Binder D, Georgopoulos A, Noe C R, Nussbaumer J, Prager B C, Turnowsky F
Arzneimittelforschung. 1982;32(1):10-4.
The position selective synthesis of substituted pyrido[2,3-b]-pyrazine-1,4-dioxides is reported. Compound 3g was subjected to a series of screening-tests for antibacterial activity and compared to therapeutical standards. The range of antibacterial activity mainly comprises enterobacteriaceae, above all E. coli, Klebsiella, Proteus and Shigella strains. Activity against gram-positive organisms and Serratia is much weaker and completely lacking with Pseudomonas. Therapeutic activity in septicaemic infections of the mouse is very good, especially in the case of E. coli infection with an ED50 of 13 mg/kg mouse for s.c. application. With p.o. application 3g shows activity comparable to nalidixic acid and nitrofurantoin in the experimental acute pyelonephritis in the mouse. The activity of 3g, however, is clearly inferior to that of gentamicin.
报道了取代吡啶并[2,3 - b] - 吡嗪 - 1,4 - 二氧化物的位置选择性合成。对化合物3g进行了一系列抗菌活性筛选试验，并与治疗标准进行了比较。抗菌活性范围主要包括肠杆菌科，尤其是大肠杆菌、克雷伯菌、变形杆菌和志贺菌属菌株。对革兰氏阳性菌和沙雷氏菌的活性较弱，对假单胞菌则完全没有活性。在小鼠败血症感染中的治疗活性非常好，特别是在大肠杆菌感染的情况下，皮下注射的半数有效剂量（ED50）为13mg/kg小鼠。口服时，在小鼠实验性急性肾盂肾炎中，3g的活性与萘啶酸和呋喃妥因相当。然而，3g的活性明显低于庆大霉素。
