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Updated: May 8, 2025
![Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F60786.jpg&w=3840&q=50)
Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions
Published on: July 17, 2020
Exploration of Benzofuran/Indole-Chalcone Conjugated 1,2,3-Triazole Hybrids as Candida glabrata Agents: Design,
Anuradha Singampalli1, Rani Bandela1, Pardeep Kumar1
1Department of Chemical Sciences, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, India.
Abstract:
A novel series of benzofuran/indole-chalcone linked 1,2,3-triazole hybrids (4a-k, 8a-h) were synthesized to explore their potential as antifungal agents. Among the 19 derivatives, 4b, 4c, 4i, 4j, and 8a showed inhibition against Candida glabrata at 50 µg/mL concentration that is comparable to the control drug fluconazole. Compounds 4b, 4c, and 4j showed greater activity at low concentrations (25 and 12.5 µg/mL). Among them, 4j exhibited the highest potency, with 81.82% inhibition against C. glabrata at 50 µg/mL. Compound 4j exhibited better safety profiles against human acute monocytic leukemia cells. In structural activity studies, chloro (Cl) at the 2,6th position of the phenyl ring of chalcone and p-CN substitution on the benzyl triazole moiety maximizes the potential. In addition, in silico ADME analysis supports the drug-likeness profile and strengthens the data. So, compound 4j can be used as an effective lead to develop a potent and safer antifungal drug candidate to combat Candida infections.
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