Effective Synthesis
and Biological Evaluation of Functionalized
2,3-Dihydrofuro[3,2‑c]coumarins via an Imidazole-Catalyzed
Green Multicomponent Approach
Posted on 2022-09-29 - 20:04
For the first time, an eco-friendly and efficient one-pot
green
multicomponent approach has been described to synthesize functionalized trans-2,3-dihydrofuro[3,2-c]coumarins (DHFCs).
In this synthesis, imidazole and water were used as the catalyst and
solvent, respectively, under mild conditions. Applications of the
developed catalytic process in a water medium revealed the outstanding
activity, productivity, and broad functional group tolerance, affording
a series of newly designed DHFC and derivatives in excellent yields
(72–98%). Moreover, the human serum albumin (HSA) binding ability
of the synthesized DHFC derivatives has been uncovered through the
detailed in silico and in vitro-based structure-activity analysis.
The ability to bind HSA, the most abundant serum protein, in the low
micromolar ranges unequivocally reflects the suitable absorption,
distribution, metabolism, and elimination profile of the synthesized
compounds, which may further be envisaged for their therapeutic usage
endeavors.
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Mali, Ghanshyam; Maji, Sushobhan; Chavan, Kailas Arjun; Shukla, Manjari; Kumar, Manish; Bhattacharyya, Sudipta; et al. (2022). Effective Synthesis
and Biological Evaluation of Functionalized
2,3-Dihydrofuro[3,2‑c]coumarins via an Imidazole-Catalyzed
Green Multicomponent Approach. ACS Publications. Collection. https://doi.org/10.1021/acsomega.2c05361