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Schiff bases of sulphonamides as a new class of antifungal agent against multidrug-resistant Candida auris
MicrobiologyOpen ( IF 3.9 ) Pub Date : 2021-07-23 , DOI: 10.1002/mbo3.1218 Asad Hamad 1, 2 , Yiyuan Chen 2 , Mohsin A Khan 1 , Shirin Jamshidi 2 , Naima Saeed 2 , Melanie Clifford 3 , Charlotte Hind 3 , J Mark Sutton 3 , Khondaker Miraz Rahman 2
MicrobiologyOpen ( IF 3.9 ) Pub Date : 2021-07-23 , DOI: 10.1002/mbo3.1218 Asad Hamad 1, 2 , Yiyuan Chen 2 , Mohsin A Khan 1 , Shirin Jamshidi 2 , Naima Saeed 2 , Melanie Clifford 3 , Charlotte Hind 3 , J Mark Sutton 3 , Khondaker Miraz Rahman 2
Affiliation
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Invasive Candida infections in hospitalized and immunocompromised or critically ill patients have become an important cause of morbidity and mortality. There are increasing reports of multidrug resistance in several Candida species that cause Candidemia, including C. glabrata and C. auris, with limited numbers of antifungal agents available to treat patients with invasive Candida infections. Therefore, there is an urgent need to discover new antifungal agents that work against multidrug-resistant Candida species, particularly C. auris, which has been identified as an emerging global pathogen. In this article, we report a new class of antifungal agents, the Schiff bases of sulphonamides, that show activity against all Candida species tested, with an MIC range of 4–32 µg/ml. Compound 2b showed activity against C. glabrata and a panel of fluconazole-resistant C. auris strains, with MICs of 4–16 µg/ml. The drug-like nature of these Schiff bases offers opportunities to optimize these compounds with medicinal chemistry techniques to obtain more potent analogs that can be progressed toward pre-clinical evaluation.
中文翻译：
磺胺类希夫碱作为新型抗真菌剂对抗多重耐药念珠菌
住院和免疫功能低下或危重患者的侵袭性念珠菌感染已成为发病和死亡的重要原因。越来越多的报道表明，几种引起念珠菌血症的念珠菌属具有多重耐药性，其中包括念珠菌。光滑念珠菌和耳念珠菌，可用于治疗侵袭性念珠菌感染患者的抗真菌药物数量有限。因此，迫切需要发现针对多重耐药念珠菌，特别是念珠菌的新抗真菌剂。耳念珠菌，已被确定为一种新兴的全球病原体。在本文中，我们报告了一类新型抗真菌剂，即磺胺类希夫碱，它对所有测试的念珠菌均具有活性，MIC 范围为 4–32 µg/ml。化合物2b显示出针对C 的活性。 glabrata和一组耐氟康唑C . auris菌株，MIC 为 4–16 µg/ml。这些希夫碱的药物性质提供了利用药物化学技术优化这些化合物的机会，以获得更有效的类似物，并可进行临床前评估。
更新日期：2021-07-24
中文翻译：
磺胺类希夫碱作为新型抗真菌剂对抗多重耐药念珠菌
住院和免疫功能低下或危重患者的侵袭性念珠菌感染已成为发病和死亡的重要原因。越来越多的报道表明，几种引起念珠菌血症的念珠菌属具有多重耐药性，其中包括念珠菌。光滑念珠菌和耳念珠菌，可用于治疗侵袭性念珠菌感染患者的抗真菌药物数量有限。因此，迫切需要发现针对多重耐药念珠菌，特别是念珠菌的新抗真菌剂。耳念珠菌，已被确定为一种新兴的全球病原体。在本文中，我们报告了一类新型抗真菌剂，即磺胺类希夫碱，它对所有测试的念珠菌均具有活性，MIC 范围为 4–32 µg/ml。化合物2b显示出针对C 的活性。 glabrata和一组耐氟康唑C . auris菌株，MIC 为 4–16 µg/ml。这些希夫碱的药物性质提供了利用药物化学技术优化这些化合物的机会，以获得更有效的类似物，并可进行临床前评估。
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