2-(Diethylamino)thieno[1,3]oxazin-4-ones as Stable Inhibitors of Human Leukocyte Elastase

Gütschow, Michael; Kuerschner, Lars; Neumann, Ulf; Pietsch, Markus; Löser, Reik; Koglin, Norman; Eger, Kurt

doi:10.1021/jm991108w

Cited by 100 publications

(80 citation statements)

References 50 publications

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“…Four receptor subtypes (A 1 , A 2A , A 2B , A 3 ) have been defined based on pharmacological properties. 137,138 Considerable effort has been directed towards developing therapeutic agents targeting these receptors. 139 The first allosteric enhancers acting at the adenosine A 1 receptor were reported in early 1990s.…”

Section: -Substituted 2-aminothiophenes As a 1 Adenosine Receptor Almentioning

confidence: 99%

Gewald reaction: synthesis, properties and applications of substituted 2-aminothiophenes

Puterová¹,

Krutošíková²,

Végh³

2010

Arkivoc

177

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Chemistry of 2-aminothiophenes is arguably one of the most extensive and dynamic field of present-day thiophene research. Since 1961 when first report on the Gewald reaction was reported it became a universal method for synthesis of substituted 2-aminothiophenes and has gained prominence in recent times. The availability of reagents and the mild reaction conditions all contribute to the versatility of this reaction. This review summarizes the synthetic strategies for substituted 2-aminothiophenes. Consequently, details about the proposed mechanism of Gewald-like reactions and the wide scope of substituted 2-aminothiophenes for real life applications.

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Section: -Substituted 2-aminothiophenes As a 1 Adenosine Receptor Almentioning

confidence: 99%

Gewald reaction: synthesis, properties and applications of substituted 2-aminothiophenes

Puterová¹,

Krutošíková²,

Végh³

2010

Arkivoc

177

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“…DOT-3 ( Fig. 1) was synthesized as previously described (26) and was dissolved in chloroform (3 mg/ml).…”

Section: Methodsmentioning

confidence: 99%

Cholesterol esterase action on human high density lipoproteins and inhibition studies: detection by MALDI-TOF MS

Zschörnig

Pietsch

Süß

et al. 2005

Journal of Lipid Research

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“…Aryl 1,3-oxazine-4-thiones are pharmaceutical important heterocycles [1,2] [21]. The spatial arrangement of protons such as cis and trans of organic stereo chemical compounds [22] were studied using NMR spectra.…”

Section: Intrductionmentioning

confidence: 99%

“…Aryl 1,3-oxazine-4-thiones are pharmaceutical important heterocycles [1,2]. They possess various biological activities such as antimicrobial [3], hypolipidacmic [4], antidiabetic [5], anti-inflammatory [6], antimycobacterial [7], antithrombotic [8], antagonism to progesterone receptor [9], antitumor [10], antiviral [11], leucocyte clastase [12] and scrotonin reuptakes [13].…”

Section: Intrductionmentioning

confidence: 99%

Hammett Spectral Correlations in some Aryl 1,3-Oxazine-4-Thione Derivatives

Thirunarayanan

Sekar

2014

ILCPA

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A series of some aryl 1,3-oxazine-4-thione derivatives have been synthesized by 1-methyl imidazole catalyzed three component one pot synthetic method in room temperature. The purities of these thiones were studied by their physical constants and spectroscopic data. The infrared and 13 C NMR spectral data of CN and CS were correlated with Hammett substituent constants, F and R parameters using single and multi-linear regression analysis. From the results of statistical analysis, the effect of substituent on the spectral data was studied.Keywords: 1,3-oxazine-4-thiones; IR spectra; 13 C NMR spectra; Hammett correlation INTRDUCTIONAryl 1,3-oxazine-4-thiones are pharmaceutical important heterocycles [1,2] [21]. The spatial arrangement of protons such as cis and trans of organic stereo chemical compounds [22] were studied using NMR spectra. Currently chemists and spectroscopic researchers [23][24][25][26][27][28][29] have paid much more interest for correlation of spectral data with Hammett substituent constants. Thirunarayanan and Ravi [30] have studied the effect of substituents of some pyrazoline-1-ethanones. Substituent effects on the spectral group frequencies of 9H-fluorenayl bromides were studied by Thirunarayanan [31]. Sakthinathan et al., have investigated the effect of substituents on naphthyl based pyrazoline derivatives [32]. Sasikala et al.,[22] have evaluated the effect of substituents and antimicrobial activities of some 5-bromo-2-thienyl based pyrazolines. The spectral correlation of infrared and nuclear magnetic resonance spectra of E-imines have been predicted by Sakthinathan et. al. and Suresh et al.,[33,34]. Thirunarayanan and Sekar have investigated the substituent effects on the IR and NMR spectral frequencies of some 3-(3,4-

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2-(Diethylamino)thieno[1,3]oxazin-4-ones as Stable Inhibitors of Human Leukocyte Elastase

Cited by 100 publications

References 50 publications

Gewald reaction: synthesis, properties and applications of substituted 2-aminothiophenes

Gewald reaction: synthesis, properties and applications of substituted 2-aminothiophenes

Cholesterol esterase action on human high density lipoproteins and inhibition studies: detection by MALDI-TOF MS

Hammett Spectral Correlations in some Aryl 1,3-Oxazine-4-Thione Derivatives

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