Archives of Pharmacal Research
- Volume 13 Issue 1
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- Pages.82-96
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- 1990
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- 0253-6269(pISSN)
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- 1976-3786(eISSN)
Quantitative Structure-Activity Relationships in MAO-Inhibitor~' 2-Phenylcyclopropylarnines: Insights into the Topography of MAO-A and MAO-B
- Kang, Gun-Il (College of Pharmacy, Sookmyung Womens University) ;
- Hong, Suk-Kil (College of Pharmacy, Sookmyung Womens University)
- Published : 1990.03.01
Abstract
Ten (E)-and (Z)-isomers of 2-phenylcyclopropylamine (PCA), 1-Me PCA, 2-Me-PCA, N-Me-PCA, and N, N-diMe PCA and fifteen o-. m-, p- isomers of (E) PCA with substituents of Me, Cl, F, OMe, OH were synthesized in this laboratory and tested for the inhibition of rat brain mitochondrial MAO-A and MAO-B. The effects of substituents, their positions, and stereochemistry on the inhibition were assessed for the compounds with substituents at cyclopropyl and amino groups and QSAR analyses were performed using the potency data of ring-substituted compounds. The best correlated QSAR equations are as follows : pI