7189-04-0Relevant articles and documents
A New Series of 1,3,4-Oxadiazole Linked Quinolinyl-Pyrazole/Isoxazole Derivatives: Synthesis and Biological Activity Evaluation
Basavanna, V.,Bhadraiah, U. K.,Chandra,Chandramouli, M.,Doddamani, Shridevi,Kempaiah, C.,Lingegowda, N. S.,Ningaiah, S.
, p. 2257 - 2266 (2021/12/23)
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.
Discovery of pyrazole derivatives as potent inhibitor of NF-?B for possible benefit in abdominal aortic aneurysms
Guo, Yun,Bao, Dongming,Zhang, Chaogang
, p. 4917 - 4925 (2021/06/07)
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
Novel 5-functionalized-pyrazoles: Synthesis, characterization and pharmacological screening
Doddaramappa, Shridevi D.,Lokanatha Rai,Srikantamurthy, Ningaiah,Chandra,Chethan, Javarasetty
, p. 3671 - 3675 (2015/08/11)
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.
One-pot tandem synthesis of tetrasubstituted pyrazoles via 1,3-dipolar cycloaddition between aryl hydrazones and ethyl but-2-ynoate
Ningaiah, Srikantamurthy,Doddaramappa, Shridevi D.,Chandra,Madegowda, Mahendra,Keshavamurthy, Shubakara,Bhadraiah, Umesha K.
, p. 2222 - 2231 (2014/07/07)
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
PYRAZOLE SYNTHESIS BY COUPLING OF CARBOXYLIC ACID DERIVATIVES AND ENAMINES
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Paragraph 0167-0169, (2013/03/26)
The invention describes a novel process for synthesizing pyrazoles by means of oxidative conversion of enamines with suitable N-containing carboxylic acid derivatives.
Sc(OTf)3-catalyzed, solvent-free domino synthesis of functionalized pyrazoles under controlled microwave irradiation
Kumari, Kumkum,Raghuvanshi, Dushyant Singh,Jouikov, Viatcheslav,Singh, Krishna Nand
experimental part, p. 1130 - 1133 (2012/03/26)
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
Regioselective multicomponent synthesis of fully substituted pyrazoles and bispyrazoles catalyzed by zinc triflate
Safaei, Shirin,Mohammadpoor-Baltork, Iraj,Khosropour, Ahmad Reza,Moghadam, Majid,Tangestaninejad, Shahram,Mirkhani, Valiollah
experimental part, p. 2214 - 2222 (2011/10/18)
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
Silica chloride catalyzed one-pot synthesis of fully substituted pyrazoles
Jawale, Dhanaji V.,Pratap, Umesh R.,Mali, Jyotirling R.,Mane, Ramrao A.
scheme or table, p. 1187 - 1190 (2012/01/05)
Silica chloride catalysted one pot cyclocondensation of aldehydes, ethyl acetoacetate and phenyl hydrazine leading to substituted pyrazoles has been reported.
Efficient synthesis of pyrazoles: Oxidative C-C/N-N bond-formation cascade
Neumann, Julia J.,Suri, Mamta,Glorius, Frank
supporting information; experimental part, p. 7790 - 7794 (2011/01/09)
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
An effective and general method for the highly regioselective synthesis of 1-phenylpyrazoles from β-enaminoketoesters, tandem Blaise-acylation adducts
Ko, Young Ok,Chun, Yu Sung,Park, Cho-Long,Kim, Youngmee,Shin, Hyunik,Ahn, Sungho,Hong, Jongki,Lee, Sang-Gi
supporting information; experimental part, p. 1132 - 1136 (2009/05/30)
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
