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Xiao-Xin Tan, Kao-Qi Lian, Xiang Li, Nan Li, Wei Wang, Wei-Jun Kang, Hong-Mei Shi
Hydrogen sulfide (H2S) plays major functional and structural roles in diverse physiological functions and the pathogenesis of a variety of disorders in biological matrices. The significance of H2S has prompted the development of sensitive and selective methods to determine its concentration in biological samples. The fluorescent reagent monobromobimane (MBB) has been widely used to measure various thiol-containing species through alkylation. MBB may prevent the oxidation of sulfide and the reaction of sulfide with several different species (such as superoxide radicals, hydrogen peroxide and peroxynitrite)...
April 13, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Jinlai Yang, Xu Xu, Jian Rui, Zhonglong Wang, Yan Zhang, Shifa Wang, Liangru Wu
Pyrazole derivatives (4-6) were directly synthesized from β-pinene derivative nopinone, and they were characterized by Fourier transform infrared (FTIR) spectoscope, nuclear magnetic resonance (NMR), and mass spectrometry. Their optical properties were investigated by ultraviolet-visible spectroscopy and fluorescence spectroscopy. The three compounds emitted strong blue fluorescence in ethanol. Using a fluorescence quenching method, compound 4 could be used to detect the content (100.57%) of copper sulfate pentahydrate (≥99%) with a RSD of 1...
April 20, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Shadia A Galal, Ahmed S Abdelsamie, Samia A Shouman, Yasmin M Attia, Hamed I Ali, Ashraf Tabll, Reem El-Shenawy, Yasmine S El Abd, Mamdouh M Ali, Abeer E Mahmoud, Abeer H Abdel-Halim, Amal A Fyiad, Adel S Girgis, Hoda I El-Diwani
Activated checkpoint kinase 2 (Chk2) is a tumor suppressor as one of the main enzymes that affect the cell cycle. 2-Biarylbenzimidazoles are potent selective class of Chk2 inhibitors; the structure-based design was applied to synthesize a new series of this class with replacing the lateral aryl group by substituted pyrazoles. Ten pyrazole-benzimidazole conjugates from the best fifty candidates according to docking programs have been subjected to chemical synthesis in this study. The activities of the conjugates 5-14 as checkpoint kinase inhibitors and as antitumor alone and in combination with genotoxic drugs were evaluated...
April 14, 2017: European Journal of Medicinal Chemistry
Nagat Ghareb, Hosam A Elshihawy, Mohamed M Abdel-Daim, Mohamed A Helal
COX-2 is an inducible enzyme mediating inflammatory responses. Selective targeting of COX-2 is useful for developing anti-inflammatory agents devoid of ulcerogenic activity. Herein, we report the design and synthesis of a series of pyrazoles and pyrazolo[1,2-a]pyridazines with selective COX-2 inhibitory activity and in vivo anti-inflammatory effect. Both series were accessed through acid-catalyzed ultrasound-assisted reactions. The most active compounds in this study are two novel molecules, 11 and 16, showing promising selectivity and decent IC50 of 16...
April 8, 2017: Bioorganic & Medicinal Chemistry Letters
Younes Hanifehpour, Ali Morsali, Babak Mirtamizdoust, Sang Woo Joo, Behzad Soltani
Nano-structures of a new supramolecular coordination compound of divalent nickel with the pyrazol (pzH) containing the terminal azide anions, [Ni(pzH)2(N3)2] (1), with discrete molecular architecture (DMA) in solid state was synthesized via sonochemical method. The new nanostructure was characterized by scanning electron microscopy, X-ray powder diffraction, IR, and elemental analysis. Compound 1 was structurally characterized by single crystal X-ray diffraction and the single-crystal X-ray data shows that the coordination number of Ni (II) ions is six, (NiN6), with four N-donor atoms from neutral "pzH" ligands and two N-donors from two terminal azide anions...
