428840-36-2Relevant academic research and scientific papers
Microwave-assisted synthesis and biological evaluation of pyrazole-4-carbonitriles as antimicrobial agents
Kumar, Anil,Kumari, Poonam,Singh, Karan,Sood, Sumit,Yadav, Ajar Nath
, (2020/05/25)
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.
Design, synthesis, in Silico toxicity prediction, molecular docking, and evaluation of novel pyrazole derivatives as potential antiproliferative agents
Parameshwar, Ravula,Harinadha Babu, Vamaraju,Manichandrika, Paturi,Narendra Sharath Chandra,Swetha, Kolli
, p. 187 - 202 (2016/03/12)
A new series of pyrazole derivatives were designed by docking into vascular endothelial growth factor receptor-2 (VEGFR-2) kinase active site. The designed compounds were synthesized and evaluated for in vitro antiproliferative activity against HT-29 colo
Synthesis of novel pyrazolyl tetrazoles as selective COX-2 inhibitors
Swetha, Kolli Sri,Parameshwar, Ravula,Reddy, B. Madhava,Babu, V. Harinadha
, p. 4886 - 4892 (2013/09/23)
A series of novel pyrazolyl tetrazoles were synthesized by introducing tetrazole moiety at the fourth position of 1,3-substituted pyrazole nucleus. Synthesis was carried out by cyclization of different pyrazolonitriles using sodium azide in the presence of triethylammonium chloride as phase transfer catalyst. The structures of the synthesized compounds were confirmed on the basis of physical and spectral data. Among the synthesized compounds, 4b and 4e displayed significant anti-inflammatory activity with no observable ulcerogenic effect when compared with diclofenac sodium. Furthermore, compounds 4b and 4e were found to have COX-2 selectivity with a ratio of 0.44 and 0.48, respectively.
Synthesis and antinociceptive activity of pyrazolyl isoxazolines and pyrazolyl isoxazoles
Karthikeyan,Veenus Seelan,Lalitha,Perumal
scheme or table, p. 3370 - 3373 (2010/02/28)
Pyrazolyl isoxazolines and isoxazoles were synthesised in moderate to good yields using 1,3-dipolar cycloaddition of pyrazole derived nitrile oxide with various dipolarophiles such as N-substituted maleimide, diethylacetylene dicarboxylate and phenylacety
One-pot synthesis of oxime derivatives of 1,3-diphenylpyrazole-4- carboxaldehydes from acetophenone phenylhydrazones using vilsmeier-haack reagent
Prakash, Om,Pannu, Kamaljeet,Naithani, Rajesh,Kaur, Harpreet
, p. 3479 - 3485 (2007/10/03)
A one-pot synthesis of oxime derivatives 3a-3f of 1-phenyl-3-arylpyrazole- 4-carboxaldehydes has been accomplished by the Vilsmeier-Haack reaction of acetophenone phenylhydrazones 1a-1f under a new workup procedure. Copyright Taylor & Francis Group, LLC.
Synthesis of 1,3-diaryl-4-cyanopyrazoles from the corresponding aldoximes using dimethylformamide-thionylchloride complex
Reddy, G. Jagath,Sailaja,Pallavi,Rao, K. Srinivasa
, p. 180 - 183 (2007/10/03)
A mild and convenient method for the synthesis of 1,3-diaryl-4- cyanopyrazoles 4 from the corresponding aldoximes 2 using dimethylformamide- thionylchloride complex 3 is reported.
