477566-76-0Relevant academic research and scientific papers
Design, synthesis, pharmacological evaluation and DNA interaction studies of binuclear Pt(II) complexes with pyrazolo[1,5-a]pyrimidine scaffold
Lunagariya, Miral V.,Thakor, Khyati P.,Waghela, Bhargav N.,Pathak, Chadramani,Patel, Mohan N.
, (2018/01/22)
Substituted pyrazolo[1,5-a]pyrimidine ligands were synthesized by cyclization, using 3-(thiophen-2-yl)-1H-pyrazol-5-amine with substituted enones (3-phenyl-1-(pyridin-2-yl)prop-2-en-1-one) in presence of KOH and DMF as solvent to form cyclic aromatic compounds. The substituted pyrazolo[1,5-a] pyrimidine based binuclear PtII complexes containing neutral tetradentated ligands have general formula [Pt2(5a–5f)Cl4], (where, (5a -5f) = pyrazolo[1,5-a] pyrimidine ligand). This compounds were characterized by physicochemical and spectroscopic method like elemental analyses, UV-Visible, FT-IR, EDX, TGA, molar conductivity, magnetic susceptibility measurements, mass spectroscopy, 1H and 13C NMR method. The square planar geometry was predicted by electronic spectral study. All PtII compounds were evaluated by antimicrobial assay, in vitro brine shrimp assay, in vivo cellular level bioassay using S. Pombe cells and anti-tuberculosis study. LC50 (50% lethal concentration) values of compounds are observed between 6.450 - 102.07?μg/mL. UV-vis absorption titration, competitive displacement assay, molecular docking and viscosity measurement were carried out to examine the binding type and binding strength of complexes. The binding studies suggest partial intercalative binding mode of the complexes and the observed binding constant (Kb) values are found in the order of 6d > 6b > 6c > 6a > 6e > 6?f. The anti-proliferative cytotoxicity of the synthesized PtII complexes (6a-6f) were tested against the HCT-116 (Human Colorectal Carcinoma) cancer cell line.
Reinvestigation of synthesis of halo-substituted 3-phenyl-1-(2-pyridyl)-2-propen-1-ones (azachalcones). A tandem reaction for formation of penta-substituted cyclohexanols
Li, Chia-Wai,Shen, Tzu-Hsuan,Shih, Tzenge-Lien
, p. 4644 - 4652 (2017/07/11)
A systematic study of the synthesis of halo-substituted azachalcones was conducted. During the reaction course, we obtained not only the target azachalcones, but also penta-substituted cyclohexanols, which are seldom reported in the literatures. The forma
Synthesis, physicochemical properties, antimicrobial and antioxidant studies of pyrazoline derivatives bearing a pyridyl moiety
Lone, Imtiyaz Hussain,Khan, Khaliquz Zaman,Fozdar, Bharat Inder
, p. 363 - 369 (2014/03/21)
A series of new pyrazoline compounds bearing a pyridyl moiety (4a-i) were synthesized by condensing appropriate chalcones with hydrazine hydrate and tested for antimicrobial and antioxidant activities. According to in vitro antimicrobial activity against Bacillus subtilis, Staphylococcus epidermidis, Proteus vulgaris, Pseudomonas aeruginosa, Aspergillus niger and Penicillium chrysogenum and antioxidant activity by DPPH method, the compounds 4a, 4d, 4i and 4e, 4f, 4h showed maximum antimicrobial and antioxidant activities, respectively. Physiochemical properties and Lipinski's 'Rule of Five' analysis predicted higher intrinsic quality of the synthesized compounds and revealed that these compounds have good bioavailability and druglikeness properties.
Synthesis of mono-substituted 2,2′-bipyridines
Cordaro, Joseph G.,McCusker, James K.,Bergman, Robert G.
, p. 1496 - 1497 (2007/10/03)
The rapid synthesis of 4-aryl-2,2′-bipyridines is described leading to some previously reported compounds in good yields in addition to some new functionalized bipyridines.
