Structure-Activity Relationships of Alkylxanthine Inhibitors of Phosphodiesterase IV Isoenzyme
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概要
- 論文の詳細を見る
The structural and electronic properties of seventeen alkylxanthine derivatives were calculated using the MO program PM3 to elucidate the key features related to their inhibitory activity on phosphodiesterase (PDE) IV isoenzyme. Except for 7-alkylxanthine derivatives, a good correlation could be established between the distance between the tops of the two alkyl groups at the N^1 and N^3 positions of the xanthine skeleton (molecular length) and the PDE IV inhibitory activity (r=0.973,n=13). The same inhibitory activity could also be significantly correlated with the following electronic parameters of alkylxanthines : HOMO energy (r=0.850), absolute hardness (r=-0.806), and absolute electronegativity (r=-0.825). These results suggest that the electronic properties are partly responsible for PDE IV inhibition as far as the effects of structural properties associated with molecular length are concerned. Alkylxanthines may also act as electron donors in the charge-transfer interaction with the active sites on PDE IV isoenzyme.
- 公益社団法人日本薬学会の論文
- 1998-04-15
著者
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YAMAMOTO Kenji
Department of Medical Ecology and Informatics, Research Institute, International Medical Center of J
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Sawanishi Hiroyuki
Department Of Medicinal Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University
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Sawanishi H
Hokuriku Univ. Kanazawa
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Yokogawa Koichi
Department Of Clinical Pharmaceutics Graduate School Of Pharmaceutical Sciences Kanazawa University
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Yokogawa Koichi
Department Of Hospital Pharmacy Kanazawa University Hospital
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Miyamoto Ken-ichi
Department Of Hospital Pharmacy School Of Medicine Kanazawa University
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Miyaamoto Ken-ichi
Department Of Medical Informatics Graduate School Of Medical Science Kanazawa University
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Miyamoto Ken-ichi
Graduate School Of Natural Science And Technology Kanazawa University
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Sawanishi Hiroyuki
Faculty Of Pharmaceutical Sciences Hokuriku University
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Yamamoto K
Faculty Of Pharmaceutical Sciences Josai University
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Miyamoto K
Kanazawa Univ. Hospital Ishikawa Jpn
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Sawanishi H
Department Of Medicinal Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University
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Yamamoto Kenji
Department Of Cardiovascular Surgery Kanagawa Cardiovascular And Respiratory Center
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