Design, docking, synthesis and biological evaluation of novel isoindole-1,3-(2H)-diones
By: Raj Kumar, T
.
Contributor(s): VAmsi Krishna, L. V.
Publisher: New Delhi CSIR 2019Edition: Vol.58b(9), Sep.Description: 1056-1062p.Subject(s): GENERAL CHEMISTRYOnline resources: Click here
In:
Indian journal of chemistry (Section B)Summary: Isoindole-1,3(2H)-diones have various biological activities like anti-tubercular, anti-convulsant, anti-inflammatory, anti-microbial, anti-influenza, anti-angiogenesis, anti-viral. The present study involves the docking of these derivatives by various anti tubercular and microbial targets like 1MRU, 2A87, 1SM8 1NKT, 1AAQ and 1A30 by using Hex 8.0 andthe synthesis involves the reaction of 4-amino acetophenone withpthalic anhydride andthen with different aldehydes to give 2-{4-[(2E)-3-phenylprop-2-enoyl]phenyl}-1H-isoindole-1,3(2H)-diones which were converted to 2-[4-(2-amino-6-phenyl-6H-1,3-oxazin-4-yl)phenyl]-1H-isoindole-1,3(2H)-diones (3a-e). The structures are proposed based on their 1H and 13C NMR, and mass spectral and FT-IR data. All the synthesized compounds have been screened for anti-tubercular, anti-inflammatory and anti-microbial activities. 3b, 3c, 3e have shown the highest activity at 25 μg/mL against Mycobaterium tuberculosispathogen. In vitro anti-inflammatory activity of the synthesized moieties in heat induced haemolysis 3b and 3e have shown 73.01% and 65.90% inhibition at 500 μg/mL, In bovine albumin denaturation, 3c and 3e have shown 79.86% and 78.72% inhibition at 500 μg/mL and 3d has MIC of 0.8 μL/mL have shown highest activity than standard ciprofloxacin2 μL /mLtowards gram positive Staphylococus aureus.
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School of Pharmacy Archieval Section | Not for loan | 2020688 |
Isoindole-1,3(2H)-diones have various biological activities like anti-tubercular, anti-convulsant, anti-inflammatory, anti-microbial, anti-influenza, anti-angiogenesis, anti-viral. The present study involves the docking of these derivatives by various anti tubercular and microbial targets like 1MRU, 2A87, 1SM8 1NKT, 1AAQ and 1A30 by using Hex 8.0 andthe synthesis involves the reaction of 4-amino acetophenone withpthalic anhydride andthen with different aldehydes to give 2-{4-[(2E)-3-phenylprop-2-enoyl]phenyl}-1H-isoindole-1,3(2H)-diones which were converted to 2-[4-(2-amino-6-phenyl-6H-1,3-oxazin-4-yl)phenyl]-1H-isoindole-1,3(2H)-diones (3a-e). The structures are proposed based on their 1H and 13C NMR, and mass spectral and FT-IR data. All the synthesized compounds have been screened for anti-tubercular, anti-inflammatory and anti-microbial activities. 3b, 3c, 3e have shown the highest activity at 25 μg/mL against Mycobaterium tuberculosispathogen. In vitro anti-inflammatory activity of the synthesized moieties in heat induced haemolysis 3b and 3e have shown 73.01% and 65.90% inhibition at 500 μg/mL, In bovine albumin denaturation, 3c and 3e have shown 79.86% and 78.72% inhibition at 500 μg/mL and 3d has MIC of 0.8 μL/mL have shown highest activity than standard ciprofloxacin2 μL /mLtowards gram positive Staphylococus aureus.
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