- Synthesis and biological evaluation of some coumarin hybrids as selective carbonic anhydrase IX and XII inhibitors
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Two series, coumarin-linked to thiazolidinone via a pyrazole linker (6a-m, Series 1) and coumarin-linked 1,2,3-triazoles (5a-j, Series 2) were synthesized and the synthesized compounds were subjected for evaluation against the four physiologically and pha
- Alvala, Mallika,Angeli, Andrea,Argulwar, Omkar S.,Arifuddin, Mohammed,Soman, Jyothsna,Sridhar Goud, Nerella,Supuran, Claudiu T.,Thacker, Pavitra S.
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- Simple Michael acceptor type coumarin derived turn-on fluorescence probes to detect cyanide in pure water
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The present article describes design and synthesis of coumarin derived chemical reaction based chemodosimeter to recognize cyanide in aqueous medium. The Michael acceptor type coumarin derived probes 3 and 4 upon interaction with cyanide undergo Michael t
- Razi, Syed S.,Ali, Rashid,Srivastava, Priyanka,Misra, Arvind
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- Synthesis of novel substituted 3-(4-((1H-benzo[d]imidazol-2-ylthio)methyl)-1-phenyl-1H-pyrazol-3-yl)-2H-chromen-2-ones: various approaches
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Abstract: Considering benzimidazole as a privileged structure for developing probes of impressive pharmacological potentials, some new coumarin and pyrazole conjugates of benzimidazoles were synthesized with a sulphur linkage. Thus, 3-(2-oxo-2H-chromen-3-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde (3) was prepared starting from simple salicylaldehyde which has been?used as an important synthon and incorporated in a series of structural manipulations to obtain various of pharmacophoric motif conjugates 9(a–b) and 13(a–f), in fair yields. We have developed facile and stepwise methods for the synthesis of all these compounds in various approaches, which also involves sub-sequences. All synthesized compounds were well characterized by IR, 1HNMR, 13CNMR and mass spectra data.
- Srikrishna, Devulapally,Dubey, Pramod Kumar
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- Synthesis of some hippuric acid substrate linked novel pyrazoles as antimicrobial agents
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Escalating resistance of microorganisms to the currently accessible antimicrobial drugs has forced to synthesize some novel biologically active compounds as efficient alternates via economical substrates. Hence, hippuric acid was used as one of the starting materials to synthesize pyrazole derivatives. All the synthesized compounds were characterized by IR, NMR (1H & 13C) and mass spectral data. The antimicrobial potential of synthesized compounds has been explored against four bacterial and two fungal strains. Among the 12 compounds, 3 compounds 8j, 8k and 8l were found to exhibit prominent antimicrobial potential as compared with the standards ciprofloxacin and amphotericin-B.
- Verma, Anil,Kumar, Vinod,Khare, Rajshree,Singh, Joginder
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- Instantaneous and Selective Bare Eye Detection of Inorganic Fluoride Ion by Coumarin–Pyrazole-Based Receptors
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A series of rationally designed coumarin–pyrazole-based scaffolds, equipped with N―H and C―H hydrogen bond donors (R1–R5) and containing various electron-withdrawing groups at key positions, are synthesized and characterized in order to investigate their
- Jain, Anshu,Gupta, Ragini,Agarwal, Madhu
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- 3-(2,2-Dicyano-1-methylvinyl)coumarin in Heterocyclic Synthesis: Synthesis of Some New Coumarin Derivatives
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The reaction of 3-acetylcoumarin with activated nitrites provides a convenient route to a range of new coumarin derivatives.
- Selim, Mohamed R.
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- Synthesis, Photophysical and Computational Study of Novel Coumarin-based Organic Dyes
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A series of novel coumarin pyrazoline moieties combined with tetrazoles, 3-(1-phenyl-4-(1H-tetrazol-5-yl)-1H-pyrazol-3-yl)-2H-chromen-2-one, 6-chloro-3-(1-phenyl-4-(1H-tetrazol-5-yl)-1H-pyrazol-3-yl)-2H-chromen-2-one, 6-bromo-3-(1-phenyl-4-(1H-tetrazol-5-
- Kumbar, Mahadev N.,Sannaikar, Madivalagouda S.,Shaikh, Saba Kauser J.,Kamble, Atulkumar A.,Wari, Manjunath N.,Inamdar, Sanjeev R.,Qiao, Qiquan,Revanna, Bhavya N.,Madegowda, Mahendra,Dasappa, Jagadeesh P.,Kamble, Ravindra R.
