881667-32-9Relevant articles and documents
One pot synthesis of thiazolo[2,3-b]dihydropyrimidinone possessing pyrazole moiety and evaluation of their anti-inflammatory and antimicrobial activities
Viveka, Shivapura,Dinesha,Nagaraja, Gundibasappa Karikannar,Shama, Prasanna,Basavarajaswamy, Guru,Rao, K. Poornachandra,Yanjarappa Sreenivasa, Marikunte
, p. 171 - 185 (2018)
A series of pyrazole integrated thiazolo[2,3-b]dihydropyrimidinone derivatives were synthesized as dual anti-inflammatory and antimicrobial agents. Among the compounds studied, 3-fluoro-4-methylphenyl analogues (3a, 3e, and 3i) are considered to be promising leads for novel anti-inflammatory agents compared with the standard drug. The superior antimicrobial property of the compounds 3a, 3b, and 3d indicates that 3-(3,4-dichlorophenyl)-1-phenyl-1H-pyrazole substitution is a favourable site for high activity. Molecular docking studies were carried out in order to predict the hypothetical binding mode of these compounds to the COX-2 isoenzyme. The results of the present study suggest that 1,3-diaryl pyrazole substitution on thiazolo[2,3-b]dihydropyrimidinone derivatives might potentially constitute a novel class of anti-inflammatory agents with antimicrobial property and could be an interesting approach for the design of new selective COX-2 inhibitory agents.
New library of pyrazole–imidazo[1,2-α]pyridine molecular conjugates: Synthesis, antibacterial activity and molecular docking studies
Ebenezer, Oluwakemi,Awolade, Paul,Koorbanally, Neil,Singh, Parvesh
, p. 162 - 173 (2019/11/03)
A library of novel pyrazole–imidazo[1,2-α]pyridine scaffolds was designed and synthesized through a one-pot three-component tandem reaction. The structures of synthesized conjugates were confirmed by spectroscopic techniques (NMR, IR and HRMS). In vitro antibacterial evaluation of the twelve synthesized molecules (7a, 8a–k) against methicillin-resistant Staphylococcus aureus and normal strains of Escherichia coli, Salmonella typhimurium, Klebsiella pneumonia and Pseudomonas aeruginosa established 8b, 8d, 8e, 8h and 8i as potent antibacterial agents with superior minimum bactericidal concentration, compared with standard drug ciprofloxacin. Molecular docking studies of all active compounds into the binding site of glucosamine-6-phosphate synthase were further performed in order to have a comprehensive understanding of putative binding modes within the active sites of the receptor.
Synthesis of new pyrazole derivatives via multicomponent reaction and evaluation of their antimicrobial and antioxidant activities
Viveka, Shivapura,Dinesha,Madhu, Leelavathi Narayana,Nagaraja, Gundibasappa Karikannar
, p. 1547 - 1555 (2015/02/19)
Abstract This work describes a facile synthesis and characterization of a new series of pyrazole containing pyrimidine, 1,4-dihydropyridine, and imidazole derivatives using substituted 4-formylpyrazole as a key intermediate via multicomponent reaction seq
THIAZOLIDIN-4-ONES HAVING ANTI-HEPATITIS B ACTIVITY
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Page/Page column 30, (2010/10/20)
The invention provides compounds having the following general structure (I): wherein X is S, O, or N and X’ is N or C. The compounds are useful for preventing and treating hepatitis B virus (HBV) infections in mammals, and for preventing and treating diseases associated with HBV infection.