A series of novel N,N′′-diaryl cyanoguanidines were synthesized by reacting diphenyl N-cyanocarbonimidate with sulfanilamide followed by treatment of the obtained cyano-O-phenylisourea with substituted aromatic amines. The newly prepared N,N′′-diaryl cyanoguanidines showed a very interesting inhibition profile against four selected human carbonic anhydrase (CA, EC 4.2.1.1) isoforms, hCA I and hCA II (cytosolic), hCA IV (membrane-bound), and hCA IX (transmembrane). All these compounds showed a potent inhibition against isoform hCA II,with inhibition constants in the low nanomolar range, as well as a high selectivity for hCA II over hCA I, IV and IX. Since hCA II is an important drug target for antiglaucoma agents, these isoform-selective inhibitors may be considered of interest for further medicinal/pharmacologic studies.

通过使二苯基N-氰基碳酰亚胺酸酯与亚磺酰胺反应，然后用取代的芳族胺处理所得的氰基-O-苯基异脲，合成了一系列新颖的N，N′-二芳基氰基胍。新制备的N，N′′-二芳基氰基胍显示出对四种选定的人碳酸酐酶（CA，EC 4.2.1.1）同工型，hCA I和hCA II（胞质），hCA IV（膜结合）和hCA IX（跨膜）的非常有趣的抑制作用。所有这些化合物均显示出对同工型hCA II的有效抑制作用，其抑制常数在低纳摩尔范围内，并且对hCA II的选择性高于hCA I，IV和IX。由于hCA II是抗青光眼药物的重要药物靶标，因此这些同工型选择性抑制剂可能被认为是进一步医学/药理学研究的关注对象。