July 2017: Ultrasonics Sonochemistry
Yu Cui, Zi-Man Chen, Xuan-Feng Jiang, Jin Tong, Shu-Yan Yu
Three hexametal-organic cages [(N^N)6Pd6L2](6+) with syn, syn, syn conformation were synthesized via the coordination of tris(4-(1H-pyrazol-3-yl)phenyl)amine ligands and [(N^N)2Pd2(NO3)2](NO3)2 dimetallic corners (N^N = 2,2'-bipyridine for 1; 4,4'-dimethylbipyridine for 2; 1,10-phenanthroline for 3). These hexametal-organic cages exhibit anion sensing toward HSO3(-) in aqueous solution via fluorescent titration and NMR spectroscopy studies.
April 20, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
Sourav Pradhan, Pinaki Bhusan De, Tharmalingam Punniyamurthy
A copper-mediated picolinamide directed regioselective cross-coupling of naphthylamines with azoles is developed via C-H functionalization and C-N bond formation. The reaction of indoles leads to the formation of chiral C-N cross-coupled products with functional group tolerance. These reaction conditions can also be extended to the cross-coupling of pyrazole and pyrrole scaffolds.
April 19, 2017: Journal of Organic Chemistry
Heba A Abd El Razik, Mona H Badr, Attia H Atta, Samar M Mouneir, Marwa M Abu-Serie
Two series of benzodioxole-pyrazole hybrids were synthesized and the IC50 values for in vitro inhibition of the enzymes cyclooxygenase 1/2 (COX-1, COX-2) and 5-lipoxygenase (5-LOX) were investigated. All compounds were tested for their in vivo anti-inflammatory and analgesic potentials using diclofenac sodium as a reference standard. Compounds 4, 11, 17, 20, 21, 26, and 27, which showed good analgesic and/or anti-inflammatory activities, were also evaluated for their ability to inhibit tumor necrosis factor (TNF)-α production, myeloperoxidase and proteinase, beside their antioxidant activity...
April 18, 2017: Archiv der Pharmazie
Marco Pierini, Simone Carradori, Sergio Menta, Daniela Secci, Roberto Cirilli
The enantiomers of five chiral compounds incorporating the 3-(phenyl-4-oxy)-5-phenyl-4,5-dihydro-(1H)-pyrazole scaffold and differing only in the linear alkyl chain (varying in length from 1 to 5 carbon atoms) linked to the oxygen atom were directly separated on the amylose (3,5-dimethylphenylcarbamate) based Chiralpak AD-3 chiral stationary phase. The effects of the mobile phase composition, the structure of the analytes and temperature on the retention and enantioselectivity were investigated. It was found that the enantiomeric separations were in all cases enthalpy-driven and disfavored by entropic term...
April 4, 2017: Journal of Chromatography. A
Sujay Basu, Dinesh A Barawkar, Vidya Ramdas, Meena Patel, Yogesh Waman, Anil Panmand, Santosh Kumar, Sachin Thorat, Minakshi Naykodi, Arnab Goswami, B Srinivasa Reddy, Vandna Prasad, Sandhya Chaturvedi, Azfar Quraishi, Suraj Menon, Shalini Paliwal, Abhay Kulkarni, Vikas Karande, Indraneel Ghosh, Syed Mustafa, Siddhartha De, Vaibhav Jain, Ena Ray Banerjee, Sreekanth R Rouduri, Venkata P Palle, Anita Chugh, Kasim A Mookhtiar
Adenosine induces bronchial hyperresponsiveness and inflammation in asthmatics through activation of A2B adenosine receptor (A2BAdoR). Selective antagonists have been shown to attenuate airway reactivity and improve inflammatory conditions in pre-clinical studies. Hence, the identification of novel, potent and selective A2BAdoR antagonist may be beneficial for the potential treatment of asthma and Chronic Obstructive Pulmonary Disease (COPD). Towards this effort, we explored several prop-2-ynylated C8-aryl or heteroaryl substitutions on xanthine chemotype and found that 1-prop-2-ynyl-1H-pyrazol-4-yl moiety was better tolerated at the C8 position...
