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In the past century, hundreds of medicinal chemists focused their efforts on explorations of urease inhibitors. Despite the FDA\u2019s approval of acetohydroxamic acid as a urease inhibitor for the treatment of struvite nephro-lithiasis and the widespread use of N-(n-butyl)thiophosphoric triamide as a soil urease inhibitor as nitrogen fertilizer synergists in agriculture, urease inhibitors with high potency and safety are urgently needed. Exploration of novel urease inhibitors has therefore become a hot research topic recently. Herein, inhibitors identified worldwide from 2016 to 2021 have been reviewed. They structurally belong to more than 20 classes of compounds such as urea\/thioure analogues, hydroxamic acids, sul-fonamides, metal complexes, and triazoles. Some inhibitors showed excellent potency with IC50 val-ues lower than 10 nM, having 10000-fold higher potency than the positive control thiourea.<\/jats:p>\n<\/jats:sec>","DOI":"10.2174\/1568026621666211129095441","type":"journal-article","created":{"date-parts":[[2021,11,30]],"date-time":"2021-11-30T04:35:55Z","timestamp":1638246955000},"page":"95-107","update-policy":"https:\/\/doi.org\/10.2174\/bsp_crossmark_policy","source":"Crossref","is-referenced-by-count":39,"title":["Recent Efforts in the Discovery of Urease Inhibitor Identifications"],"prefix":"10.2174","volume":"22","author":[{"given":"Wan-Qing","family":"Song","sequence":"first","affiliation":[{"name":"Hunan Provincial Key Laboratory of Research, Resource Mining and High-valued Utilization on Edible &amp; Medicinal\nPlant, Hunan Engineering Laboratory for Analyse and Drugs Development of Ethnomedicine in Wuling Mountains,\nNational Demonstration Center for Experimental Chemistry Education, Jishou University, Jishou 416000, P.R. 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