- Microwave-assisted Vilsmeier-Haack synthesis of Pyrazole-4-carbaldehydes
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The synthesis of 4-formylpyrazoles using Vilsmeier-Haack reagent is a common protocol in pyrazole chemistry. An efficient microwave-assisted synthesis of 4-formylpyrazoles by employing Vilsmeier-Haack reagent (OPC-VH) derived from phthaloyl dichloride/dimethylformamide has been described. This method offers the advantages of operational simplicity, avoiding the use of POCl3 as toxic reagents and reuse of the by-product in the preparation of phthaloyl dichloride.
- Kumari, Poonam,Sood, Sumit,Kumar, Anil,Singh, Karan
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p. 796 - 804
(2019/11/28)
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- Microwave-assisted synthesis and biological evaluation of pyrazole-4-carbonitriles as antimicrobial agents
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An efficient microwave-assisted method of synthesis of pyrazole-4-carbonitriles has been developed. Condensation of pyrazole-4-carbaldehydes with hydroxylamine hydrochloride followed by reaction of the resulting oximes with the Vilsmeier-Haack reagent pre-formed from phthaloyl dichloride and dimethylformamide under microwave irradiation afforded the corresponding pyrazole-4-carbonitriles in 73percent to 91percent yield. The operational simplicity, avoidance of toxic reagents such as POCl3, shorter reaction time, higher yield compared to the classical version, easy work up, and the use of the by-product in the regeneration of phthaloyl dichloride are the advantages of this methodology. All the target compounds were tested for antimicrobial activity against Gram-positive bacteria Bacillus cereus and Staphylococcus aureus; Gram-negative bacteria Escherichia coli and Yersinia enterocolitica, and the fungal species Candida albicans.
- Kumar, Anil,Kumari, Poonam,Singh, Karan,Sood, Sumit,Yadav, Ajar Nath
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- Synthesis and evaluation of biological activities of 4-cyclopropyl-5-(2-fluorophenyl) arylhydrazono-2,3-dihydrothiazoles as potent antioxidant agents
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A new series of 4-cyclopropyl-5-(2-fluorophenyl)arylhydrazono-2,3-dihydrothiazole derivatives was synthesized via the reaction of prepared thiosemicarbazones with 2-bromo-1-cyclopropyl-2-(2-uorophenyl)ethanone in the presence of Et3 N as a catalyst throug
- Ghanbari Pirbasti,Mahmoodi, Nosrat O.,Abbasi Shiran, Jafar
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p. 196 - 210
(2016/03/25)
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- Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease
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A series of thirty (30) thiazole analogs were prepared, characterized by 1H NMR, 13C NMR and EI-MS and evaluated for Acetylcholinesterase and butyrylcholinesterase inhibitory potential. All analogs exhibited varied butyrylcholinester
- Rahim, Fazal,Javed, Muhammad Tariq,Ullah, Hayat,Wadood, Abdul,Taha, Muhammad,Ashraf, Muhammad,Qurat-Ul-Ain,Khan, Muhammad Anas,Khan, Fahad,Mirza, Salma,Khan, Khalid M.
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p. 106 - 116
(2015/09/02)
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- Structure-activity relationship study of thiosemicarbazones on an African trypanosome: Trypanosoma brucei brucei
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To explore the structure-activity relationships of thiosemicarbazones on African trypanosome: Trypanosoma brucei brucei, a series of thirty-five thiosemicarbazones (1-35) have been synthesized and characterized by their 1H NMR, 13C NMR, and FT-IR spectra. All compounds were tested for trypanocidal activity using the method "Lilit alamar blue". The comparison of trypanocidal power of thiosemicarbazones was performed considering their structures. This study that was done using acetophenone thiosemicarbazone (1) as basic model, showed that: (a) the presence of lipophilic substituents in para position on benzene ring, (b) substitution of benzene ring and (c) substitution of hydrogen of thioamide function by a phenyl, strongly influence trypanocidal activity. The various modifications to basic structure (1) allowed the synthesis of 1-(4-chlorophenyl) ethylidene-4-phenyl- thiosemicarbazide (34). With a trypanocidal activity of 3.97 μM, this compound is the most active of the series.
- Fatondji, Houssou Raymond,Kpoviessi, Salome,Gbaguidi, Fernand,Bero, Joanne,Hannaert, Veronique,Quetin-Leclercq, Joelle,Poupaert, Jacques,Moudachirou, Mansourou,Accrombessi, Georges Coffi
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p. 2151 - 2162
(2013/07/26)
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- Ketonethiosemicarbazones: Structure-activity relationships for their melanogenesis inhibition
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A series of 2-(1-phenylalkylidene)hydrazinecarbothioamides 2, 2-(1-phenylalkyl)hydrazinecarbothioamides 3, 2-(3,4-dihydronaphthalen-1(2H)- ylidene)hydrazinecarbothioamide (4), and 2-(1-(thiophen-2-yl)ethylidene) hydrazinecarbothioamide (5) were synthesize
- Thanigaimalai, Pillaiyar,Lee, Ki-Cheul,Sharma, Vinay K.,Roh, Eunmiri,Kim, Youngsoo,Jung, Sang-Hun
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supporting information; experimental part
p. 3527 - 3530
(2011/07/31)
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- Ruthenium(II) mediated C-H activation of substituted acetophenone thiosemicarbazones: Synthesis, structural characterization, luminescence and electrochemical properties
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Treatment of [RuHCl(CO)(AsPh3)3] with 4′-substituted acetophenone thiosemicarbazone derivatives in methanol under reflux afford a series of air stable new ruthenium(II) cyclometalated complexes containing thiosemicarbazone of general
- Prabhu, Rupesh Narayana,Pandiarajan, Devaraj,Ramesh, Rengan
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experimental part
p. 4170 - 4177
(2010/03/24)
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- 1-(1-Arylethylidene)thiosemicarbazide derivatives: A new class of tyrosinase inhibitors
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A series of 1-(1-arylethylidene)thiosemicarbazide compounds and their analogues were synthesized and characterized by 1H NMR, MS. Their tyrosinase inhibitory activities were investigated by an assay based on the catalyzing ability of tyrosinase
- Liu, Jinbing,Yi, Wei,Wan, Yiqian,Ma, Lin,Song, Huacan
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p. 1096 - 1102
(2008/09/18)
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- M-STAGE KINESIN INHIBITOR
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A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, -C(=W)R6 (wherein W represents an oxygen atom or a sulfur atom, and R6 represents substituted or unsubstituted lower alkyl and the like) and the like, R3 represents -C(=Z)R19 (wherein Z represents an oxygen atom or a sulfur atom, and R19 represents substituted or unsubstituted lower alkyl and the like) and the like, R4 represents substituted or unsubstituted lower alkyl and the like, and R5 represents substituted or unsubstituted aryl and the like] and the like are provided.
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Page/Page column 73
(2010/11/08)
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- THIADIAZOLINE DERIVATIVE
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(wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents -C(-W)R6 or the like; R3 represents a hydrogen atom, -C(=WA)R6A, or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.
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