against different strains of bacteria and fungi.
