Zhuravel' Irina O, Kovalenko Sergiy M, Ivachtchenko Alexandre V, Balakin Konstantin V, Kazmirchuk Victor V
National Pharmaceutical University, Kharkiv, Ukraine.
Bioorg Med Chem Lett. 2005 Dec 15;15(24):5483-7. doi: 10.1016/j.bmcl.2005.08.081. Epub 2005 Sep 23.
Several novel 2-imino-5-hydroxymethyl-8-methyl-2H-pyrano[2,3-c]pyridine-3-(N-aryl) carboxamides were prepared by reaction of pyridoxal hydrochloride with various N-arylcyanoacetamides. Reaction of these compounds with aromatic amines furnished a wide series of 2-(N-R-phenyl) imino-5-hydroxymethyl-8-methyl-2H-pyrano[2,3-c]pyridine-3-carboxamides. Antibacterial and antifungal activities of the synthesized compounds were studied. Most of the obtained compounds demonstrated significant activity against bacterial or fungal strains (MIC in the range of 12.5-25microg/mL), displaying comparable or even better efficacy than the standard drugs.
通过盐酸吡哆醛与各种N-芳基氰基乙酰胺反应制备了几种新型的2-亚氨基-5-羟甲基-8-甲基-2H-吡喃并[2,3-c]吡啶-3-(N-芳基)羧酰胺。这些化合物与芳香胺反应得到了一系列2-(N-R-苯基)亚氨基-5-羟甲基-8-甲基-2H-吡喃并[2,3-c]吡啶-3-羧酰胺。研究了合成化合物的抗菌和抗真菌活性。大多数所得化合物对细菌或真菌菌株表现出显著活性（最低抑菌浓度在12.5-25微克/毫升范围内），显示出与标准药物相当甚至更好的疗效。
