Synthesis and antibacterial activities of some chloro analogs of 3-amino-3,4-dihydro-1-hydroxycarbostyril
作者:Alvie L. Davis、William H. Chambers、Don H. Kelley、David A. Fell、John R. Haynes、Karen L. Hulme、Larry D. Gage、Tommy J. McCord
DOI:10.1021/jm00241a022
日期:1975.7
dextranicum 8086, and Lactobacillus plantarum 8014. The relative inhibitory activities of the chloro analogs were 7-Cl greater than 6-Cl greater than 8-Cl greater than 5-Cl in E. coli and 7-Cl greater than 6-Cl greater than 8-Cl = 5-Cl in L. dextranicum and L. plantarum. In each of the three microorganisms, the 7-Cl analog was a more effective growth inhibitor than the parent unsubstituted compound. The growth
确定了氯取代基对3-氨基-3,4-二氢-1-羟基卡司他韦的微生物活性的影响。通过适当的氯取代的邻硝基硝基丙氨酸的还原环化反应合成5-,6-和7-氯类似物,而从N-三氟乙酰基-3-氯-2-硝基苯丙氨酸乙酯获得8-氯类似物。 。观察到所有这些化合物均能抑制大肠杆菌9723,葡聚糖亮葡聚糖8086和植物乳杆菌8014的生长。氯类似物的相对抑制活性为7-Cl大于6-Cl大于8-Cl大于5-大肠杆菌中的Cl和大于6-Cl的7-Cl大于右旋乳酸杆菌和植物乳杆菌的8-Cl = 5-Cl。在这三种微生物中,7-Cl类似物是比母体未取代化合物更有效的生长抑制剂。事实证明,这类化合物的生长抑制活性比四种相应的内酰胺类(3-氨基-3,4-二氢咔唑的5-,6-,7-和8-氯类似物)更有效。