- Novel 4-phenoxypyridine derivatives bearing imidazole-4-carboxamide and 1,2,4-triazole-3-carboxamide moieties: Design, synthesis and biological evaluation as potent antitumor agents
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Two series of novel 4-phenoxypyridine derivatives containing imidazole-4-carboxamide and 4-methyl-5-oxo-4,5-dihydro-1,2,4-triazole-3-carboxamide moieties were synthesized and evaluated for their in vitro inhibitory activities against c-Met kinase and anti
- Chen, Ye,Ding, Shi,Du, Siyuan,Hou, Yunlei,Li, Chunyan,Li, Zhen,Liu, Fang,Liu, Ju,Shen, Jiwei,Wang, Huan,Wei, Hao,Wu, Shuang
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- Design, synthesis and anti-tumor evaluation of 1,2,4-triazol-3-one derivatives and pyridazinone derivatives as novel CXCR2 antagonists
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Chemokine receptor 2 (CXCR2) is the receptor of glutamic acid–leucine–arginine sequence-contained chemokines CXCs (ELR+ CXCs). In recent years, CXCR2-target treatment strategy has come a long way in cancer therapy. CXCR2 antagonists could block
- Chu, Bizhu,Jiang, Yuyang,Li, Qinyuan,Liu, Zijian,Luo, Jingyi,Shi, Zhichao,Xin, Qilei,Ye, Lizhen,Zhan, Feng,Zhang, Xun,Zhu, Qingyun
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- Bis-heterocycles. Part I: Tetrahydro-5,5′- bi(1,2,4-triazin-6-ones)
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Selected sets of tetrahydro-5,5′-bi(1,2,4-triazines) (1-3) appended with acetyl, benzoyl, and ester moieties at C-3 position and N-1 (p-substituted)phenyl ring have been prepared and characterized by spectral (IR, NMR, MS) data and X-ray diffraction for c
- Mohammad, Hanan H.,El-Abadelah, Mustafa M.,Sabri, Salim S.,Awwadi, Firas F.,Voelter, Wolfgang
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p. 965 - 974
(2018/11/23)
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- Triadimefon compound and uses thereof
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The present invention belongs to the field of agricultural bactericidal insecticides, and particularly relates to a triadimefon compound and uses thereof, wherein the structure of the compound is represented by a general formula I defined in the specifica
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Paragraph 0182; 0183; 0184
(2017/08/28)
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- Separation of PALMITIC acid from over used oil for production of heterogeneous organic derivatives of potential biological activities
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PALMITIC acid was extracted from Over-used cooking oil where oil was filtered off, then it was hydrolyzed with distilled water in high pressure reactor at 250°C and 2 MPa to produce glycerol and mixture of fatty acids. Fatty acids mixture was cooled at 7°C in order to precipitate all saturated fatty acids, which were then filtered off, Palmitic acid was extracted from this mixture by means of supercritical CO2 extractor at 35.0 MPa and 55°C, followed by its methylation and confirmation by GC mass. Then it was used as precursor for production of a different heterocyclic compounds which were then tested for their antimicrobial activities. Thus the long-chain methyl palmitate was interacted with hydrazine hydrate to produce the corresponding acid hydrazide (2), and then it was treated with phenyl isothiocyanate, furnished the corresponding thiosemicarbazide 4. The later was reacted with ethyl chloro(arylhydrazono) acetate 5a-b in dimethylformamide, in the presence of triethylamine, afforded thiadiazole derivatives 7a-b. A solution of thiosemicarbazide 4 in ethanol was interacted with the a-haloketones 9 in the presence of triethylamine, produced the parallel thiadiazine 12. The structure elucidation of all synthesized compounds is based on the elemental analysis and spectral data (IR, 1H NMR, 13C NMR and MS).
- Soliman, Hanaa M.,El-Shattory
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p. 591 - 600
(2019/01/30)
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- 4,5-dihydropyrazolo [3,4-c] pyridine-2-one spiro derivatives, its preparation method and application
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Disclosed are a spirocyclic derivative of 4,5-dihydropyrazolo[3,4-c]pyridine-2-one as represented by general formula (I), preparation method and use thereof, the definition of each substituent in the compound of general formula (I) being the same as the definition in the description.
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Paragraph 1038-1043
(2016/10/08)
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- Optimization of non-ATP competitive CDK/cyclin groove inhibitors through REPLACE-mediated fragment assembly
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A major challenge in drug discovery is to develop and improve methods for targeting protein-protein interactions. Further exemplification of the REPLACE (REplacement with Partial Ligand Alternatives through Computational Enrichment) strategy for generatin
- Liu, Shu,Premnath, Padmavathy Nandha,Bolger, Joshua K.,Perkins, Tracy L.,Kirkland, Lindsay O.,Kontopidis, George,McInnes, Campbell
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p. 1573 - 1582
(2013/04/10)
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- A new method for the synthesis of 1-aryl-1,2,4-triazole derivatives
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A new and convenient one-step recyclization method for the synthesis of ethyl 1-aryl-5-oxo-4,5-dihydro-1H-1,2,4-triazole-3-carboxylates is reported. Various ethyl chloro(2-arylhydrazinylidene)ethanoates react with thiazolidine-2,4-dione in the presence of potassium hydroxide to produce the 1-aryl-1,2,4-triazole derivatives in moderate to good yields. The procedure is economical, environmentally friendly and simple to perform. Georg Thieme Verlag Stuttgart - New York.
