Pyrimidine Derivatives. V. Structure-Activity Studies of Antihypertensive Quinazoline Derivatives Using the Adaptive Least-Squares Method

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概要

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• The structure-activity relationships of thirty 2-(4-cinnamoyl-1-piperazinyl)-6,7-dimethoxy-4-quinazolinamine derivatives for antihypertensive activity were analyzed by the adaptive least-squares (ALS) method. When the retention index (ΔRI) obtained from a C-18 reversed-phase column high-pressure liquid chromatography system was used as a lipophilic parameter, the discriminant equation L=-1.022ΔRI-2.560Σσ^<Ph>-1.966I^<Ph>(2-OR)+0.799 gave the best prediction, where L is the discriminant score, Σσ^<ph> is the sum of the Hammett substituent constants of the substituents on the phenyl group and I^<ph>(2-OR) is an indicator variable assigned a value of 1 for the presence of 2-alkoxy groups on the phenyl group. The effects of the lipophilicity and electronic character of substituents on the activity are discussed.

• 社団法人日本薬学会の論文
• 1983-08-25

著者

• 山田 俊一

  Faculty of Pharmaceutical Sciences, University of Tokyo

• 山田 俊一

  東京大学

• 山田 俊一

  Faculty Of Pharmaceutical Sciences University Of Tokyo

• 関谷 哲雄

  Research Laboratory, Mitsubishi Yuka Pharmaceutical Co., Ltd.

• 今田 悟史

  Research Laboratory, Mitsubishi Yuka Pharmaceutical Co., Ltd.

• 畑 俊輔

  Research Laboratory, Mitsubishi Yuka Pharmaceutical Co., Ltd.

• 関谷 哲雄

  Pharmaceuticals Laboratory, Research Center, Mitsubishi Kasei Corporation

• 畑 俊輔

  Research Laboratory Mitsubishi Yuka Pharmaceutical Co. Ltd.

• 関谷 哲雄

  Pharmaceuticals Laboratory Research Center Mitsubishi Kasei Corporation

• 今田 悟史

  Research Laboratory Mitsubishi Yuka Pharmaceutical Co. Ltd.

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