1zsn: Difference between revisions

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~~'''~~Synthesis, Biological Activity, and X-Ray Crystal Structural Analysis of Diaryl Ether Inhibitors of Malarial Enoyl ACP Reductase. Part 1:4'-Substituted Triclosan Derivatives~~'''~~

===Synthesis, Biological Activity, and X-Ray Crystal Structural Analysis of Diaryl Ether Inhibitors of Malarial Enoyl ACP Reductase. Part 1:4'-Substituted Triclosan Derivatives===

~~==Overview==~~

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~~A structure-based approach has been taken~~ to ~~develop 4'-substituted analogs of triclosan that target~~ the ~~key malarial enzyme Plasmodium falciparum enoyl acyl carrier protein reductase~~ (~~PfENR)~~. ~~Many of these compounds exhibit nanomolar potency against purified PfENR enzyme and modest (2-10microM~~) ~~potency against in vitro cultures of drug-resistant and drug-sensitive strains of~~ the P. ~~falciparum parasite. X~~-~~ray crystal structures of nitro 29, aniline 30, methylamide 37, and urea 46 demonstrate the presence of hydrogen~~-~~bonding interactions with residues in the active site and point to future rounds of optimization to improve compound potency against purified enzyme and intracellular parasites.~~

The line below this paragraph, {{ABSTRACT_PUBMED_16198563}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 16198563 is the PubMed ID number.

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==About this Structure==

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[[Category: Yu, M.]]

[[Category: Oxidoreductase]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sat May 3 18~~:01:24 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 07:36:17 2008''

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-[[Image:1zsn.gif|left|200px]]
+{{Seed}}
+[[Image:1zsn.png|left|200px]]
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 {{STRUCTURE_1zsn|  PDB=1zsn  |  SCENE=  }}
-'''Synthesis, Biological Activity, and X-Ray Crystal Structural Analysis of Diaryl Ether Inhibitors of Malarial Enoyl ACP Reductase. Part 1:4'-Substituted Triclosan Derivatives'''
+===Synthesis, Biological Activity, and X-Ray Crystal Structural Analysis of Diaryl Ether Inhibitors of Malarial Enoyl ACP Reductase. Part 1:4'-Substituted Triclosan Derivatives===
-==Overview==
+<!--
-A structure-based approach has been taken to develop 4'-substituted analogs of triclosan that target the key malarial enzyme Plasmodium falciparum enoyl acyl carrier protein reductase (PfENR). Many of these compounds exhibit nanomolar potency against purified PfENR enzyme and modest (2-10microM) potency against in vitro cultures of drug-resistant and drug-sensitive strains of the P. falciparum parasite. X-ray crystal structures of nitro 29, aniline 30, methylamide 37, and urea 46 demonstrate the presence of hydrogen-bonding interactions with residues in the active site and point to future rounds of optimization to improve compound potency against purified enzyme and intracellular parasites.
+The line below this paragraph, {{ABSTRACT_PUBMED_16198563}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 16198563 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_16198563}}
 ==About this Structure==
@@ Line 35: / Line 39: @@
 [[Category: Yu, M.]]
 [[Category: Oxidoreductase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 18:01:24 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 07:36:17 2008''