Structure-activity relationships of novel anti-malarial agents.: Part 7:: N-(3-benzoyl-4-tolylacetylaminophenyl)-3-(5-aryl-2-uryl)acrylic acid amides with polar moieties
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作者:
Wiesner, J
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机构:Univ Munich, Zentrum Pharmaforsch, Dept Pharm, D-81377 Munich, Germany
Wiesner, J
Mitsch, A
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机构:Univ Munich, Zentrum Pharmaforsch, Dept Pharm, D-81377 Munich, Germany
Mitsch, A
Jomaa, H
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机构:Univ Munich, Zentrum Pharmaforsch, Dept Pharm, D-81377 Munich, Germany
Jomaa, H
Schlitzer, M
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机构:Univ Munich, Zentrum Pharmaforsch, Dept Pharm, D-81377 Munich, Germany
Schlitzer, M
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[1] Univ Munich, Zentrum Pharmaforsch, Dept Pharm, D-81377 Munich, Germany
In a previous report, we have provided evidence that novel anti-malarial compounds based on 2,5-diaminobenzophenone farnesyltransferase inhibitors might benefit from the presence of a polar moiety at the para position of the terminal phenyl of the arylfurylacryloyl partial structure. Here, we demonstrate that different moieties with hydrogen bond acceptor properties lead to equipotent or even improved anti-malarial activity in comparison to the nitro group described before. (C) 2003 Elsevier Science Ltd. All rights reserved.
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Shin, SS
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Noh, MS
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Noh, MS
;
Byun, YJ
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Byun, YJ
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Choi, JK
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Choi, JK
;
Kim, JY
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Kim, JY
;
Lim, KM
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Lim, KM
;
Ha, JY
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Ha, JY
;
Kim, JK
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Kim, JK
;
Lee, CH
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Lee, CH
;
Chung, S
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Shin, SS
;
Noh, MS
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Noh, MS
;
Byun, YJ
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Byun, YJ
;
Choi, JK
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机构:
Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Choi, JK
;
Kim, JY
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机构:
Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Kim, JY
;
Lim, KM
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Lim, KM
;
Ha, JY
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Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Ha, JY
;
Kim, JK
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机构:
Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Kim, JK
;
Lee, CH
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机构:
Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea
Lee, CH
;
Chung, S
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机构:
Pacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South KoreaPacific Corp, Ctr Res & Dev, Drug Discovery, Yongin Si 449900, Kyounggi Do, South Korea