Fig 2 - uploaded by Jimish Patel
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![Reaction scheme 4-((4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)phenyl)thio)-N-(2-morpholinoethyl)picolinamide (R1) Yield (%): 52.8, IR (KBr, Vmax, cm -1 ): 3327 (NH str), 1724 (C=O str), 1648 (C=O str), 1338 (CF3), 1116 (Aliphatic ether), 804(C-Cl) 699 (C-S), 1 H NMR (400MHz, DMSO) δ ppm: 2.35-2.37 (t, 4H, CH2), 2.51-2.54 (t, 2H, CH2), 3.34-3.36 (t, 2H, CH2), 3.64-3.67 (t, 4H, CH2), 7.35-7.36 (d, 2H, ArH), 7.63-7.64 (d, 1H, ArH), 7.74-7.76 (d, 1H, ArH), 7.89-7.91 (m, 3H, ArH), 8.05 (s, 2H, ArH and amide), 8.27 (s, 1H, ArH), 8.74-8.76 (d, 1H, ArH), 9.10 (s, 1H, CONH), 9.24 (s, 1H, CONH), 13 C NMR (DMSO) δ ppm: 54, 55.8 (x2), 57.6, 66.7 (x2), 118.8, 120.5 (x2), 123.3, 124.9, 126.4 (x2), 128.5, 128.9, 129.1, 129.3, 129.5, 132.0, 134.3, 136.2, 140.5, 148.2, 151.9, 152.9, 160.7. Mass (LC-MS): m/z: 581.1[M+H] + ,583.2[M+2] +](profile/Jimish-Patel-2/publication/360092645/figure/fig1/AS:1167613631700992@1655392191057/Reaction-scheme.png)
Reaction scheme 4-((4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)phenyl)thio)-N-(2-morpholinoethyl)picolinamide (R1) Yield (%): 52.8, IR (KBr, Vmax, cm -1 ): 3327 (NH str), 1724 (C=O str), 1648 (C=O str), 1338 (CF3), 1116 (Aliphatic ether), 804(C-Cl) 699 (C-S), 1 H NMR (400MHz, DMSO) δ ppm: 2.35-2.37 (t, 4H, CH2), 2.51-2.54 (t, 2H, CH2), 3.34-3.36 (t, 2H, CH2), 3.64-3.67 (t, 4H, CH2), 7.35-7.36 (d, 2H, ArH), 7.63-7.64 (d, 1H, ArH), 7.74-7.76 (d, 1H, ArH), 7.89-7.91 (m, 3H, ArH), 8.05 (s, 2H, ArH and amide), 8.27 (s, 1H, ArH), 8.74-8.76 (d, 1H, ArH), 9.10 (s, 1H, CONH), 9.24 (s, 1H, CONH), 13 C NMR (DMSO) δ ppm: 54, 55.8 (x2), 57.6, 66.7 (x2), 118.8, 120.5 (x2), 123.3, 124.9, 126.4 (x2), 128.5, 128.9, 129.1, 129.3, 129.5, 132.0, 134.3, 136.2, 140.5, 148.2, 151.9, 152.9, 160.7. Mass (LC-MS): m/z: 581.1[M+H] + ,583.2[M+2] +
Source publication
A novel series of pyridine ring containing diaryl urea derivatives (R1-R9) were synthesized in four chemical steps using pyridine-2-carboxylic acid as starting material. The synthesized compounds were design by using Autodock vina in the crystal structure of the Kinase domain of Human B-raf (PDB ID: 4DBN) to get insights into structural requirement...
Citations
... The quinazoline is ubiquitous in pharmaceutical (2)(3)(4)(5), Natural product like lactones, alkaloids and terpenoids (6)(7)(8), dyes (9,10), agrochemicals (11)(12)(13) and Material science like luminescent material (14,15) so Indolo[2,1-b]quinazoline-6,12-dione (Tryptanthrin) is important class of heterocycle containing promising pharmacophore. They have anti-inflammatory (16,17), Antifungal (18), Anti-microbial (19)(20)(21)(22), anti-malarial (23)(24)(25)(26)(27)(28)(29), anti-viral (30), anti-cancer (31)(32)(33)(34)(35)(36)(37)(38)(39)(40)(41)(42), antitubercular (43)(44)(45)(46),Anti-trypanosomal (47), Anti-leishmanial activities (48),intestinal disorder (49), Photoelectric and surface activities (50)(51)(52)(53). ...
Synthesis of Spiro-Pyrrolizine and Pyrrolidine derivative of Tryptanthrin and Evaluation of Their anti-bacterial, anti- fungal and anti-mycobacterial activities.
... Since 1884 various synthetic drug molecules are used for the treatment of various disease due to structural similarities with these endogenous molecule. 8 Synthesis of dihydropyrimidine has great importance as these derivative are used as antiviral, anti-infective, antibacterial, anticancer, antioxidant, anti-proliferative drugs. Pyrimidine heterocycle is important in many medicinal agents with diverse activity especially anticancer because it inhibits kinase activity and also act on cell cycle by apoptosis 9 . ...
Synthesis of Substituted 2-[(2-chloro-4-oxo-3-phenylazetidin-1-yl)amino]-1-methyl-6-oxo-4-phenyl-1,6-dihydropyrimidine-5-carbonitrile(6a-r) and 1-methyl-6-oxo-2-[(4-oxo-2-phenyl-1,3-thiazolidin-3-yl)amino]-4-phenyl-1,6-dihydropyrimidine-5-carbonitrile (7a-o)Derivatives was completed using aromatic aldehyde, ethylcyanoacetate and thiourea in absolute ethanol as per the standard procedure.The completion of reactionmonitored by TLC and structure were confirmed by spectroscopic method viz FT-IR and 1H NMR and elemental analysis.The affinity of synthesized compounds with CDK4 protein was predicted by molecular docking studies. The docking results showed that compound 6l, 6p and 6r has highest affinity with CDK4 protein with minimum energy with good hydrogen bonding interaction.
