Chromanone or Chroman-4-one is the most important and interesting heterobicyclic compound and acts as a building block in medicinal chemistry for isolation, designing and synthesis of novel lead compounds. Structurally, absence of a double bond in chromanone between C-2 and C-3 shows a minor difference from chromone but exhibits significant variations in biological activities. In the present review, various studies published on synthesis, pharmacological evaluation on chroman-4-one analogues are addressed to signify the importance of chromanone as a versatile scaffold exhibiting a wide range of pharmacological activities. But, due to poor yield in the case of chemical synthesis and expensive isolation procedure from natural compounds, more studies are required to provide the most effective and cost-effective methods to synthesize novel chromanone analogs to give leads to chemistry community. Considering the versatility of chromanone, this review is designed to impart comprehensive, critical and authoritative information about chromanone template in drug designing and development.
A series of 3-(O-R) substituted compounds (SI-SX) of 2-(4-hydroxybenzyl) 3,5,7-trihydroxychroma-4-one were synthesized from easily accessible starting materials such as, p-hydroxybenzaldehyde and ethyl bromopyruvate. All the ten derivatives (SI-SX) were synthesized in appropriate yields, and they were characterized by IR, 1H NMR and C NMR. Molecular docking of all the derivatives were performed using Molegro virtual docker tool 6.0.2 (MVD) tool. CYCLOOXYGENASE-2 (COX2) or PROSTAGLANDIN SYNTHASE-2 was taken as the target protein and was downloaded from Research Collaboratory for Structural Bioinformatics (RCSB) Protein Data Bank (PDB) (https://www.rcsb.org/structure/1CX2) with PDBID: ICX2, 10.2210/pdb1CX2/pdb). The 3D images of ligand protein interactions were extracted using the software, MVD 6.0.2 visualizer interface. Among all the derivatives, SII, SVI has shown good moldock score values -77.59 and -75.75 with high number of interactions (09) towards the target protein, indicating its ability to act as an anti-inflammatory and analgesic activity.
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