- Matiychuk, Vasyl S.,Potopnyk, Mykhaylo A.,Luboradzki, Roman,Obushak, Mykola D.
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experimental part
p. 1799 - 1803
(2011/07/08)
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- Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB1 receptor antagonists
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The synthesis, structure-activity relationship (SAR) studies and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles are described. The target compounds 6-18 represent a novel class of potent and selective CB1 r
- Lange, Jos H.M.,van der Neut, Martina A.W.,den Hartog, Arnold P.,Wals, Henri C.,Hoogendoorn, Jan,van Stuivenberg, Herman H.,van Vliet, Bernard J.,Kruse, Chris G.
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experimental part
p. 1752 - 1757
(2010/07/08)
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- Methyl 3-cyclopropyl-3-oxopropanoate in the synthesis of heterocycles having a cyclopropyl substituent
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Reactions of methyl 3-cyclopropyl-3-oxopropanoate with chloroacetone and ammonia, benzaldehyde and ammonia, and benzoquinone gave, respectively, methyl 2-cyclopropyl-5-methyl-1H-pyrrole-3-carboxylate, dimethyl 2,6-dicyclopropyl-4- phenyl-1,4-dihydropyridi
- Pokhodylo,Matiichuk,Obushak
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scheme or table
p. 894 - 897
(2010/11/03)
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- Synthesis, cannabinoid receptor affinity, and molecular modeling studies of substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides
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The new 1-phenyl-5-(1H-pyrrol-1-yl)pyrazole-3-carboxamides were compared with the reference compounds AM251 and SR144528 for cannabinoid hCB1 and hCB2 receptor affinity. Compounds bearing 2,4-dichlorophenyl or 2,4-difluorophenyl groups at position 1 and 2,5-dimethylpyrrole moiety at position 5 of the pyrazole nucleus were generally more selective for hCB 1. On the other hand, the N-cyclohexyl group at the 3-carboxamide was the determinant for the hCB2 selectivity, in particular when a 3,4-dichlorophenyl group was also present at position 1. Compound 26 was the most selective ligand for the hCB1 receptor (Ki (CB 2)/Ki (CB1) = 140.7). Derivative 30, the most potent hCB1 ligand (Ki = 5.6 nM), was equipotent to AM251 and behaved as an inverse agonist in the cAMP assay (EC50 ~1 nM). The carbonyl oxygen of both 26 and 30 formed a H-bond with K3.28(192), while the substituents at the nitrogen fitted in a pocket formed by lipophilic residues. This H-bonding interaction was proposed to account for the high affinity for receptors' inactive state and the inverse agonist activity.
- Silvestri, Romano,Cascio, Maria Grazia,La Regina, Giuseppe,Piscitelli, Francesco,Lavecchia, Antonio,Brizzi, Antonella,Pasquini, Serena,Botta, Maurizio,Novellino, Ettore,Di Marzo, Vincenzo,Corelli, Federico
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p. 1560 - 1576
(2008/12/20)
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- 1,3,5-trisubstituted 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
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The present invention relates to 1,3,5-trisubstituted 4,5-dihydro-1H-pyrazole derivatives as CB1 antagonists, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said pyrazole derivatives. Th
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Page/Page column 6
(2010/02/13)
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- Insecticidal pyrazolines
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Pyrazolines and their intermediates, including all geometric and stereoisomers of the pyrazolines and intermediates, agricultural compositions containing the pyrazolines, and methods for use as insecticides.
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- Kinetics and mechanism of dehydrochlorination of N-aryl-C-ethoxycarbonylformohydrazidoyl chlorides
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The kinetics of triethylamine (TEA) catalyzed dehydrochlorination of a series of N-aryl-C-ethoxycarbonylformohydrazidoyl chlorides 1a-m have been studied under pseudo-first-order conditions in 4:1 (v/v) dioxane-water solution at 30 deg C.For all compounds
- Shawali, Ahmad S.,Albar, Hassan A.
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p. 871 - 875
(2007/10/02)
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- Synthesis and evaluation of furan, thiophene, and azole bis[(carbamoyloxy)methyl] derivatives as potential antineoplastic agents
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A series of bis(hydroxymethyl)-substituted heterocycles were synthesized and converted to the corresponding bis(methylcarbamate) derivatives. The heterocyclic systems studied were based on 2-phenyl-3-methylfuran, 1-phenylpyrazole, 1-phenyl-5-methylpyrazole, 1-phenyl-5-methylthiopene, 1-phenyl-1,2,3-triazole, 3-phenylisoxazole, 3-phenylisothiazole, 2-phenylthiazole, and 2-phenyloxazole. None of the bis(carbamates) prepared was active against murine P388 lymphocytic leukemia. Pyrrole bis(carbamate), which exhibited antileukemic activity, also showed reactivity toward 4-(p-nitrobenzyl)pyridine while the inactive bis(carbamates) were unreactive in the 4-(p-nitrobenzyl)pyridine assay.
- Anderson,Jones
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p. 1559 - 1565
(2007/10/02)
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