87100-61-6Relevant academic research and scientific papers
Evaluation of heteroatom-rich derivatives as antitubercular agents with InhA inhibition properties
Moulkrere, Bachar Rébat,Orena, Beatrice S.,Mori, Giorgia,Saffon-Merceron, Nathalie,Rodriguez, Frédéric,Lherbet, Christian,Belkheiri, Nadji,Amari, Mohamed,Hoffmann, Pascal,Fodili, Mokhtar
, p. 308 - 320 (2018/04/19)
Two series of heterocyclic compounds derived from 3-acetyl-4-hydroxy-6-methyl-2H-pyran-2-one (DHA) and 2-acetylbutyrolactone have been synthesized and characterized. The compounds were evaluated for their activities against Mycobacterium tuberculosis stra
1,4-Disubstituted-5-hydroxy-3-methylpyrazoles and some derived ring systems as cytotoxic and DNA binding agents. Synthesis, in vitro biological evaluation and in silico ADME study
Hany Badr, Mona,Abd El Razik, Heba Attia
, p. 442 - 457 (2017/09/27)
Some novel polysubstituted pyrazoles, bipyrazoles and pyranopyrazoles, supported with various chemotherapeutically-active pharmacophores, were synthesized and biologically evaluated for their cytotoxic potential. Fifteen compounds (7–9, 12, 16, 17, 19, 21
One-Pot Three-Component Synthesis of Bispyrazole-thiazole-pyran-2-one Heterocyclic Hybrids
Saidoun, Aicha,Boukenna, Leila,Rachedi, Yahia,Talhi, Oualid,Laichi, Yacine,Lemouari, Najet,Trari, Mohamed,Bachari, Khaldoun,Silva, Artur M.S.
, p. 1776 - 1780 (2018/07/02)
A new series of some interesting bispyrazole-thiazole-pyran-2-one heterocyclic hybrids has been efficiently synthesized via a one-pot catalyst-free three-component reaction of α-bromoacetylated pyran-2-one derivatives, thiosemicarbazide, and polysubstitut
Synthesis, Anti-Inflammatory Activity, and COX-1/2 Inhibition Profile of Some Novel Non-Acidic Polysubstituted Pyrazoles and Pyrano[2,3-c]pyrazoles
Faidallah, Hassan M.,Rostom, Sherif A. F.
, (2017/05/05)
The synthesis and evaluation of the anti-inflammatory activity of some structure hybrids comprising basically the 5-hydroxy-3-methyl-1-phenyl-4-substituted-1H-pyrazole scaffold directly linked to a variety of heterocycles and functionalities, or annulated
N-substituted [phenyl-pyrazolo]-oxazin-2-thiones as COX-LOX inhibitors: Influence of the replacement of the oxo -group with thioxo- group on the COX inhibition activity of N-substituted pyrazolo-oxazin-2-ones
Bennamane, Nora,Nedjar-Kolli, Bellara,Geronikaki, Athina A.,Eleftheriou, Phaedra Th.,Kaoua, Rachedine,Boubekeur, Kamal,Hoffman, Pascal,Chaudhary, Shailendra S.,Saxenaf, Anil K.
scheme or table, (2011/05/06)
Targeting to the synthesis of potent dual acting COX/LOX inhibitors as future anti-inflammatory drugs, we attempted a modification of the compounds based on docking analysis results. A substitution of the oxygen of the oxo-group of the oxazin-2-one ring b
Synthesis of some pyrano[2,3-c]pyrazoles
Pavlik, James W.,Ervithayasuporn, Vuthichai,Tantayanon, Supawan
, p. 710 - 714 (2011/07/31)
Synthetic methods have been developed to prepare pyrano[2,3-c]pyrazoles with various substituents at ring positions 1, 3, and 6. The 1H- and 13C-NMR properties of these products and their precursors are presented and discussed.
Synthesis and in silico biological activity evaluation of new N-substituted pyrazolo-oxazin-2-one systems
Benaamane, Nora,Nedjar-Kolli, Bellara,Bentarzi, Yamina,Hammal, Lamouri,Geronikaki, Athina,Eleftheriou, Phaedra,Lagunin, Alexey
, p. 3059 - 3066 (2008/09/20)
Cyclisation of pyrazolo-β-enaminones 3 readily obtained from 4-aceto acetyl pyrazol 2 with triphosgene led to the formation of N-substituted pyrazolo-1,3-oxazin-2-ones 4 in good yields. Estimation of pharmacotherapeutic potential, possible molecule mechan
C-C bond cleavage studies in bipyrazoles: A convenient synthesis of pyrazolo-5-ols
Singh, Shiv P.,Naithani, Rajesh,Aggarwal, Ranjana,Prakash, Om
, p. 611 - 619 (2007/10/03)
The treatment of 4-acetoacetyl derivative (3) of the pyrazoles with hydrazines in ethanol/HCl furnished a variety of bipyrazoles (4). However, when the reaction was performed in sodium acetate/acetic acid/ethanol, different hydrazines gave different products. Under these conditions an unexpected C-C bond cleavage was observed thus affording a convenient route for the formation of pyrazolo-5-ols (5 and 6).
Pyranopyrazoles III synthesis of 1H-pyrano[2,3-c]pyrazol-4-ones [1]
Khan,Ellis,Pagotto
, p. 193 - 197 (2007/10/03)
Various derivatives of title ring system were synthesized by Claisen condensation of 4 acetyl-5-hydroxypyrazoles with appropriate esters, followed by acid-catalyzed ring closure.
Synthesis and A1 and A(2A) adenosine binding activity of some pyrano[2,3-c]pyrazol-4-ones
Colotta, Vittoria,Catarzi, Daniela,Varano, Flavia,Melani, Fabrizio,Filacchioni, Guido,Cecchi, Lucia,Trincavelli, Letizia,Martini, Claudia,Lucacchini, Antonio
, p. 189 - 196 (2007/10/03)
A series of pyrano[2,3-c]pyrazol-4-ones was synthesized and evaluated for bovine brain adenosine A1 and A(2A) receptor binding affinity. Substituents at positions 5 and/or 6 were varied in order to define the structure-activity relationships in
