Structure-based approach to falcipain-2 inhibitors: synthesis and biological evaluation of 1, 6, 7-trisubstituted dihydroisoquinolines and isoquinolines

S Batra, YA Sabnis, PJ Rosenthal, MA Avery

文献索引：Batra, Sanjay; Sabnis, Yogesh A.; Rosenthal, Philip J.; Avery, Mitchell A. Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 10 p. 2293 - 2299

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被引用次数: 60

摘要

1, 4, 7-Trisubstituted isoquinolines were designed, synthesized and evaluated for their inhibition against Plasmodium falciparum cysteine protease falcipain-2. The 1- benzyloxyphenyl-dihydroisoquinoline and-isoquinoline derivatives were found to exhibit better activity against falcipain-2 than their corresponding 1-hydroxyphenyl or 1- methoxyphenyl analogues. The docking scores correlate with the IC50 values of ...