US EPA

7457288 

Journal Article 

Design and synthesis of novel heterocyclic compounds as a ppar-γ agonist 

Zambare, YB; Bhole, RP; Chitlange, SS 

2020 

J. K. Welfare and Pharmascope Foundation 

11 

2 

2063-2069 

English 

10.26452/ijrps.v11i2.2147 

The multifarious metabolic syndrome, diabetes mellitus (DM), is a diseaseof concern all over the world and is approximate to affect 400 million indi-viduals by the 2020. Several classes of drugs at the moment are avail-able to lessen hyperglycemia in diabetes mellitus especially in Type-II. These drugs mostly have dangerous side effects and thus incisive for a new class of compounds is necessary to conquer this inconvenience. A series of 6 novel 5-nitrobenzofuran-2yl-carbamides derivatives were synthesized and molecular docking studies were performed on PPAR-γ target using (PDB code-4rfm).The preparation of5-nitro-1-benzofuran-2-carbohydrazide(4) on action with acetic acid, 1, 4-diaxone and sodium nitrite resulted in 5-nitro-1-benzofuran-2-carbonyl azide (5).The related compound (5) on action with substituted aromatic substituted amines undergoes Curtis type of rearrangement to give 5-nitro-N-(sub. carbamoyl)-1-benzofuran-2-carboxamide.The characterization and identification of prepared compounds were identified on the basis of NMR, IR, Mass and elemental analysis. Docking study of tar-geted compounds were done using software Autodock Tools 1.5.6 and visu-alisation done by Discovery Studio 3.5 software (Accelrys Inc. San Diego, CA USA). Molecular docking studies, the binding energies are determined to be in the range of –5.90 to –9.80 kcal/mol, with peroxisome proliferator activated receptor γ (PPAR-γ) receptors (PDB ID: 4RFM). The prepared compounds have been studied for their oral glucose tolerance test to distinguish the effect on plasma glucose level. © International Journal of Research in Pharmaceutical Sciences. 

1,4 dioxane; Benzofuran; Curtis rearrangement; Oral glucose Tolerance Test; 1.4 diaxone; 5 nitro 1 benzofuran 2 carbonyl azide; 5 nitro 1 benzofuran 2 carboxamide; 5 nitro 1 benzofuran 2 yl carbamate; 5 nitro benzofuran 2 carbohydrazide; 5 nitro benzofuran 2 carboxyazide; 5 nitro benzofuran carbamide; 5 nitro salicylaldehyde; acetic acid; acetic acid ethyl ester; aryl 5 nitro benzofuran 2 carbamide; benzaldehyde; benzofuran derivative; ethyl 5 nitro 1 benzofuran 2 carboxylate; ethyl 5 nitro benzofuran 2 carboxylate; glibenclamide; heterocyclic compound; hydrazine; peroxisome proliferator activated receptor gamma; peroxisome proliferator activated receptor gamma agonist; potassium carbonate; salicylaldehyde; sodium nitrite; sodium sulfate; toluene; unclassified drug; antidiabetic activity; Article; binding affinity; controlled study; diabetes mellitus; drug design; drug synthesis; elemental analysis; glucose blood level; human; hyperglycemia; infrared spectroscopy; liquid chromatography; mass spectrometry; melting point; molecular docking; non insulin dependent diabetes mellitus; nonhuman; nuclear magnetic resonance; oral glucose tolerance test; physical chemistry; thin layer chromatography