The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 2-Furoic hydrazide( cas:3326-71-4 ) is researched.Computed Properties of C5H6N2O2.Dige, Nilam C.; Mahajan, Prasad G.; Raza, Hussain; Hassan, Mubashir; Vanjare, Balasaheb D.; Hong, Hansol; Hwan Lee, Ki; Latip, Jalifah; Seo, Sung-Yum published the article 《Ultrasound mediated efficient synthesis of new 4-oxoquinazolin-3(4H)-yl)furan-2-carboxamides as potent tyrosinase inhibitors: Mechanistic approach through chemoinformatics and molecular docking studies》 about this compound( cas:3326-71-4 ) in Bioorganic Chemistry. Keywords: oxoquinazolinyl furancarboxamide green preparation tyrosinase inhibitor chemoinformatic docking antioxidant; isatoic anhydride furoic hydrazide salicylaldehyde acid catalyst ultrasound irradiation; Drug score; Lipinski’s rule; Molecular docking; Oxoquinazolin-3(4H)-yl)furan-2-carboxamides; Tyrosinase; Ultrasound sonication. Let’s learn more about this compound (cas:3326-71-4).
Synthesis of new (4-oxoquinazolin-3(4H)-yl)furan-2-carboxamide derivatives I [R = H, 5-Br, 3-NO2, etc.] via p-TSA catalyzed reaction between isatoic anhydride, 2-furoic hydrazide and substituted salicylaldehydes in ethanol:water (5:5 volume/volume) solvent system under ultrasound irradiation at room temperature was carried out. The important features of this protocol were simple and easy workup procedure, reaction carried out at ambient temperature, use of ultrasound and high yield of (4-oxoquinazolin-3(4H)-yl)furan-2-carboxamides in short reaction time. The synthesized compounds I were screened against tyrosinase enzyme and all these compounds found to be potent inhibitors with much lower IC50 value of 0.028 ± 0.016 to 1.775 ± 0.947 μM than the standard kojic acid (16.832 ± 1.162 μM). The kinetics mechanism for compound I [R = 3,5-di-Br] was analyzed by Lineweaver-Burk plots which revealed that compound inhibited tyrosinase non-competitively by forming an enzyme-inhibitor complex. Along with this all the synthesized compounds I were scanned for their DPPH free radical scavenging ability. The outputs received through in vitro and in silico anal. were coherent to the each other with good binding energy values (kcal/mol) posed by synthesized ligands.
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Reference:
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics