ChemInform Abstract: Synthesis and Preliminary Evaluation of New 5‐Pyrazolinone Derivatives as Analgesic Agents.

Guersoy, A.; Demirayak, Şeref; Çapan, Gültaze; Erol, Kevser; Vural, Kamıl

doi:10.1002/chin.200030104

Cited by 35 publications

(39 citation statements)

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“…Pyrazolidine and pyrazoline heterocycles are attractive subunits in many complex natural products and bioactive compounds, which demonstrate high potential as antidepressants, [1] acyltransferase inhibitors, [2] analgesic agents, [3] and antimicrobial agents; [4] they show antitumor [5] and anticonvulsant [6] ( Figure 1) activities or can be used in agriculture as arthropodicidal agents. [7] [3+2] Cycloaddition of hydrazones to olefins is one of the most versatile reactions providing direct access to pyrazolidines and pyrazolines.…”

Section: Introductionmentioning

confidence: 99%

Silicon Lewis Acid Catalyzed [3+2] Cycloaddition Reactions of Hydrazones/Cyclopentadiene: Mild Access to Pyrazolidine Derivatives

et al. 2011

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A first and fairly mild metal-free catalytic route was developed for the [3+2] cycloadditions of different N-acylhydrazones to cyclopentadiene, providing the synthetically and biologically important five-membered cyclic compounds pyrazolidines. The reaction was successfully conducted in high yields (up to 99 %) with high diastereoselectivities (up to 98:2 dr) by using catalytic amounts of TMSOTf (trimethylsilyl

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Section: Introductionmentioning

confidence: 99%

Silicon Lewis Acid Catalyzed [3+2] Cycloaddition Reactions of Hydrazones/Cyclopentadiene: Mild Access to Pyrazolidine Derivatives

et al. 2011

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“…As part of our continuous research in this area, several new pyrazoline derivatives were synthesized. Previously, pyrazoline moieties showed a broad spectrum of biological activities such as anticonvulsant [9], antidepressant [10], antibacterial [11], analgesic [12], antimicrobial [13], and antiandrogenic [14] activities.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and In‐Vivo Pharmacological Screening of N,3‐(Substituted Diphenyl)‐5‐phenyl‐1H‐pyrazoline‐1‐carbothioamide Derivatives

Siddiqui¹,

Alam

Ahsan

2009

Archiv der Pharmazie

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Various 3,5-(substituted diphenyl)-4,5-dihydro-pyrazole-1-carbothioic acid phenylamides were synthesized starting from substituted acetophenones. Structures of the compounds were confirmed on the basis of spectral data. The compounds were evaluated for their anticonvulsant and antidepressant activity. Interestingly, out of 26 compounds, four (3f, 3g, 3t, and 3u) were found to protect 100% of the animals in the MES screen at a dose of 25 mg/kg. They were also found to have appreciable anticonvulsant activity in scPTZ screen. Two compounds, 3j and 3o, significantly reduced the duration of the immobility time at 25 mg/kg dose, when compared to control.

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“…[10][11][12][13][14][15][16][17][18][19] On the other hand, pyrazole and their derivatives are associated with various pharmaceutical activities. 20,21 We reported previously the synthesis and biological activity evaluation of a new series of Nsubstituted pyrazolo-oxazin-2-one compounds on the basis of PASS prediction results. Positive COX-1 inhibition activity predicted by PASS was confirmed by experimental evaluation 22 although the compounds exhibited only mild inhibitory action.…”

Section: Introductionmentioning

confidence: 99%

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

Geronikaki¹,

Bennamane²,

Nedjar-Kolli³

et al. 2010

Arkivoc

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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 by sulphur resulted in a four to over ten fold improvement of COX and LOX inhibitory action. N-phenyl derivatives exhibited the best biological properties with the 4-methoxy-phenyl derivative showing the best COX-1 and LOX inhibitory action and the 4-Br-phenyl derivative exhibiting the best COX-2 inhibitory action combined with good COX-1 and LOX inhibitory capacity.

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ChemInform Abstract: Synthesis and Preliminary Evaluation of New 5‐Pyrazolinone Derivatives as Analgesic Agents.

Cited by 35 publications

References 1 publication

Silicon Lewis Acid Catalyzed [3+2] Cycloaddition Reactions of Hydrazones/Cyclopentadiene: Mild Access to Pyrazolidine Derivatives

Silicon Lewis Acid Catalyzed [3+2] Cycloaddition Reactions of Hydrazones/Cyclopentadiene: Mild Access to Pyrazolidine Derivatives

Design, Synthesis, and In‐Vivo Pharmacological Screening of N,3‐(Substituted Diphenyl)‐5‐phenyl‐1H‐pyrazoline‐1‐carbothioamide Derivatives

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

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