- Synthesis, structure and acetylcholinesterase inhibition activity of new diarylpyrazoles
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A variety of diarylpyrazole derivatives III-VI were synthesized and structurally characterized using FTIR, 1H and 13C NMR spectroscopy, and in case of compound VIb by X-ray single crystal analysis. The in vitro biological studies rev
- Arshad, Iqra,Dege, Necmi,Hameed, Shahid,Kharl, Aamir Ali,Nadeem, Humaira,Naseer, Muhammad Moazzam,Paracha, Rehan Zafar,Zia, Mehwash
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- A Convenient One-Pot Synthesis of Chalcones and Their Derivatives and Their Antimicrobial Activity
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Abstract: A series of chalcones were synthesized by base-catalyzed Clasien-Schmidtcondensation of substituted benzaldehydes and substituted acetophenones at roomtemperature. The addition of hydrazine hydrate and hydroxylamine hydrochlorideacross the double bond of the obtained chalcones gave pyrazole and isoxazolederivatives, respectively. All the synthesized compounds were characterized by1H and 13C NMR andFT-IR spectroscopy and screened for their in vitro antimicrobial activityagainst two bacterial strains, Pseudomonasaeruginosa and Pseudomonasoryzihabitans using Ciprofloxacin as standard drug.1-(2-Methoxyphenyl)-3-phenylprop-2-en-1-one and1-(4-chlorophenyl)-3-phenylprop-2-en-1-one showed significant activity againstboth bacterial strains and hence proved to be potent antimicrobialagents.
- Salotra,Utreja,Sharma
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p. 2207 - 2211
(2021/02/09)
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- Aurones and Analogues: Promising Heterocyclic Scaffolds for Development of Antioxidant and Antimicrobial Agents
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Synthesis of some new multi-functional analogues of 2′-hydroxy chalcone containing isoxazole and pyrazole functions were synthesized, and their pharmacological activity was tested. Chalcone derivatives were synthesized by the reaction of 2′-hydroxy acetophenone with various substituted benzaldehydes in a basic medium. Aurones were isolated upon treatment with mercuric acetate. Synthesized chalcones and aurones were converted into the corresponding isoxazole and pyrazole derivatives upon their reaction with hydroxylamine hydrochloride or hydrazine hydrate, respectively. Structures of the compounds were confirmed by spectroscopic methods. All synthesized compounds were tested for antioxidant and antibacterial potential. Some of those demonstrated excellent antioxidant activity, and one product was identified as a promising antimicrobial candidate.
- Irshad,Ali,Iram,Ahamad,Saleem,Saadia,Batool,Kanwal,Tabassum
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p. 1519 - 1527
(2019/08/21)
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- Diversity-oriented synthesis of pyrazoles derivatives from flavones and isoflavones leads to the discovery of promising reversal agents of fluconazole resistance in Candida albicans
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Diversity-oriented synthesis of derivatives of natural products is an important approach for the discovery of novel drugs. In this paper, a series of novel 3,4-diaryl-1H-pyrazoles and 3,5-diaryl-1H-pyrazoles derivatives were synthesized through the one-po
- Cui, Chang-Yi,Liu, Jun,Zheng, Hong-Bo,Jin, Xue-Yang,Zhao, Xiao-Yu,Chang, Wen-Qiang,Sun, Bin,Lou, Hong-Xiang
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supporting information
p. 1545 - 1549
(2018/04/02)
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- ESIPT-active organic compounds with white luminescence based on crystallization-induced keto emission (CIKE)
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Structurally simple pyrazole derivatives that exhibit excited-state intramolecular proton transfer (ESIPT) were synthesized. While these compounds displayed deep violet fluorescence in solution, in the crystalline state they showed white emission from the
- Liu, Huapeng,Cheng, Xiao,Zhang, Houyu,Wang, Yue,Zhang, Hongyu,Yamaguchi, Shigehiro
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supporting information
p. 7832 - 7835
(2017/07/15)
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- Decoupling Activation of Heme Biosynthesis from Anaerobic Toxicity in a Molecule Active in Staphylococcus aureus
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Small molecules active in the pathogenic bacterium Staphylococcus aureus are valuable tools for the study of its basic biology and pathogenesis, and many molecules may provide leads for novel therapeutics. We have previously reported a small molecule, 1, which activates endogenous heme biosynthesis in S. aureus, leading to an accumulation of intracellular heme. In addition to this novel activity, 1 also exhibits toxicity towards S. aureus growing under fermentative conditions. To determine if these activities are linked and establish what features of the molecule are required for activity, we synthesized a library of analogs around the structure of 1 and screened them for activation of heme biosynthesis and anaerobic toxicity to investigate structure-activity relationships. The results of this analysis suggest that these activities are not linked. Furthermore, we have identified the structural features that promote each activity and have established two classes of molecules: activators of heme biosynthesis and inhibitors of anaerobic growth. These molecules will serve as useful probes for their respective activities without concern for the off target effects of the parent compound.
- Dutter, Brendan F.,Mike, Laura A.,Reid, Paul R.,Chong, Katherine M.,Ramos-Hunter, Susan J.,Skaar, Eric P.,Sulikowski, Gary A.
