- Preparation and pharmacologic activity of amido- derivatives of 3-methyl-3,4-dihydro benzo- and pyrido-1,2,4-triazin-3-acetic acids
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Thirteen amidoderivatives of 3-methyl-3,4-dihydro-6-R-benzo-1,2,4-triazin-3-yl-acetic acids and of 3-methyl-3,4-dihydro-pyrido [3,2-e]/[3,4-e]-1,2,4-triazin- 3-yl-acetic acids were prepared and submitted to a wide pharmacological screening. The dihydrobenzotriazine and dihydropyridotriazine moieties were endowed with a wide pharmacogenic capacity; in fact, several compounds exhibited high antiinflammatory [(I c), (I d), (II d), (V f), (VI f)], diuretic [(I f), (I g), (I h)] and antihypertensive activities [(I d), (III d)], as well as minor effects on the C.N.S.
- Boido,Novelli,Savelli,Sparatore,Russo,Filippelli,Susanna,Marmo
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p. 279 - 301
(2007/10/02)
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- Competitive Cyclisations of Singlet and Triplet Nitrenes. Part 8. The 1-(2-Nitrenophenyl)pyrazoles and Related Systems
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The title nitrenes, derived by nitro-group deoxygenation with triethyl phosphite or by thermolysis or photolysis of the corresponding azide, have been studied.The effect of substituents (Cl, Br, OMe, NMe2, Me, CF3, and NO2) both meta and para to the nitrene has been examined as a determinant of the preferred mode of cyclisation to either a pyrazolobenzotriazole or a pyrazoloquinoxaline.Similarly, the role of solvents, sensitisers, and quenchers has been studied.Routes to the isomeric 1- and 2-(2-nitrophenyl)-4,5,6,7-tetrahydroindazoles have been defined and the literature corrected by studing the nitrene-mediated cyclisation of these products.The chemistry of the analogous 1-(2-carbenophenyl)- and the 1-(2-nitrenosulphonylphenyl)-3,5-dimethylpyrazoles has also been examined, the former giving 2-(3,5-dimethylpyrazol-1-yl)-benzaldazine and -benzyl alcohol while the latter gave products of intramolecular nitrene attack (a pyrazolobenzothiatriazine) and intermolecular reaction.Rationalisations for all the reaction pathways have been advanced.
- Lindley, John M.,McRobbie, Ian M.,Meth-Cohn, Otto,Suschitzky, Hans
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p. 982 - 994
(2007/10/02)
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