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Solution conformations of antihistamines

✍ Scribed by Norman S. Ham

Publisher: John Wiley and Sons
Year: 1971
Tongue: English
Weight: 238 KB
Volume: 60
Category: Article
ISSN: 0022-3549
DOI: 10.1002/jps.2600601152

No coin nor oath required. For personal study only.

✦ Synopsis

Keyphrases 0 Antihistamines-activity-conforrnation relationships 0 Conformation, analysis-related to antihistamine activity Stereospecificity-antihistamine activity-trans-conformation relationships 0 PMR spectroscopy-structure, conformation, antihistamines Sir:

On the basis of similarities in the crystal structures of histamine and the antihistamine methapyrilene hydrochloride' (I), it was concluded that for XCHzCHzN+-HMez compounds to show antihistaminic activity, it is essential that N+ and X be in a trans-conformation (1).

Many antihistamines have this general formula, in which the substituent X may be >N, -0, or saturated C, with a variety of groups attached. + X-CH2-CH2-NHMee thenyl \ /N-I : X = a-pyridyl

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