OSDDMalaria:GSK Arylpyrrole Series - Revision history

Matthew Todd: Added Asclepia Routes

2013-05-12T02:41:19Z

Added Asclepia Routes

←Older revision		Revision as of 02:41, 12 May 2013
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	[http://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20091112&DB=EPODOC&locale=en_EP&CC=WO&NR=2009137133A2&KC=A2&ND=5 WO 2009137133 (A2)] 5-Substituted-2-Imino-Thiazolidinone Compounds And Their Use As Inhibitors Of Bacterial Infection		[http://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20091112&DB=EPODOC&locale=en_EP&CC=WO&NR=2009137133A2&KC=A2&ND=5 WO 2009137133 (A2)] 5-Substituted-2-Imino-Thiazolidinone Compounds And Their Use As Inhibitors Of Bacterial Infection
	[[Image:WO2009137133A2.png\|thumb\|none\|Bacterial inhibitor]]		[[Image:WO2009137133A2.png\|thumb\|none\|Bacterial inhibitor]]
		+
		+	===Synthetic Routes to Analogs Proposed By Others===
		+
		+	The CRO Asclepia, via Frederik Doroose, contributed these synthetic routes to the project:
		+
		+	sD and sI compounds: [http://openwetware.org/images/4/41/SD_and_sI.doc Word file].
		+	sC, sD, sF, sJ, sI: [http://openwetware.org/images/e/ee/Ascelpia_Several.doc Word file]. Note prices are for S/M and should not be taken as a quote value.

	== Biology ==		== Biology ==

2012-06-06T04:29:46Z

Other known incidences of these molecules/this series

←Older revision		Revision as of 04:29, 6 June 2012
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	Misc papers to digest/assimilate regarding antimycobacterial/tuberculosis activity: [http://dx.doi.org10.1021/jm701560p Antimycobacterial 1,5-diphenyl pyrroles], [http://dx.doi.org/10.1016/j.ejmech.2009.06.005 10.1016/j.ejmech.2009.06.005], [http://dx.doi.org/10.1016/j.bmc.2010.09.006 10.1016/j.bmc.2010.09.006], [http://dx.doi.org/10.1002/cmdc.201000526 10.1002/cmdc.201000526]<br>		Misc papers to digest/assimilate regarding antimycobacterial/tuberculosis activity: [http://dx.doi.org10.1021/jm701560p Antimycobacterial 1,5-diphenyl pyrroles], [http://dx.doi.org/10.1016/j.ejmech.2009.06.005 10.1016/j.ejmech.2009.06.005], [http://dx.doi.org/10.1016/j.bmc.2010.09.006 10.1016/j.bmc.2010.09.006], [http://dx.doi.org/10.1002/cmdc.201000526 10.1002/cmdc.201000526]<br>
		+
		+	''' ChEMBL-NTD '''
		+
		+	Searches on [https://www.ebi.ac.uk/chemblntd/compound/structure_home ChEMBL-NTD] reveal:
		+	* 19 iminothiazolidinones
		+	* 55 2,5-dialkylpyrroles
		+	* 58 rhodanines. These do not contain any biological data, presumably omitted due to promiscuity/PAINS issues.

	'''Scifinder Search:'''		'''Scifinder Search:'''

2012-05-21T23:43:16Z

In vivo

←Older revision		Revision as of 23:43, 21 May 2012
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	==== '''''In vivo''''' ====		==== '''''In vivo''''' ====

-	TCMDC-123812, TCMDC-123794 and near neighbour ZYH 3-1 have been [http://www.thesynapticleap.org/node/395 submitted] for study oral ''in vivo'' mouse model. Unfortunately it was found that the compounds possess zero oral efficacy (Results available [http://malaria.ourexperiment.org/uri/ed here] in this initial trial.	+	TCMDC-123812, TCMDC-123794 and near neighbour ZYH 3-1 have been [http://www.thesynapticleap.org/node/395 submitted] for study oral ''in vivo'' mouse model. Unfortunately it was found that the compounds possess zero oral efficacy (Results available [http://malaria.ourexperiment.org/uri/ed here]) in this initial trial.