April 12, 2017: European Journal of Medicinal Chemistry
Iziara F Florentino, Daiany P B Silva, Dayane M Silva, Carina Sofia Cardoso, André L E Moreira, Clayton L Borges, Célia M de A Soares, Pablinny M Galdino, Luciano M Lião, Paulo C Ghedini, Ricardo Menegatti, Elson A Costa
The pyrazole compound LQFM-021 exhibits vasorelaxant, antinociceptive and anti-inflammatory activities. Furthermore, it has low toxicity, indicating that this compound may be considered to be a good prototype for the development of new analgesic/anti-inflammatory drugs. Therefore, the aim of this study was to investigate the potential anti-inflammatory activity of LQFM-021 using a model of carrageenan-induced inflammation as well as the mechanism of action and role of nitric oxide in this effect. Acute treatments with LQFM-021 (30 and 60 mg/kg p...
April 12, 2017: Nitric Oxide: Biology and Chemistry
Fei Zhao, Le-Duo Zhang, Yu Hao, Na Chen, Rui Bai, Yu-Ji Wang, Chun-Chun Zhang, Gong-Sheng Li, Li-Jun Hao, Chen Shi, Jing Zhang, Yu Mao, Yi Fan, Guang-Xin Xia, Jian-Xin Yu, Yan-Jun Liu
c-Met/HGF signaling pathway plays an important role in cancer progression, and it was considered to be related to poor prognosis and drug resistance. Based on metabolite profiling of (S)-7-fluoro-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-1H-imidazo[4,5-b]pyrazin-1-yl)ethyl)quinoline (1), a series of 2-substituted or 3-substituted-6-(1-(1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)ethyl)quinoline derivatives was rationally designed and evaluated. Most of the 3-substituted derivatives not only exhibited potent activities in both enzymatic and cellular assays, but also were stable in liver microsomes among different species (human, rat and monkey)...
April 4, 2017: European Journal of Medicinal Chemistry
Wei Sun, Xiuli Huang, Hao Li, Gregory Tawa, Ethan Fisher, Takeshi Q Tanaka, Paul Shinn, Wenwei Huang, Kim C Williamson, Wei Zheng
BACKGROUND: Blocking malaria transmission is an important step in eradicating malaria. In the field, transmission requires the production of sexual stage Plasmodium parasites, called gametocytes, which are not effectively killed by the commonly used anti-malarials allowing individuals to remain infectious after clearance of asexual parasites. METHODS: To identify new gametocytocidal compounds, a library of 45,056 compounds with diverse structures was screened using a high throughput gametocyte viability assay...
April 13, 2017: Malaria Journal
Raghavendra Achary, Gangadhar Rao Mathi, Dong Ho Lee, Chang Soo Yun, Chong Ock Lee, Hyoung Rae Kim, Chi Hoon Park, Pilho Kim, Jong Yeon Hwang
In this study, a series of novel 2,4-diaminopyrimidines bearing fused tricyclic ring moiety was described for ALK inhibitor. The pyrazole, imidazole, 1,2,4-triazole, piperazine and phenanthridine moieties were employed at the 2-position of pyrimidine. Among the compounds synthesized, 28, 29, 36, and 42 showed promising anti-ALK activities in enzymatic- and cell-based assays. In vivo H3122 xenograft model study showed that compound 29 effectively suppressed ALK-driven tumor growth, similar to the extent of ceritinib, suggesting that it could be used for a novel ALK inhibitor development...
