Synthesis and pharmacological properties of N,N-dialkyl(dialkenyl)amides of 7-methyl-3-phenyl-1-[2-hydroxy-3-(4-phenyl-1-piperazinyl)propyl]-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-5-carboxylic acid

Sladowska, H; Sabiniarz, Aleksandra; Filipek, Barbara; Kardasz, Małgorzata; Maciąg, Dorota

doi:10.1016/s0014-827x(02)00011-3

Cited by 12 publications

(3 citation statements)

References 6 publications

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“…4 Compound V has analgesic effect [Median Lethal Dose 50 (LD 50 ) = 25 mg/kg]. 5 Compound VI demonstrates dual antileishmanial and antituberculosis activity (IC 50 = 10.23 ± 1.50 μg/mL; MIC = 25 μg/mL) 6 (Figure 1 ). Thus, the construction of pyrido[2,3- d ]pyrimidines has attracted much interest from chemists and a number of efficient methodologies have been developed.…”

Section: Table 1 Optimization Of the Reaction Condition...mentioning

confidence: 99%

Synthesis of Pyrido[2,3-d]pyrimidines Catalyzed by 2,3-Dichloro-5,6-dicyano-1,4-benzoquinone (DDQ)/tert-Butyl Nitrite (TBN)/O2

Cheng,

Li,

et al. 2023

Synthesis

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Catalyzed by 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ)/tert-butyl nitrite (TBN)/O2, an efficient tandem oxidative reaction of uracils/thiouracil with 1,3-diarylpropenes is disclosed. It undergoes oxidative coupling, intramolecular cyclization, and dehydro-aromatization to provide multi-substituted pyrido[2,3-d]pyrimidines/thiopyrido[2,3-d]pyrimidines in moderate to excellent yields. It has the advantages of high atom economy, green terminal oxidant, and metal-free conditions.

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Section: Table 1 Optimization Of the Reaction Condition...mentioning

confidence: 99%

Synthesis of Pyrido[2,3-d]pyrimidines Catalyzed by 2,3-Dichloro-5,6-dicyano-1,4-benzoquinone (DDQ)/tert-Butyl Nitrite (TBN)/O2

Cheng,

Li,

et al. 2023

Synthesis

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“…However, TRP is able to give therapeutic improvement in cases of chronic and severe insomniacs characterized by both sleep-onset and sleep-maintenance problems only after several days to weeks of therapy [7]. The heterocyclic antidepressants are the mainstay of antidepressant treatment and the development of new synthetic heterocyclic compounds as antidepressant, sedative, or analgesic agents has progressed considerably during the past decade [8][9][10]. In the scope of a research program aimed at the development of new alternatives to treat neurological disorders [11][12][13], in the present study, we describe the synthesis of new functionalized bi-heterocyclic or tri-heterocyclic compounds ( Fig.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antidepressant Evaluation of Five Novel Heterocyclic Tryptophan‐Hybrid Derivatives

Elmegeed

Baiuomy

Abdelhalim

et al. 2010

Archiv der Pharmazie

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This study aimed at evaluating the reactivity of L-Tryptophan (TRP) 1 towards various chemical reagents to produce new bi- and tri-heterocyclic systems providing basic pharmacological activities. Indol-3-yl hydroxyoxazol-2-yl acetonitrile derivatives 5 and 6, indol-3-yl-hydroxyoxazol-2-yl-1,2,4-triazine derivatives 8 and 9, indol-3-yl-hydroxyoxazol-2-yl-aminopyrazole derivatives 11a, b, and indol-3-yl-hydroxyoxazol-2-yl-aminoisoxazole derivative 12 were synthesized via straightforward and efficient methods. The structures were characterized by spectral data (IR, (1)H-NMR, (13)C-NMR, and MS) and the purity was ascertained by microanalysis. Also, this work was extended to study the potential role of the novel synthesized TRP derivatives 5, 6, 9, 11a, and 12 as antidepressant and sedative agents in comparison with TRP. All compounds showed significant antidepressant activity in the forced-swimming test at two doses (50 or 100 mg/kg). Also, all tested compounds (at 50 or 100 mg/kg) produced a significant decrease in locomotor activity of mice during a 30 min observation period. The most potent antidepressant and sedative effect was produced by the tri-heterocyclic compounds 9 and 12, followed by 11a and TRP.

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“…Furthermore, many fused pyridine derivatives such as pyrazolo [3,4-b]pyridines induced reduction of pro-inflammatory cytokines and were found to possess anti-inflammatory and analgesic activities [3,4]. Several reports revealed that pyrido [2,3-d]pyrimidine exerted promising anti-inflammatory and analgesic activities [5,6]. Herein, we report the preparation and evaluation of anti-inflammatory and analgesic activities of a new series of 1-pyrazolyl-2-pyridone-3-carbonitriles and fused analogs, with the objective of determining the influence of different 4-, 5-, and 6-substituents of the pyridine-2-one nucleus on the biological activity.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Novel 1‐Pyrazolylpyridin‐2‐ones as Potential Anti‐Inflammatory and Analgesic Agents

Ismail

Ammar

El‐Zahaby

et al. 2007

Archiv der Pharmazie

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A new series of 4-alkyl/aryl-2-oxo-1-pyrazolyl-1,2-dihydropyridine-3-carbonitriles, pyrazolo[3,4-b]pyridine-5-carbonitriles and pyrido[2,3-d]pyrimidine-6-carbonitriles have been synthesized and tested for their anti-inflammatory and analgesic activities. Among the tested compounds, 3e and 8b exhibited comparable anti-inflammatory activity to the standard (indomethacin). Compounds 5, 7a, and 8b displayed potent analgesic activity. Detailed syntheses, spectroscopic and biological data are reported.

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Synthesis and pharmacological properties of N,N-dialkyl(dialkenyl)amides of 7-methyl-3-phenyl-1-[2-hydroxy-3-(4-phenyl-1-piperazinyl)propyl]-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-5-carboxylic acid

Cited by 12 publications

References 6 publications

Synthesis of Pyrido[2,3-d]pyrimidines Catalyzed by 2,3-Dichloro-5,6-dicyano-1,4-benzoquinone (DDQ)/tert-Butyl Nitrite (TBN)/O2

Synthesis of Pyrido[2,3-d]pyrimidines Catalyzed by 2,3-Dichloro-5,6-dicyano-1,4-benzoquinone (DDQ)/tert-Butyl Nitrite (TBN)/O2

Synthesis and Antidepressant Evaluation of Five Novel Heterocyclic Tryptophan‐Hybrid Derivatives

Synthesis of Novel 1‐Pyrazolylpyridin‐2‐ones as Potential Anti‐Inflammatory and Analgesic Agents

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