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Exploring Benzo[h]chromene Derivatives as Agents against Protozoal and Mycobacterial Infections. | LitMetric

AI Article Synopsis

  • The study investigates the effectiveness of benzo[h]chromene derivatives against protozoa and mycobacteria, synthesizing 20 different compounds for testing.
  • Compounds displayed strong activity, with several outperforming the commonly used treatment benznidazole, indicating promising antiprotozoal properties.
  • The research highlights certain compounds' low IC values and high selectivity indices, suggesting their potential as viable alternatives to existing treatments for resistant infections.

Article Abstract

In this study, the efficacy of benzo[h]chromene derivatives as antiprotozoal and antimycobacterial agents was explored. A total of twenty compounds, including benzo[h]chromene alkyl diesters and benzo[h]chromene-triazole derivatives, were synthesized and tested against , , , and strains of and LIID-01. Notably, compounds , , , and exhibited superior activity against , with IC values of 19.2, 37.3, 68.7, and 24.7 µM, respectively, outperforming the reference drug benznidazole (IC: 54.7 µM). Compounds and showed excellent selectivity indices against , with SI values of 19 and 18, respectively, suggesting they could be potential alternatives to the commonly used, but more selective, miltefosine (IC: 64.0 µM, SI: 43.0). Additionally, compounds , , and were most effective against , with IC values of 24.9, 30.5, and 46.6 µM, respectively. Compounds and were particularly potent against various strains, highlighting their significance given the inherent resistance of these bacteria to standard antimicrobials. The sensitivity of LIID-01 to these compounds also underscored their potential in managing infections by the Mycobacterium avium-intracellulare complex.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11510191PMC
http://dx.doi.org/10.3390/ph17101375DOI Listing

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