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Title

Quantitative structure-affinity relationships of dopamine D2 receptor antagonists - a comparison between orthopramides and 6-methoxysalicylamides

Authors
de Paulis, Tomas
el Tayar, Nabil
Testa, Bernard
Van de Waterbeemd, Hans
Published in Helvetica Chimica Acta. 1991, vol. 74, no. 2, p. 241-254
Abstract A large series of orthopramides (= 2-methoxybenzamides), 6-methoxysalicylamides, and 2,6-dimethoxybenzamides were examined for their affinity to the dopamine D2 receptor. The binding data were correlated with physicochemical parameters and C-13-NMR chemical shifts using the cross-validated partial least-squares method and multiple linear regression analysis. The results quantitate the influence of electronic factors and lipophilicity to D2 receptor binding. They also show that the N-[(1-ethylpyrrolidin-2-yl)methyl] and N-(1-benzylpiperidin-4-yl) side-chains affect the mode of binding of these compounds
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DE PAULIS, Tomas et al. Quantitative structure-affinity relationships of dopamine D2 receptor antagonists - a comparison between orthopramides and 6-methoxysalicylamides. In: Helvetica Chimica Acta, 1991, vol. 74, n° 2, p. 241-254. https://archive-ouverte.unige.ch/unige:9923

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Deposited on : 2010-08-06

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