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p. 1354 - 1361
(2016/06/09)
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- A facile and expeditious approach to substituted 1H-pyrazoles catalyzed by iodine
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A facile and expeditious method for the synthesis of 1H-pyrazoles by the reaction of α,β-unsaturated aldehydes/ketones and sulfonyl hydrazide catalyzed by as low as 2 mol % I2 has been demonstrated. This synthetic system features simple operation and mild reaction conditions, and displays a broad functional group tolerance furnishing good to excellent yields.
- Zhang, Hailei,Wei, Qian,Zhu, Guodong,Qu, Jingping,Wang, Baomin
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supporting information
p. 2633 - 2637
(2016/06/01)
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- Copper (II) chloride: A regioselective catalyst for oxidative aromatization of pyrazoline, isoxazoline and 3-methyl flavanones
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A new protocol has been reported in which a series of pyrazoline, isoxazoline and 3-methyl flavanone has been conveniently aromatized by using CuCl2.2H2O in DMSO within a short reaction time in excellent yields. The attraction of this new protocol is regioselective aromatization of substrate 3i-j and 5a-e which has been carried out to afford the aromatized product with O-allyl group intact in excellent yield.
- Lokhande, Pradeep D.,Dalvi, Bhakti A.,Humne, Vivek T,Nawghare, Beena R.,Kareem, Abdul
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p. 1091 - 1097
(2014/09/30)
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- GLUCOKINASE ACTIVATORS
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Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.
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Page/Page column 49
(2010/11/28)
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- Synthesis of pyrazole and isoxazole in triethanolamine medium
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Reactions of 2′-hydroxy chalcone dibromides 2a-1 with phenyl hydrazine and hydrazine hydrate afford pyrazoles 1a-1 and with hydroxylamine hydrochloride give isoxazoles 5a-f in triethanolamine medium. Similarly reaction of β-diketone 3b-e with phenyl hydra
- Agrawal, Nitin N.,Soni
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p. 532 - 534
(2008/09/18)
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- Benzodiazepine binding activity of some tricyclic heteroatomic systems to define the hydrogen bonding strength of the proton donors of the receptor site
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Comparison of the benzodiazepine receptor affinities of some known and newly synthesized tricyclic derivatives of similar size and shape, and bearing the same pharmacophoric descriptors allowed us to suggest the different hydrogen bonding power of the proton donors of the benzodiazepine receptor recognition site. In particular, we propose, according to a previous model, that the lack of the a1 acceptor, which corresponds to a weak hydrogen donor of the receptor site, is not crucial for receptor-ligand interaction but, like the hydrogen donor d, only affects the potency. On the contrary, the presence of a proton acceptor atom in the a2 area is essential for the anchoring of our tricyclic derivatives to the benzodiazepine receptor recognition site.
- Colotta,Catarzi,Varano,Melani,Filacchioni,Cecchi,Galli,Costagli
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p. 223 - 229
(2007/10/03)
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- Oxidation of Pyrazolines with Manganese Dioxide
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Pyrazolines have been oxidised with manganese dioxide in chloroform at room temperature to give pyrazoles in good yields.
- Agrawal, Kumkum
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p. 408 - 410
(2007/10/02)
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- Reaction of 2-acyl-3-aminobenzofurans with hydrazines
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While 2-acetyl and 2-benzoyl-3-aminobenzofurans did not react with hydrazine, monomethyl- and N,N-dimethylhydrazine to give the related hydrazones, their 3-N-(p-toluenesulfonyl) derivatives afforded them smoothly in good yields. Depending upon reaction conditions, products arising from hydrazone cyclization to benzofuropyrazoles and/or from furan ring cleavage at the C2-O bond to give 5-(2-hydroxyphenyl)pyrazoles were also formed. The formation of these products depends upon hydrazones configuration and is discussed. Only (E)-isomers appear to undergo furan ring opening. In acidic media at room temperature either the hydrazones or the monomethylhydrazones gave the same related α-azines. Microanalyses, ir, uv, 1H-nmr and ms spectra are in agreement with the proposed structures.
- Gatta,Settimj
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p. 937 - 943
(2007/10/02)
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- Synthesis of Some Imidazole- and Pyrazole- Derived Chelating Agents
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Procedures involving condensation of o-phenylenediamines with carboxylic acids, and reaction of bifunctional alkyl halides with bifunctional nucleophiles are described.Syntheses are reported of 2,6-bis(2-benzimidazyl)-pyridine, 1,3-bis(2-benzimidazyl)-2-thiapropane, 1,7-bis(2-benzimidazyl)-2,6-dithiaheptane, 2-hydroxymethyl-5,6-dimethylbenzimidazole, 2-chloromethyl-5,6-dimethylbenzimidazole hydrochloride, 1,7-bis(5,6-dimethyl-2-benzimidazyl)-2,6-dithiaheptane, 3,6-bis(1-pyrazolyl)pyridazine, 2-(2-hydroxy-3-methylphenyl)benzimidazole, 2-(2-hydroxyphenyl)benzimidazole, 5-(2-hydroxyphenyl)-3-methyl-1-phenylpyrazole, 3(5)-(2-hydroxyphenyl)-5(3)-methylpyrazole, 3(5)-(2-hydroxyphenyl)-5(3)-phenylpyrazole, and 1,3-bis((5-methylpyridyl)imino)isoindoline.
- Addison, Anthony W.,Burke, Philip J.
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p. 803 - 805
(2007/10/02)
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