OSDDMalaria:Arylpyrazole Series: Difference between revisions

Revision as of 20:55, 23 March 2012

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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:

CID372804. Commercially available.
CID11609708
CID3568222. Commercially available. Has been assayed for antimalarial activity AID504832, data submitted by David Fidock
CID4028326. Commercially available.
CID45589299. Limited commercial availability (AKos).
CID46188955
CID15338085

The core can be synthesised with apparent ease from ethylacetoacetate, DMF dimethyl acetal and phenylhydrazine.

@@ Line 19: / Line 19: @@
 * [http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3568222&loc=ec_rcs CID3568222]. Commercially available. Has been assayed for antimalarial activity [http://pubchem.ncbi.nlm.nih.gov/assay/assay.cgi?aid=504832 AID504832], data submitted by [http://www.microbiology.columbia.edu/faculty/fidock.html David Fidock]
 * [http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4028326&loc=ec_rcs CID4028326]. Commercially available.
-* [http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=45589299&loc=ec_rcs CID45589299]. Limited commercial availability.
+* [http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=45589299&loc=ec_rcs CID45589299]. Limited commercial availability (AKos).
 * [http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=46188955&loc=ec_rcs CID46188955]
 * [http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=15338085&loc=ec_rcs CID15338085]