- Synthesis, characterization and in vitro antimicrobial evaluation of some novel hydrazone derivatives bearing pyrimidinyl and pyrazolyl moieties as a promising heterocycles
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In the present investigation, ten new 2-((3-aryl-1-phenyl-1H-pyrazol-4-yl)methylene)-1-(4,6-dimethylpyrimidin-2-yl)hydrazine (3a-j) having pyrimidinyl and pyrazolyl moieties were synthesized. Structures of all compounds were confirmed by their spectral and elemental data. Most of the tested compounds were found to be significantly more effective against bacterial strains Staphylococcus aureus, Bacillus subtilis and Pseudomonas aeruginosa than the reference drug ciprofloxacin. All the newly synthesized compounds were found to be more potent antifungal agents than reference drug against Candida albicans, whereas except 3e all other compounds also shown good activity against Saccharomyces cerevisiae.
- Kamal, Raj,Kumar, Vipan,Bhardwaj, Vikas,Kumar, Vikas,Aneja, Kamal Rai
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- Synthesis and antiviral activity of nonannulated tetrazolylpyrimidines
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[Figure not available: see fulltext.] Nonannulated tetrazolylpyrimidines in the structure of which the heterocyclic fragments are separated by hydrazinocarbonylmethyl, methylpyrazolyl groups or a sulfur atom were synthesized. Some of these compounds showed moderate in vitro activity against H1N1 subtype of influenza A virus. The selectivity index of the anti-influenza action of {5-[(4,6-dimethylpyrimidin-2-yl)sulfanyl]-1H-tetrazol-1-yl}acetic acid, which has very low cytotoxicity, was twice as high as the selectivity index of the reference drug rimantadine.
- Ostrovskii, Vladimir А.,Danagulyan, Gevorg G.,Nesterova, Olga M.,Pavlyukova, Yulia N.,Tolstyakov, Vladimir V.,Zarubina, Olga S.,Slepukhin, Pavel А.,Esaulkova, Yana L.,Muryleva, Anna А.,Zarubaev, Vladimir V.,Trifonov, Rostislav E.
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p. 448 - 454
(2021/05/21)
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- Solvatochromic behavior of a pyrene-pyrimidine-based Schiff base and detection of heavy metal ions in aqueous media
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The synthesis and solvatochromic behavior of pyrimidine based Schiff-base (PYPH) were studied to develop a fluorescent chemo sensor for the detection of Hg2+ in aqueous solution. The characterization of PYPH was investigated on the basis of UV–vis, FTIR, 1H-NMR and mass spectral data. PYPH displays selective fluorescent turn-off response to Hg2+ in aqueous solution. The sensitivity and selectivity of PYPH toward Hg2+ among different metal ions was examined by absorption, fluorescence, 1H-NMR and mass spectral studies. Binding stoichiometry (2:1) has been confirmed by a Job’s plot, HRMS spectral studies and 1H-NMR analysis. A low detection limit was 4.2 × 10?6 M for Hg2+. Ground state geometry of PYPH has been optimized using density functional theory (DFT). These results demonstrate that PYPH has promise to detect Hg2+ ion in environmental analysis systems.
- Ghosh, Swadesh,Singharoy, Dipti,Konar, Saugata,Naskar, Jnan Prakash,Bhattacharya, Subhash Chandra
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p. 1272 - 1283
(2021/03/26)
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- Nonionic Surfactants as Potential Carriers of a Synthesized Pyrimidine Derivative: Spectroscopic and Quantum Chemical Investigations
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Currently, a major problem is the poor water solubility and bioavailability of many pharmaceuticals. Using different types of surfactants is an effective strategy to overcome this problem. Herein a pyrimidine-based Schiff base, 2-[2-(anthracen-9-ylmethylene) hydrazinyl]-4,6-dimethyl pyrimidine (ANHP), has been synthesized and characterized by different spectroscopic methods. A comparative study of drug carrier properties of cationic, anionic, and the nonionic surfactants with this pyrimidine derivative (ANHP) in aqueous solution is the key research interest of this work. From fluorescence studies, the interaction of ANHP with the different types of surfactants were compared and binding constants of ANHP in vesicles were determined. The drug carrier properties of different surfactants were investigated by using different spectroscopic techniques. DLS, zeta potential, and AFM studies have shown that in the presence of ANHP, nonionic surfactants take a vesicular shape. Several experimental results clearly indicate that Ig-720 is the better choice as ANHP carrier among all the surfactants investigated. In addition, the structure of ANHP has been optimized by density functional theory (DFT). The theoretical and experimental results have been compared.
- Ghosh, Swadesh,Singharoy, Dipti,Dhara, Anamika,Naskar, Jnan Prakash,Bhattacharya, Subhash Chandra
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p. 2695 - 2701
(2018/06/27)
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- A spectroscopic exploration of the influence of charge donor group on ESIPT process and its consequences in a salicylimine
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Photophysical properties of a newly designed synthetic compound DYMDAP have been investigated in combination with computational calculations. DYMDAP shows a solvent dependent emissive behavior which in non-polar solvents shows two distinct peaks along wit
- Makhal, Subhash Chandra,Bhattacharyya, Arghyadeep,Ghosh, Soumen,Guchhait, Nikhil
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p. 138 - 146
(2018/03/21)
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- PROTEOSTASIS REGULATORS FOR TREATING CYSTIC FIBROSIS AND OTHER PROTEIN MISFOLDING DISEASES
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The present invention is directed to compounds of Formulae (Ia-Ib), (Ila-IId), (Illa- Illb), (IV), (V), (VI), (Vlla-VIIc), (VIII), (IXa-IXb), (Xa-Xb), (XIa-XIb) and (Xlla-XIIb), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis.
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Page/Page column 60
(2012/12/13)
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- Synthesis of new triazolopyrimidines and substituted pyrimidines.
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Hydrazinopyrimidine 3 was prepared and transformed into 4, 5 by the reaction with Ar-Cl and POCl3, respectively. Also 3 transformed into 6, 7 by the reaction with ArCHO and FeCl3 respectively. Compound 8 was prepared and transformed into 9, 10, 11 by the reaction with DDC, ethyl bromoacetate and Sodium ethoxide respectively.
- Ouf
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p. 275 - 279
(2007/10/03)
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- Amino-substituted pyrimidines, derivatives and methods of use therefor
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The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation end products of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
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- SYNTHESIS OF SUBSTITUTED METHYL ARYL KETONE PYRIMIDINYLOXIMES AND THEIR REACTIONS WITH NUCLEOPHILES
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Chloropyrimidines react readily with the sodium salts of alkyl aryl ketoximes to give acetophenone O-(2,4-dimethylpyrimidin-6-yl)- and O-(4,6-dimethylpyrimidin-2-yl)oximes, the oximino-groups in which readily undergo nucleophilic substitution.
- Danagulyan, G. G.,Balasanyan, N. G.,Terent'ev, P. B.,Zalinyan, M. G.
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p. 1369 - 1373
(2007/10/02)
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