OSDDMalaria:Arylpyrazole Series

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=== Synthesis ===
=== Synthesis ===
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The core can be synthesised with [http://dx.doi.org/10.1002/jhet.5570240634 apparent ease] from ethylacetoacetate, DMF dimethyl acetal and phenylhydrazine.
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The core can be synthesised with [http://dx.doi.org/10.1002/jhet.5570240634 apparent ease] from ethylacetoacetate, DMF dimethyl acetal and phenylhydrazine. ELN entries [http://malaria.ourexperiment.org/uri/c0 PMY 43-1]  [http://malaria.ourexperiment.org/uri/c4 PMY 44-1] for the core synthesis and hydrolysis respectively.  
[[Image:PMY43-1.png|thumb|center|450px|Synthesis of pyrazole core]]
[[Image:PMY43-1.png|thumb|center|450px|Synthesis of pyrazole core]]

Revision as of 01:01, 5 April 2012

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Aryl Pyrazole Sub-series

The OSDDMalaria pyrazole series is derived from the OSDDMalaria GSK arylpyrrole set.


ChEMBL-NTD TCAMS data set has 89 hits with aryl-pyrazole core; 18 hits with an 5-alkyl aryl pyrazole core; 14 with activity below 500 nanomolar:


Other compounds of interest from PubChem:

Synthesis

The core can be synthesised with apparent ease from ethylacetoacetate, DMF dimethyl acetal and phenylhydrazine. ELN entries PMY 43-1 PMY 44-1 for the core synthesis and hydrolysis respectively.

Synthesis of pyrazole core
Synthesis of pyrazole core
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