- Pyrimidine-thiazolidinone derivatives
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Pyrimidine-thiazolidinone derivatives may be used for preventing or treating diseases in humans or animals, and have demonstrated efficacy specifically in treating type-2 diabetes. Methods of synthesizing the pyrimidine-thiazolidinone derivatives, described herein, can provide high yields in a short time and with high purity. The pyrimidine-thiazolidinone derivatives demonstrate improved hypoglycemic activity compared to most anti-diabetic drugs currently available.
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Page/Page column 11; 3
(2020/07/09)
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- Antibacterial activity and mechanism of action of the benzazole acrylonitrile-based compounds: In?vitro, spectroscopic, and docking studies
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A new series of pyrimidine derivatives 5, 9a-d and 12a-d was synthesized by an efficient procedure. The antibacterial activity of the new compounds was studied against four bacterial strains. Compound 5 was found to exhibit the highest potency, with?=?1.0?μg/ml, against both Escherichia coli and Pseudomonas aeruginosa when compared with amoxicillin (MIC?=?1.0–1.5?μg/mL). Transmission electron microscope results confirmed that activities against bacteria occurred via rupturing of the cell wall. Molecular modeling results suggested that compounds 5, 9a-d and 12a-d have the potential to irreversibly bind to the penicillin-binding protein (PBP) Ser62 residue in the active site and were able to overcome amoxicillin resistance in bacteria by inhibiting the β-lactamase enzyme. Docking studies showed that compounds 5, 9a-d and 12a-d inhibit the β-lactamase enzyme through covalent bonding with Ser70. The synergistic effect with amoxicillin was studied. The newly synthesized compounds reported in this study warrant further consideration as prospective antimicrobial agents.
- AlNeyadi, Shaikha S.,Salem, Alaa A.,Ghattas, Mohammad A.,Atatreh, Noor,Abdou, Ibrahim M.
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p. 270 - 282
(2017/05/15)
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- HETEROARYL SUBSTITUTED HETEROCYCLYL SULFONES
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The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 134
(2015/11/09)
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- NEW COMPOUNDS
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The present invention provides certain compounds according to formula (I) which are inhibitors of SSAO activity wherein V, W, X, Y, Z, R1 and R2 are as defined in the specification.
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- Synthesis of Soai Type 2-Arylpyrimidine-5-carbaldehydes through Desulfurative Cross-Coupling with Arylboronic Acids
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A two-step synthesis of 2-arylpyrimidine-5-carbaldehydes, which are of relevance as substrates for Soai's asymmetric autocatalysis, was realized by exploiting a hidden threefold symmetry in the target core structure. Condensation of Arnold's C 3-symmetric vinamidinium cation with S-methylisothiouronium sulfate provides 2-methylsulfanyl-pyrimidine-5-carbaldehyde; introduction of aryl groups at C-2 of the latter was accomplished by a Liebeskind-Srogl palladium-catalyzed desulfurative (de-methylsulfanylative) coupling with aryl boronic acids to obtain the target compounds 1 (14 examples, 60-95 % yield). 2-Arylpyrimidine-5-carbaldehydes, which are of relevance as substrates in Soai's asymmetric autocatalysis, are prepared through Liebeskind-Srogl coupling of aryl boronic acids with 2-methylthiopyrimidine-5-carbaldehyde; the latter is obtained in a hydrolytic condensation of two symmetric amidinium salts.
- Maltsev, Oleg V.,Rausch, Rodger,Quan, Zheng-Jun,Hintermann, Lukas
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supporting information
p. 7426 - 7432
(2016/02/20)
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- IMIDAZO[4,5-C]PYRIDINE AND PYRROLO[2,3-C]PYRIDINE DERIVATIVES AS SSAO INHIBITORS
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The compounds of formula (I) are inhibitors of semicarbazide- sensitive amine oxidase (SSAO) activity useful in the treatment of inflammation, an inflammatory disease, an immune or an autoimmune disorder, or inhibition of tumour growth.
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Page/Page column 43
(2014/09/29)
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- PYRAZOLOPYRIMIDINES AS CYCLIN-DEPENDENT KINASE INHIBITORS
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In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
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- An Alternative Preparation of the 2-Dimethylaminomethylene-1,3-bis(dimethylimminio)propane Salt from Phosphonoacetic Acids and Some Applications in Heterocyclic Synthesis
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An alternative preparation of a 2-iminovinamidinium salt from phosphonoacetic acids is described along with its application to the synthesis of 5-formylpyrimidines and masked 4-formylpyrazoles.
- Gupton, John T.,Gall, John E.,Riesinger, Steve W.,Smith, Stanton Q.,Bevirt, Kathy M.,et al.
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p. 1281 - 1285
(2007/10/02)
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