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由于磺胺有利尿作用并且证明了它能抑制碳酸酐酶,1950年罗伯林(Roblin)和克来伯(Clapp)乃开始综合大量的磺胺衍化物以寻找更强有力的碳酸酐酶抑制者。Miller等乃发现了醋唑磺胺(Diamox),具有更强的利尿作用,但在用此药过程中常易失效而引起严重的低钾症。在1957年Novello和Spraque二人合成了氯噻嗪又名氯散疾(Chlorothiazidum,Diuril, 或Chlorurit),以后又合成了一系列的衍化物。当时的设想是将醋唑磺胺化学构造中的一个磺胺基团加至两个,第二个磺胺基放在圜内使成杂圜,企图加强抑制碳酸酐酶作用。实验结果大出意
Because of the diuretic effect of sulfanilamide and its demonstrated ability to inhibit carbonic anhydrase, Roblin and Clapp began to synthesize large amounts of sulfonamide derivatives in 1950 in search of more potent carbonic anhydrase inhibitors. Miller et al. Found Diamox, a more potent diuretic, but caused severe hypokalemia when used in the drug. In 1957, Novello and Spraque both synthesized chlorothiazide, also known as Chlorothiazidum (Diuril, or Chlorurit), and later synthesized a series of derivatives. The idea at that time was to add one sulfonamide group to the acetosyringosine chemical construct and the second sulfanilamide to make it a miscellaneous compound in an attempt to enhance the inhibition of carbonic anhydrase. Experimental results of the big idea