	=== Mode of action ===		=== Mode of action ===

2012-05-21T23:42:57Z

In vivo

←Older revision		Revision as of 23:42, 21 May 2012
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	==== '''''In vivo''''' ====		==== '''''In vivo''''' ====

-	TCMDC-123812, TCMDC-123794 and near neighbour ZYH 3-1 have been [http://www.thesynapticleap.org/node/395 submitted] for study oral ''in vivo'' mouse model.	+	TCMDC-123812, TCMDC-123794 and near neighbour ZYH 3-1 have been [http://www.thesynapticleap.org/node/395 submitted] for study oral ''in vivo'' mouse model. Unfortunately it was found that the compounds possess zero oral efficacy (Results available [http://malaria.ourexperiment.org/uri/ed here] in this initial trial.

	=== Mode of action ===		=== Mode of action ===

2012-05-08T04:29:41Z

The Arylpyrrole Series

←Older revision		Revision as of 04:29, 8 May 2012
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	== The Arylpyrrole Series ==		== The Arylpyrrole Series ==

-	This page contains a summary of all the data associated with this open source project. A more ~~human-readable summary can be found~~ [[OSDDMalaria:GSK_Arylpyrrole_Series:Story_so_far\|~~here~~]].	+	This page contains a summary of all the data associated with this open source project. A more [[OSDDMalaria:GSK_Arylpyrrole_Series:Story_so_far\|'''human-readable summary''']] is available.

	These compounds are currently under study by the Todd lab at the University of Sydney and the Medicines for Malaria Venture, Geneva. As an open source project, anyone may participate:<br>		These compounds are currently under study by the Todd lab at the University of Sydney and the Medicines for Malaria Venture, Geneva. As an open source project, anyone may participate:<br>

2012-05-02T01:18:45Z

added link to human summary

←Older revision		Revision as of 01:18, 2 May 2012
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	== The Arylpyrrole Series ==		== The Arylpyrrole Series ==
		+
		+	This page contains a summary of all the data associated with this open source project. A more human-readable summary can be found [[OSDDMalaria:GSK_Arylpyrrole_Series:Story_so_far\|here]].

	These compounds are currently under study by the Todd lab at the University of Sydney and the Medicines for Malaria Venture, Geneva. As an open source project, anyone may participate:<br>		These compounds are currently under study by the Todd lab at the University of Sydney and the Medicines for Malaria Venture, Geneva. As an open source project, anyone may participate:<br>

2012-04-16T00:19:05Z

The Arylpyrrole Series

←Older revision		Revision as of 00:19, 16 April 2012
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	Compounds are [http://www.thesynapticleap.org/node/345 commercially-available]<br>		Compounds are [http://www.thesynapticleap.org/node/345 commercially-available]<br>
-	Series was [http://pubs.acs.org/doi/abs/10.1021/ml200135p listed as one of the most promising leads] from TCAMS set (though lacking aryl F)<br>	+
		+	Series was released in a [http://www.nature.com/nature/journal/v465/n7296/full/nature09107.html large dataset] by GSK and later [http://pubs.acs.org/doi/abs/10.1021/ml200135p listed as one of the most promising leads] from TCAMS set (though lacking aryl F)<br>

	==== TCMDC 123812 ====		==== TCMDC 123812 ====

2012-04-11T00:13:34Z

In vitro

←Older revision		Revision as of 00:13, 11 April 2012
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	=== Malaria Assays ===		=== Malaria Assays ===
	==== '''''In vitro''''' ====		==== '''''In vitro''''' ====
		+	Current tested compounds and their biological activities are summarised on a Google [http://bit.ly/OSDDcompounds spreadsheet]
		+
		+	The results are collected on [http://malaria.ourexperiment.org/biological_data malaria.ourexperiment.org].
		+
	==== '''''In vivo''''' ====		==== '''''In vivo''''' ====

2012-04-11T00:06:26Z

In vivo: link

←Older revision		Revision as of 00:06, 11 April 2012
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	==== '''''In vivo''''' ====		==== '''''In vivo''''' ====

-	TCMDC-123812, TCMDC-123794 and near neighbour ZYH 3-1 have been submitted for study oral ''in vivo'' mouse model.	+	TCMDC-123812, TCMDC-123794 and near neighbour ZYH 3-1 have been [http://www.thesynapticleap.org/node/395 submitted] for study oral ''in vivo'' mouse model.

	=== Mode of action ===		=== Mode of action ===

2012-04-11T00:05:48Z

In vivo

←Older revision		Revision as of 00:05, 11 April 2012
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	==== '''''In vivo''''' ====		==== '''''In vivo''''' ====

		+	TCMDC-123812, TCMDC-123794 and near neighbour ZYH 3-1 have been submitted for study oral ''in vivo'' mouse model.

	=== Mode of action ===		=== Mode of action ===