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p. 261 - 276
(2018/02/06)
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- Some new indole-coumarin hybrids; Synthesis, anticancer and Bcl-2 docking studies
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Hybrid molecules have attracted attention for their improved biological activity, selectivity and lesser side effects profile, distinct from their individual components. In the quest for novel anticancer drug entities, three series of indole-coumarin hybrids - 3-(1-benzyl-1H-indol-2-yl)-2H-chromen-2-ones, 2-(2-oxo-2H-chromen-3-yl)-1H-indole-3-carbaldehydes and 2-(2-oxo-2H-chromen-3-yl)-1H-indole-3-carboxylic acids were synthesized. All the synthesized compounds were characterized by spectral techniques like IR, 1H NMR, 13C NMR, mass spectrometry and elemental analysis. In silico docking studies of synthesized molecules with apoptosis related gene Bcl-2 that is recognized to play an important role in tumerogenesis were carried out. Dose-dependent cytotoxic effect of the compounds in human breast adenocarcinoma (MCF-7) and normal cell lines were assessed using MTT assay and compared with that of the standard marketed drug, Vincristine. Compound 4c had a highly lipophilic bromine substituent capable of forming halogen bond and was identified as a potent molecule both in docking as well as cytotoxicity studies. Flow cytometric cell cycle analysis of 4c exhibited apoptotic mode of cell death due to cell cycle arrest in G2/M phase. Structure activity relationship of these hybrid molecules was also studied to determine the effect of steric and electronic properties of the substituents on cell viability.
- Kamath, Pooja R.,Sunil, Dhanya,Ajees, A. Abdul,Pai,Das, Shubhankar
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p. 101 - 109
(2015/10/28)
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- 3-(1-Phenyl-4-((2-(4-arylthiazol-2-yl)hydrazono)methyl)-1H-pyrazol-3-yl)-2H-chromen-2-ones: One-pot three component condensation, in vitro antimicrobial, antioxidant and molecular docking studies
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In an attempt to find a new class of heterocyclic bio-active agents, a series of novel 3-(1-phenyl-4-((2-(4-arylthiazol-2-yl)hydrazono)methyl)-1H-pyrazol-3-yl)-2H-chromen-2-one derivatives (5a-l) have been synthesized efficiently both quantitatively and q
- Gondru, Ramesh,Banothu, Janardhan,Thatipamula, Ranjith Kumar,Hussain Sk, Althaf,Bavantula, Rajitha
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p. 33562 - 33569
(2015/04/27)
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- Potassium carbonate-mediated efficient and convenient synthesis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1 H)-ones
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Unprecedented cyclization was observed during N-sulfonylation of 3-[1-(phenylhydrazono)-ethyl]-chromen-2-one in pyridine, affording 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones. To avoid use of noxious pyridine, reaction was tried in different basic
- Grover, Jagdeep,Roy, Somendu Kumar,Jachak, Sanjay Madhukar
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p. 1914 - 1923
(2014/07/07)
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- An efficient multichannel probe to detect anions in different media and its real application in human blood plasma
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A simple coumarin derived chromo and fluorogenic chemosensor has been synthesized and tested to detect anions in different medium. The designed chemosensor has shown a high colorimetric response for F- and AcO- ions in acetonitrile i
- Razi, Syed S.,Ali, Rashid,Srivastava, Priyanka,Shahid, Mohammad,Misra, Arvind
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p. 22308 - 22317
(2014/06/23)
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- Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors
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As a part of our continued efforts to discover new COX inhibitors, a series of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones were synthesized and evaluated for in vitro COX inhibitory potential. Within this series, seven compounds (3a-d, 3h, 3k and 3
- Grover, Jagdeep,Kumar, Vivek,Sobhia, M. Elizabeth,Jachak, Sanjay M.
