- A New Series of 1,3,4-Oxadiazole Linked Quinolinyl-Pyrazole/Isoxazole Derivatives: Synthesis and Biological Activity Evaluation
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Abstract: A series of 1,3,4-oxadiazole bridged pyrazole/isoxazole bearing quinoline derivatives has been designed and synthesized by a clean and convenient method. Structures of the newly synthesized compounds have been confirmed by FTIR, 1H and 13C NMR, and HRMS spectral data. The titled compounds have been evaluated for their molecular docking guided antimicrobial and anti-inflammatory activity. One of 1,3,4-oxadiazole bridged quinolinyl-pyrazole derivatives has interacted efficiently with E. Coli protein (PDB file: 1KZN), and has been characterized by good antimicrobial activity against the majority of the tested pathogens. Another product has exhibited excellent anti-inflammatory activity.
- Basavanna, V.,Bhadraiah, U. K.,Chandra,Chandramouli, M.,Doddamani, Shridevi,Kempaiah, C.,Lingegowda, N. S.,Ningaiah, S.
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p. 2257 - 2266
(2021/12/23)
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- Discovery of pyrazole derivatives as potent inhibitor of NF-?B for possible benefit in abdominal aortic aneurysms
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Numerous 3-(4-substitutedyphenyl)-5-methyl-1-phenyl-1H-pyrazole-4-carboxylate derivatives have been synthesized using H2SO4.SiO2 as a catalyst. These derivatives were subsequently screened for NF-?B transcription inhibitor
- Guo, Yun,Bao, Dongming,Zhang, Chaogang
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p. 4917 - 4925
(2021/06/07)
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- Novel 5-functionalized-pyrazoles: Synthesis, characterization and pharmacological screening
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In the present study a series of O-substituted pyrazoles 7(a-f) and N-substituted pyrazoles 9(a-f) were synthesized via phase-transfer catalyzed reaction of ethyl 5-(bromomethyl)-1,3-diphenyl-1H-pyrazole-4-carboxylate 5 with various oxygen and nitrogen containing compounds in presence of tetrabutylammonium bromide (TBAB) in THF. The compound 5 was obtained by the efficient bromination with N-bromosuccinimide (NBS) in presence of a catalytic amount of azoiso-bis-butyro nitrile (AIBN) in refluxing CCl4. The synthesized compounds were evaluated for their in vitro antimicrobial and antidiabetic activity and were compared with standard drugs. Among the synthesized compounds, compound 9b emerged as an excellent antimicrobial and antidiabetic agent. Newly synthesized compounds were characterized by analytical and spectral (IR, 1H NMR, 13C NMR and LC-MS) methods.
- Doddaramappa, Shridevi D.,Lokanatha Rai,Srikantamurthy, Ningaiah,Chandra,Chethan, Javarasetty
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p. 3671 - 3675
(2015/08/11)
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- One-pot tandem synthesis of tetrasubstituted pyrazoles via 1,3-dipolar cycloaddition between aryl hydrazones and ethyl but-2-ynoate
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1,3,4,5-Tetrasubstituted pyrazoles are rapidly and regioselectively synthesized in a one-pot, three-step sequence consisting of condensation, nitrilimine generation, and cycloaddition using mercuric acetate. Newly synthesized compounds were characterized by spectral studies. Regiochemistry of compounds 6a and 8a was determined as 1,4- and 1,5-regioisomers respectively by X-ray crystallography. Copyright
- Ningaiah, Srikantamurthy,Doddaramappa, Shridevi D.,Chandra,Madegowda, Mahendra,Keshavamurthy, Shubakara,Bhadraiah, Umesha K.
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p. 2222 - 2231
(2014/07/07)
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- PYRAZOLE SYNTHESIS BY COUPLING OF CARBOXYLIC ACID DERIVATIVES AND ENAMINES
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The invention describes a novel process for synthesizing pyrazoles by means of oxidative conversion of enamines with suitable N-containing carboxylic acid derivatives.
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Paragraph 0167-0169
(2013/03/26)
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- Sc(OTf)3-catalyzed, solvent-free domino synthesis of functionalized pyrazoles under controlled microwave irradiation
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An efficient, rapid, and green synthesis of functionalized pyrazoles has been accomplished under solvent-free conditions by the reaction of phenyl hydrazine, aldehydes and ethyl acetoacetate. This approach exploits the synthetic potential of microwave irr
- Kumari, Kumkum,Raghuvanshi, Dushyant Singh,Jouikov, Viatcheslav,Singh, Krishna Nand
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experimental part
p. 1130 - 1133
(2012/03/26)
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- Regioselective multicomponent synthesis of fully substituted pyrazoles and bispyrazoles catalyzed by zinc triflate
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A variety of fully substituted pyrazoles were easily prepared through a three-component condensation of aldehydes, arylhydrazines, and ethyl acetoacetate in the presence of catalytic amounts of zinc triflate [Zn(OTf) under solvent-free conditions. Selecti
- Safaei, Shirin,Mohammadpoor-Baltork, Iraj,Khosropour, Ahmad Reza,Moghadam, Majid,Tangestaninejad, Shahram,Mirkhani, Valiollah
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experimental part
p. 2214 - 2222
(2011/10/18)
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- Silica chloride catalyzed one-pot synthesis of fully substituted pyrazoles
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Silica chloride catalysted one pot cyclocondensation of aldehydes, ethyl acetoacetate and phenyl hydrazine leading to substituted pyrazoles has been reported.