March 29, 2017: Bioorganic & Medicinal Chemistry Letters
Pan Li, Jingjing Zhao, Xinjian Li, Fuwei Li
A novel and efficient synthesis of functionalized oxazoles from 2-amidodihydrofurans has been achieved by alkali-induced intramolecular C-O bond cleavage and formation using air as a green oxidant. Moreover, these functionalized oxazoles could be readily transformed into the corresponding oxazole substituted pyrazoles and 2H-azirines.
April 6, 2017: Journal of Organic Chemistry
Tingting Pan, Chunguang Xia, Huijuan Jiang, Zhongtang Zhang, Xueyan Zhu, Yulei Yang
An efficient synthesis of ODM-201's diastereomers has been developed from (R)-methyl 3-hydroxybutanoate or (S)-methyl 3-hydroxybutanoate, respectively, with high overall yield and excellent diastereomeric purity. The key step in this synthesis is the preparation of the key intermediate (R)-5-(1-((tert-butyldimethylsilyl)oxy)ethyl)-1H-pyrazole-3-carboxylic acid or (S)-5-(1-((tert-butyldimethylsilyl)oxy)ethyl)-1H-pyrazole-3-carboxylic acid through intramolecular 1,3-dipolar cycloaddition of the vinyl diazo carbonyl compounds...
April 5, 2017: Chemical & Pharmaceutical Bulletin
Marc Moselage, Jie Li, Frederik Kramm, Lutz Ackermann
Ruthenium(II)biscarboxylate catalysis enabled selective C-C functionalizations by means of decarbamoylative C-C arylations. The versatility of the ruthenium(II) catalysis was reflected by widely applicable C-C arylations and C-C alkylations of aryl amides, as well as acids with modifiable pyrazoles, through facile organometallic C-C activation.
May 2, 2017: Angewandte Chemie
Jiachun Liu, Mei Chen, Yanli Wang, Xiaoyin Zhao, Sijia Wang, Yanling Wu, Wen Zhang
A novel series of 2-(1H-pyrazol-4-yl)-1H-imidazo[4,5-f][1,10]phenanthrolines were designed, synthesized and evaluated for their antitumor activity against lung adenocarcinoma by CCK-8 assay, electrophoretic mobility shift assay (EMSA), UV-melting study, wound healing assay and docking study. These compounds showed good inhibitory activities against lung adenocarcinoma. Especially compound 12c exhibited potential antiproliferative activity against A549 cell line with the half maximal inhibitory concentration (IC50) value of 1...
March 18, 2017: European Journal of Medicinal Chemistry
Elda Meta, Chiara Brullo, Adama Sidibe, Beat A Imhof, Olga Bruno
Taking into account the structure activity relationship information given by our previous studies, we designed and synthesized a small library of pyrazolylureas and imidazopyrazolecarboxamides fluorinated on urea moiety and differently decorated on pyrazole nucleus. All compounds were preliminary screened by Western blotting technique to evaluate their activity on MAPK and PI3K pathways by monitoring ERK1/2, p38MAPK and Akt phosphorylation, and also screened with a wound healing assay to assess their capacity in inhibiting endothelial cell migration, using human umbilical vein endothelial cells stimulated with VEGF...
March 27, 2017: European Journal of Medicinal Chemistry
Alexander V Polezhaev, Chun-Hsing Chen, Yaroslav Losovyj, Kenneth G Caulton
A pyridyl pincer ligand is introduced to incorporate steric bulk, via a PtBu2 arm, and proton responsivity, via a pyrazole pincer ligand arm, together with reactivity at benzylic hydrogen and redox activity within a 1,4 diazabutadiene moiety. Binding it to CoCl2 yields square pyramidal (PNNH)CoCl2, that is deprotonated with Li[N(SiMe3)2] forming [Li(THF)2PNN]CoCl2. Reduction of this LiCl adduct with KC8 under CO atmosphere leads to formation of Co(I) mono- and dicarbonyls, which can be protonated but also be further deprotonated, at the benzylic CH, leading to a dearomatized pyridyl functionality...
March 28, 2017: Chemistry: a European Journal
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