Download Kirk-Othmer Encyclopedia of Chemical Technology Vol 16 by Raymond E Kirk; Donald F Othmer; Martin Grayson; David PDF
By Raymond E Kirk; Donald F Othmer; Martin Grayson; David Eckroth; et al
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Example text
Yet, substituents in the phenyl rings clearly have such an effect. The following explanations have been put forward. a. Folding. Rinneberg (124) suggested in 1955 that the relatively strong UV absorptions of diphenhydramines and related structures could be ascribed to the folding of the molecule chain, in which case the nitrogen with its substituents, if any, would approach one of the phenyl rings—from above, as it were. Mutual influence of the chromophoric phenyl system a n d the nitrogen auxochrome could accompany this folding, thus explaining the relatively strong U V absorption.
0 0 2 E e + 0 . 4 7 5 £ / - 3 . 223 (11) 54 Α. F. HARMS et al. The overall results of the in vivo work were so much in agreement with the in vitro results that it was thought useful to combine the two studies. The regression equation of the combination is shown in Eq. (12). m p 2 p log BR = 0 . 3 5 8 £ s ° ' - 0 . 2 1 6 ( £ s ) - 0 . 1 8 9 £ s + 0 . 232 n (12) Although Eqs. (10), (11), and (12) are of a good quality [the only objection is p the extreme smallness of the regression coefficient of £ s in Eq.
Evidently, not only the inductive effects, but also the bulkiness of the substituents are important for the activities studied. E. CHANGES IN THE OXYALKYLAMINE SIDE C H A I N Although less systematically than changes in the benzhydryl moiety, changes in the side chain have also been investigated. In this section the effects of such changes on antihistamine and anticholinergic activity are discussed. 1. Thio Ethers After a few thio ethers had been studied by Harms (55), Timmerman et al. (139) investigated a longer series.