- Jawale, Dhanaji V.,Pratap, Umesh R.,Mali, Jyotirling R.,Mane, Ramrao A.
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scheme or table
p. 1187 - 1190
(2012/01/05)
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- Efficient synthesis of pyrazoles: Oxidative C-C/N-N bond-formation cascade
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Golden section: A novel synthetic strategy for the synthesis of tetrasubstituted pyrazoles is provided. In an efficient C-C/N-N bond-formation cascade, enamines and nitriles are oxidatively coupled to deliver pyrazoles in good yields (see scheme). The rea
- Neumann, Julia J.,Suri, Mamta,Glorius, Frank
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supporting information; experimental part
p. 7790 - 7794
(2011/01/09)
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- An effective and general method for the highly regioselective synthesis of 1-phenylpyrazoles from β-enaminoketoesters, tandem Blaise-acylation adducts
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An effective and general route for the regioselective synthesis of 1-phenylpyrazoles has been developed from β-enaminoketoesters prepared by tandem Blaise-acylation. This method is applicable to a very broad range of substrates, generating a diverse set o
- Ko, Young Ok,Chun, Yu Sung,Park, Cho-Long,Kim, Youngmee,Shin, Hyunik,Ahn, Sungho,Hong, Jongki,Lee, Sang-Gi
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supporting information; experimental part
p. 1132 - 1136
(2009/05/30)
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- The first chemoselective tandem acylation of the Blaise reaction intermediate: A novel method for the synthesis of α-acyl-β-enamino esters, key intermediate for pyrazoles
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The Blaise reaction intermediate, a zinc bromide complex of β-enamino ester, could be activated in situ by addition of a stoichiometric or catalytic amount of n-BuLi to allow chemoselective tandem C2-acylation providing α-acyl-β-enamino esters, which are
- Sung Chun, Yu,Kon Lee, Ki,Ok Ko, Young,Shin, Hyunik,Lee, Sang-Gi
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supporting information; experimental part
p. 5098 - 5100
(2009/03/11)
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- Ytterbium(III) perfluorooctanoate catalyzed one-pot, three-component synthesis of fully substituted pyrazoles under solvent-free conditions
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A convenient one-pot synthesis of fully substituted pyrazoles via three-component condensations of phenylhydrazine, aldehydes, and 1,3-dicarbonyl compounds using ytterbium perfluorooctanoate [Yb(PFO)3] as catalyst under solvent-free conditions is described. The reusable catalyst can be easily prepared and was efficient for the reaction. A possible mechanism is suggested. Georg Thieme Verlag Stuttgart.
- Shen, Li,Cao, Song,Liu, Nianjin,Wu, Jingjing,Zhu, Longjie,Qian, Xuhong
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experimental part
p. 1341 - 1344
(2009/04/06)
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- NEUROKININ-3 RECEPTOR MODULATORS: DIARYL PYRAZOLE DERIVATIVES
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The invention relates to compounds of general Formula (I) wherein the variables are as defined herein. Pharmaceutical compositions comprising compounds of general Formula (I), and methods for treating patients suffering from a disorder responsive to neuro
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Page/Page column 41
(2010/02/12)
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- Preparation and bioactivity of pyranole derivatives as potential cross-linking agent
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A series of pyrazole derivatives with two and three alkylating sites were prepared and their cytotoxicity against cancer cells as well as antitumor activity against L1210 was investigated. The best result of cytotoxicity was obtained with the trichloride
- Katayama,Oshiyama
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p. 913 - 919
(2007/10/03)
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- TAUTOMERISM OF 1-PHENYL-3-METHYL-4-BENZYL-5-PYRAZOLONE
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The tautomerism of 1-phenyl-3-methyl-4-benzyl-5-pyrazolone - a side product in the reaction of acetoacetic ester with benzaldehyde phenylhydrazone - was studied by IR and PMR spectroscopy, and its thermodynamic characteristics were determined.
- Vinokurov, V. G.,Zykov, D. A.,Kirsanova, Z. D.,Rozenberg, S. G.,Troitskaya, V. S.,et al.
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p. 288 - 291
(2007/10/02)
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