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26th March 2013 @ 04:57
Osm: OSM-S-1_to_OSM-S-10



OSM Series 1

Original Sources

Synthesis of TCMDC-123812 via acid chloride (PMY 10-1)

Synthesis of TCMDC-123812 via acid chloride (PMY 10-2)

Synthesis of TCMDC-123812 using DIC/DMAP (PMY 10-3)

Synthesis of TCMDC-123812 using T3P (PMY 10-4)

Synthesis of TCMDC-123812 via acid chloride (PMY 10-5)

Synthesis of TCMDC-123812 via acid chloride (PMY 10-6)

Synthesis of TCMDC-123812 via acid chloride (JRC 3-1)

Ester synthesis (AEW 5-1)

Ester synthesis (AEW 5-2)

Ester synthesis (AEW 5-3)

Ester Synthesis (AEW 5-4)

Biological Data

3D7, K1 and HEK293 - Avery - Second Analysis of First Set of Compounds (Avery)

3D7 - GSK - Re-evaluation of TCMDC-123794, TCMDC-123812 and others by GSK Tres Cantos

Late Stage Gametocyte - Late stage gametocyte testing of a sample set of GSK-Arylpyrrole Series

Metabolism - Metabolism and Solubility Results

In vivo - In vivo Plasmodium Berghei mouse trial of initial leads

Plasma - Human and Mouse Plasma Stability of OSM-S-5/PMY 10-6

Pharmacokinetics - Pharmacokinetics of OSM-S-5/TCMDC-123812/PMY 10-6

hERG - hERG Assay for OSM-S-35 (ZYH 3-1) and OSM-S-5 (PMY 10)

HIP-HOP - HIP-HOP mechanism of action studies from Corey Nislow's Lab

Ion Regulation Assay for OSM Series 1 and 3


PMY 10, JRC 3, AEW 5





2-amino-2-oxoethyl 1-(4-fluorophenyl)-2,5-dimethyl-1H-pyrrole-3-carboxylate


Compound: Novel at time of synthesis and time of writing. Commercial. CAS Registry Number: 733026-12-5. Chemspider page. ChEMBL page.


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