Current Issue : October - December Volume : 2016 Issue Number : 4 Articles : 6 Articles
Several amino acid Schiff base copper complexes have been synthesized in good yield and were characterized by IR spectral technique and physicochemical parameters. The synthesized derivatives were evaluated for antiepileptic activity and compound CN8 was found to be most potent compound. Derivatives of aromatic amino acid were more active than that of aliphatic amino acids....
A series of novel thiazolidinedione derivatives as peroxisome proliferator activated receptor-gamma (PPAR-gamma) agonists bearing stearic acid esters and amides as substituent’s in the positions 3 and 4 of the benzylidene moiety have been designed, synthesized and tested as potential antihyperglycemic agents. The compounds containing stearic acid (A1TU, A2TU, A3TU, A2TS and A3TS) exhibited the maximum activity (64.7-70.3 % BG reduction) among all the synthesized compounds. The compound A3TU has been found to exhibit the maximum activity. The docking simulation of the most active compound A3TU towards PPAR-γ receptor showed that the ligand-receptor complex was stabilized by hydrophobic interactions occurring between the lipophilic and aromatic moieties of the ligand and hydrophobic residues of the binding site. Its lipophilic and aromatic moieties were oriented towards the hydrophobic region lined by ARG-280, ILE-281, GLN-283, GLY-284, CYS-285, GLN-286, PHE-287, ARG-288, SER-289, ALA-292, VAL-293, VAL-322, HIS-323, ILE-326, TYR-327, LEU-330, LEU-333, VAL-339, LEU-340, ILE-341, SER-342, MET-348, PHE-363, MET-364, LYS-367, HIS-449, LEU-453, LEU-465, LEU-469, ILE-472 and TYR-473. The binding conformation of A3TU exhibited hydrogen bonding with ARG-288, TYR-473, HIS-323 and HIS-449. The stearic acid derivatives except A2TU showed better activity profile than rosiglitazone. Docking simulations performed on PPAR-γ receptor indicated that hydrophobic and hydrophilic key interactions may govern the drug receptor binding....
(5-substituted-1-benzofuran-2-yl) (4-substituted-2-substituted phenyl) methanone and its derivatives that have previously been synthesized in our laboratory were screened for in-vitro antioxidant activity. All the compounds showed good antioxidant activity. Among them compounds 4e, 4f and 4i showed promising antioxidant properties with minimum IC50 value (47.43-60.49)....
In continuation of our study on synthesizing series of novel coumarin based triazoles derivatives, as they possess good pharmacological activity and good yield, six ethyl coumarin derivatives were synthesized based on the click chemistry reaction of coumarin azide with ethyl substituted alkyne without catalyst in toluene under reflux temperature. All the compounds were characterized by IR, NMR and MS techniques....
In this present study a series of novel methyl coumarin based triazoles derivatives has been synthesized with good yields based on the click chemistry reaction of coumarin azide with methyl substituted alkyne without catalyst in toluene under reflux temperature. All the compounds were characterized by IR, NMR and MS techniques....
A series of (1E,2E)-1-((2-chloroquinolin-3-yl)methylene)-2-hydrazine derivatives (6a-j) were synthesized by reacting 2-chloroquinoline-3-carbaldehyde (3a) with hydrazine hydrate to yield (E)-1-((2-chloroquinolin-3-yl)methylene)hydrazine (4) which upon reacting with substituted benzaldehyde 5(a-j) in methanol yield the title compounds at room temperature. The synthesized compounds were characterized by FTIR, 1H-13C NMR and mass spectral analysis. The synthesized compounds were tested for in-vitro antiproliferative activity against breast (MCF-7), leukemic (K562), cervical (HeLa), colorectal adreno (Colo205) and hepato cellular (HepG2) cancer cell lines by MTT assay. The in-silico ADMET studies of the molecules were analyzed for their drug likeliness and toxic properties. The antiproliferative study reveals that compounds 6a, 6d were found to be active against HeLa, K562 and HepG2 cell lines, respectively when compared with the drug doxorubicin. The ADMET studies of title compounds found to be obeying the Lipinski rule of five and are non-toxic. The possible hits generated from the screening could be taken as hits in the development of lead molecules in drug discovery of new antiproliferative/cytotoxic entities from quinoline....
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