el-Kousy S M, el-Torgoman A M, el-Basiouny A A, Hashem A I
Chemistry Department, Faculty of Science, Menoufia University, Shebin El-Kom, A.R.E.
Pharmazie. 1988 Feb;43(2):80-1.
alpha-(2-Thienylidene)-gamma-aryl-delta beta,gamma-butenolides 1 are prepared by condensing thiophene-2-aldehyde with beta-aroylpropionic acids in sodium acetate-acetic anhydride mixture. The butenolides react with ammonia in ethanol to give the corresponding 5-oxo-2-pyrrolines 2. Hydrazine hydrate reacts with the butenolides 1 with the formation of the corresponding acrylic acid hydrazides 3. Ring closure of the latter hydrazides with hydrochloric/acetic acid mixture gives the pyridazinones 4. The biological activity of the synthesized compounds is tested against bacterial and yeast strains. The butenolides 1 and the oxopyrrolines 2 inhibit the growth of yeast and gram-negative strain. The hydrazides 3 and the pyridazinones 4 are effective on gram-positive strains.
α-（2-噻吩叉基）-γ-芳基-δβ，γ-丁烯内酯1是通过在乙酸钠-乙酸酐混合物中将噻吩-2-醛与β-芳酰基丙酸缩合制备的。丁烯内酯与乙醇中的氨反应生成相应的5-氧代-2-吡咯啉2。水合肼与丁烯内酯1反应生成相应的丙烯酸酰肼3。后者的酰肼与盐酸/乙酸混合物闭环得到哒嗪酮4。测试了合成化合物对细菌和酵母菌株的生物活性。丁烯内酯1和氧代吡咯啉2抑制酵母和革兰氏阴性菌株的生长。酰肼3和哒嗪酮4对革兰氏阳性菌株有效。
