The differential scanning fluorimetry (DSF) screening of 5.692 fragments in combination with benzenesulfonamide (BSA) against bovine carbonic anhydrase (bCA) delivered >100 hits that either caused, on their own, a significant thermal shift (ΔTm, °C) in the protein melting temperature or significantly influenced the thermal shift observed for BSA alone. Three hits based on 1,2,3-triazole moiety represent the periphery of the recently reported potent inhibitors of hCA II, IX and XII which were efficacious in vivo. Such a re-discovery of suitable BSA periphery essentially validates the new fragment-based approach to the discovery of future CAIs. Structures of other validated fragment hits are reported.

中文翻译：

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通过差示扫描荧光法筛选苯磺酰胺与化学多样化片段组合抗碳酸酐酶。


差示扫描荧光法 (DSF) 筛选 5.692 个片段，结合苯磺酰胺 (BSA) 对抗牛碳酸酐酶 (bCA)，结果显示 >100 命中率，这些命中率要么单独引起蛋白质的显着热位移（ΔTm，°C）熔化温度或显着影响单独观察到的 BSA 的热位移。基于 1,2,3-三唑部分的三个命中代表了最近报道的在体内有效的 hCA II、IX 和 XII 的有效抑制剂的外围。这种对合适 BSA 外围设备的重新发现本质上验证了基于片段的新方法来发现未来 CAI。报告了其他经过验证的片段命中的结构。