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p. 4638 - 4642
(2015/01/09)
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- Synthesis and antimicrobial activity of coumarin pyrazole pyrimidine 2,4,6(1H,3H,5H)triones and thioxopyrimidine4,6(1H,5H)diones
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A series of 5-((3-(2-oxo-2H-chromen-3-yl)-1-phenyl-1H-pyrazol-4-yl) methylene)pyrimidine-2,4,6(1H,3H,5H)-trione (4a-f) and dihydro-5-((3-(2-oxo-2H- chromen-3-yl)-1-phenyl-1H-pyrazol-4-yl)methylene)-2-thioxopyrimidine-4,6(1H,5H) -dione (5a-f) derivatives w
- Vijaya Laxmi,Suresh Kuarm,Rajitha
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p. 768 - 774
(2013/04/10)
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- Synthesis, anticancer activity and photophysical properties of novel substituted 2-oxo-2H-chromenylpyrazolecarboxylates
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2-Oxo-2H-chromenylpyrazolecarboxylates (8a-h and 12a-zb) have been synthesized by [3 + 2] cycloaddition of 2H-chromenophenylhydrazones (7a-h and 11a-w) with diethyl/dimethylbut-2-ynedioates. Phenylchromeno[4,3-c]pyrazol-4(1H) -ones (13i-n) were prepared from corresponding phenylhydrazones (7a-h) with catalytic amount of piperidine in presence of pyridine as a solvent at 100°C. All the synthesized compounds (8a-h, 12a-zb and 13a-n) were screened for anticancer activity against three human cancer cell lines such as prostate (DU-145), lung adenocarcinoma (A549), and cervical (HeLa) by standard MTT assay method. Further, photophysical properties (UV and fluorescence) for these compounds were discussed.
- Kumar, J. Ashok,Saidachary,Mallesham,Sridhar,Jain, Nishant,Kalivendi, Shashi Vardhan,Rao, V. Jayathirtha,Raju, B. China
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p. 389 - 402
(2013/10/01)
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- X-ray supramolecular structure, NMR spectroscopy and synthesis of 3-methyl-1-phenyl-1H-chromeno[4,3-c]pyrazol-4-ones formed by the unexpected cyclization of 3-[1-(phenylhydrazono)ethyl]-chromen-2-ones
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The molecular structures of nine 3-methyl-1-phenyl-1H-chromeno[4,3-c] pyrazol-4-one isomers, obtained by the oxidative cyclization of the corresponding 1-phenylhydrazono chromen-2-ones with copper acetate as catalyst, are reported. The molecular and supra
- Padilla-Martinez, Itzia I.,Flores-Larios, Irma Y.,Garcia-Baez, Efren V.,Gonzalez, Jorge,Cruz, Alejandro,Martinez-Martinez, Francisco J.
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experimental part
p. 915 - 932
(2011/04/18)
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- Synthesis of some oxazolyl - Pyrazolyl; 1,4-dihydropyridinyl-pyrazolyl and 1,2,3,4-tetrahydro pyrimidinyl-pyrazolyl coumarins
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(Chemical Equation Presented) Various 3-[1-phenyl-4-(2-substituted-5-oxo- oxazol-4-ylidenemethyl) pyrazol-3-yl] coumarins 4a-f; 3-[1-phenyl-4-(2,6- dimethyl-3,5-disubstituted-1,4-dihydropyridin-4-yl) pyrazol-3-yl] coumarins 5a-f and 3-[1-phenyl-4-(6-methy
- Patel, Mehul A.,Brahmbhatt, Dinker I.
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p. 1051 - 1055
(2008/12/20)
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- Synthesis of 3-(2-aminothiazol-4-yl)- and 3-(indol-2-yl)-coumarins using 3-acetylcoumarin as a synthon
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Condensation of 3-acetylcoumarin with formamidine disulphide dihydrobromide followed by basification gives 3-(2-aminothiazol-4-yl)coumarin, whereas its phenylhydrazone forms 3-(indol-2-yl)coumarin on heating with anhyd. zinc chloride.
- Rao, Laxmi,Mukerjee, Arya K.
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p. 166 - 167
(2007/10/02)
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