Synthesis, Structure And Biological Activities Of Novel Heterocyclic Compounds

Amino acids and their derivates were of low toxic, very effective and harmless. They were used for synthesis of pesticide, medicine etc. Homocystine thiolactone was the product of methionine (one of the needed amino acids in human body) metabolized in liver. It was of widely biological activities. The derivates of homocystine thiolactone were of pharmaceutically-acceptable and applied values. Therefore in order to find novel heterocyclic pesticides and realize the accumulation of activities, enhancement and enlargement of fungicide kind, insect hormone and pharmaceutical activity, Homocystine thiolactone and its hydrochloride salt were selected as the raw materials. Twenty-six new derivates of homocystine thiolactone were synthesized by the optimized reaction condition. Their structures have been confirmed and preliminary biological activities have been tested.Part one: Nine Schiff bases of amino-3-dihydrothiophenon-2 were synthesized by reaction of substituted benzaldehyde with DL-homocysteine thiolactone hydrochloride (ADTHC1) by means of preferable reaction conditions. Seven of them were reported for the first time. The structures of the compounds were confirmed by elemental analysis, ~1H NMR and IR spectroscopy. The biological test results of the compounds to several pathogen proved that they were highly biological activities.Part two: Thirteen acylamides of N-acyl-DL-homocysteine thiolactones were synthesized by reaction of substituted phenoxyacetic acid, pyridine carboxylic acid and benzoic acid with DL-homocysteine thiolactone hydrochloride (ADTHC1) by means of preferable reaction conditions. These compounds were reported for the first time. The structures of the compounds were confirmed by elemental analysis, ~1H NMR and IR spectroscopy. The biological test results of the compounds to several pathogen proved that parts of them were highly biological activities.Part three: Four 2,6-pyridine diacyl-heterocyclic compounds were synthesized with 2,6-pyridine dicarboxylic acid and 3,5-dimethylpyrazole, 3,5-diphenylpyrazole, 2-mercapto-benimidazole and amino-3-dihydrothiophenon-2. The structures of the compounds were confirmed by elemental analysis, lH NMR and IR spectroscopy. The biological test results of the compounds to several pathogen proved that parts of them were highly biological activities.