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Synthesis and central nervous system activity of quinazolones related to 2-methyl-3-(o-tolyl)-4(3H)-quinazolone (methaqualone)

Autor: Peter D. Kennewell, I. R. Ager, D. R. Harrison, John B. Taylor

Publikováno v: Journal of Medicinal Chemistry. 20:379-386

A number of derivatives of 2-methyl-3-(o-tolyl)-4(3H)-quinazolone bearing new substituents on the 2-methyl group have been synthesized. It was established that most substitutions at this position reduce or remove the CNS depressant activity of methaq

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f8f142dc9ab4276cde3317f6bd951f3
https://doi.org/10.1021/jm00213a013

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Synthesis and oral antiallergic activity of carboxylic acids derived from imidazo[2,1-c][1,4]benzoxazines, imidazo[1,2-a]quinolines, imidazo[1,2-a]quinoxalines, imidazo[1,2-a]quinoxalinones, pyrrolo[1,2-a]quinoxalinones, pyrrolo[2,3-a]quinoxalinones, and imidazo[2,1-b]benzothiazoles

Autor: I R, Ager, A C, Barnes, G W, Danswan, P W, Hairsine, D P, Kay, P D, Kennewell, S S, Matharu, P, Miller, P, Robson, D A, Rowlands

Publikováno v: Journal of Medicinal Chemistry. 31:1098-1115

4H-Imidazo[2,1-c][1,4]benzoxazine-2-carboxylic acid (3) was found to possess potent activity in the IgE-induced rat passive cutaneous anaphylaxis model which may be predictive of clinical antiallergic activity. Compared to disodium cromoglycate (DSCG

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7528f763f673d8039e17911274ab6180
https://doi.org/10.1021/jm00401a009

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19F nuclear magnetic resonance studies of aromatic compounds. Part II. The19F chemical shifts in meta- and para-substituted fluorobenzenes, and 4-substituted 3′- and 4′-fluoro-trans-stilbenes

Autor: Lawrence D. Phillips, T. J. Tewson, V. Wray, I. R. Ager

Publikováno v: J. Chem. Soc., Perkin Trans. 2. :1979-1987

A detailed study has been made of the effects of substituents, X, upon the shielding of 19F nuclei in series of meta and para-X-fluorobenzenes, 4-X-4′-fluoro-trans-stilbenes, and 3′-fluoro-4-X-trans-stilbenes. The correlation of substituent chemi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::be76778bff9ab5e6570c550a6add5b3f
https://doi.org/10.1039/p29720001979

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19F nuclear magnetic resonance studies of aromatic compounds. Part I. The effect of solvents on the chemical shift of fluorine nuclei in para-substituted fluorobenzenes, 4-substituted 4′-fluoro-trans-stilbenes, and 4-substituted 3′-fluoro-trans-stilbenes

Autor: L. Phillips, I. R. Ager

Publikováno v: J. Chem. Soc., Perkin Trans. 2. :1975-1979

Solvent effects upon 19F shielding in some aryl fluorides are examined. A criterion is established which, it is believed, enables solvents and reference to be chosen so that interactions other than those due to ‘reaction fields’ are minimised. Th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::211b87947da9a400754a21337d50b8cc
https://doi.org/10.1039/p29720001975

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Central nervous system activity of a novel class of annelated 1,4-benzodiazepines, aminomethylene-2,4-dihydro-1H-imidazo[1,2-a][1,4]benzodiazepin-1-ones

Autor: G. W. Danswan, I. R. Ager, Peter D. Kennewell, David Kay, John B. Taylor, D. R. Harrison

Publikováno v: Journal of medicinal chemistry. 20(8)

The synthesis and CNS activity of a noval class of annelated 1,4-benzodiazepines, the aminomethylene-2,4-dihydro-1H-imidazo[1,2-a][1,4]benzodiazepines, are described. An investigation of the structure--activity relationships in the series derived fro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::29ece156b6abdd41cc008660d09dbb54
https://pubmed.ncbi.nlm.nih.gov/19630

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