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Design, synthesis and biological activity of novel triazine inhibitors of Candida albicans secreted aspartic protease 2
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Ji YANG1, Guo-qiang DONG2, Na LIU2, *, Chun-quan SHENG1, 2, *
Acta Pharmaceutica Sinica | 2020, 55(7) : 1647 - 1660
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Acta Pharmaceutica Sinica | 2020, 55(7): 1647-1660
• Original Articles •
Design, synthesis and biological activity of novel triazine inhibitors of Candida albicans secreted aspartic protease 2
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Ji YANG1, Guo-qiang DONG2, Na LIU2, *, Chun-quan SHENG1, 2, *
Affiliations
  • 1. School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China
  • 2. School of Pharmacy, Second Military Medical University, Shanghai 200433, China
Published: 2020-07-12 doi: 10.16438/j.0513-4870.2020-0880
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In recent years, the incidence and mortality of invasive fungal infections has increased. It is highly desirable to develop novel antifungal agents with new modes of action. Targeting virulence factors represents a new strategy for antifungal drug discovery. Secreted aspartic protease 2 (SAP2), a kind of virulence factor, is an emerging antifungal target. However, discovery of small-molecule SAP2 inhibitors remains a significant challenge. Based on the structure-activity relationship of our previously identified triazine small-molecule SAP2 inhibitor, we were able to identify two potent inhibitors, 8a and 8c, which showed excellent in vivo antifungal activity for the treatment of C. albicans infection. Moreover, compounds 8a and 8b effectively inhibited fungal biofilm. Taken together, triazine SAP2 inhibitors represent promising lead compounds for the discovery of novel antifungal agents.

triazine derivative  /  SAP2 inhibitor  /  virulence factor
Ji YANG, Guo-qiang DONG, Na LIU, Chun-quan SHENG. Design, synthesis and biological activity of novel triazine inhibitors of Candida albicans secreted aspartic protease 2[J]. Acta Pharmaceutica Sinica, 2020 , 55 (7) : 1647 -1660 . DOI: 10.16438/j.0513-4870.2020-0880
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Article Info
doi: 10.16438/j.0513-4870.2020-0880
  • Receive Date：2020-06-01
  • Online Date：2026-01-21
  • Published：2020-07-12
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History
  • Received：2020-06-01
  • Revised：2020-06-24
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Affiliations
    1. School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China
    2. School of Pharmacy, Second Military Medical University, Shanghai 200433, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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