OpenSourceMalaria:Triazolopyrazine (TP) Series

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Contents

Open Source Malaria Series 4: The Triazolopyrazine (TP) Series

Introduction

Preamble

This series of compounds arises from industrial work that cannot be disclosed, followed by some hit-to-lead work funded directly by MMV which can. The series is based on a triazolopyrazine core. There is evidence that these compounds may be PfATP4 inhibitors. OSM started to look at this series following a decision by MMV to release their data into the public domain.

Current Aims

Further hit-to-lead work. Validate PfATP4 activity. Improve potency and drug likeness.

Prior Knowledge of the Series

Potency of Hits and Analogs

PfATP4 Activity

PCCBTAK-0083 : MMV669000

PCCBTAK-0127 : MMV669304

PCCBTAK-0156 : MMV669360

PCCBTAK-0160 : MMV669542

PCCBTAK-0194 : MMV669848

(Note the correlation: compound inactive in PfATP4 assay is the inactive analog)

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