Lasamide,\na Potent Human Carbonic Anhydrase Inhibitor\nfrom the Market: Inhibition Profiling and Crystallographic Studies

Lasamide is a synthetic precursor and a contaminant of\nthe diuretic\nFurosemide manufacturing process and represents a highly valuable\nbuilding block for fragment-based drug discovery approaches. We assessed\nthe ability of Lasamide to inhibit in vitro the human-expressed Carbonic\nAnhydrases by means of the stopped-flow technique, and we assessed\nits binding modes within hCAs II and XII-mimic catalytic clefts by\nX-ray crystallography. Interestingly, an unprecedented crystal form\nfor the hCA IX mimic H-tag is reported and discussed herein.