Part C Myeloperoxidase (MPO) is an enzyme that, when overactive, has been linked to chronic inflammatory diseases, ather

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Part C Myeloperoxidase Mpo Is An Enzyme That When Overactive Has Been Linked To Chronic Inflammatory Diseases Ather 1 (194.67 KiB) Viewed 24 times

Part C Myeloperoxidase (MPO) is an enzyme that, when overactive, has been linked to chronic inflammatory diseases, atherosclerosis and acute cardiovascular events. The aminotriazolopyrimidine [1] is a reversible MPO inhibitor that is a good lead compound. However, it is not sufficiently active or selective to be clinically used. Data from a recent structure activity relationship (SAR) study of aminotriazolopyrimidine molecules and their MPO inhibition are provided in the table below. i) ii) on H₂N Compound 1 2a 2b 2c 2d 2e [1] X OCH₂ N(CH3)CH2 CH2CH2 CH₂ CH₂ OCH2 H₂N Y N N N N CH CH [2] IC 50 (μm) 0.11 >40 7.5 0.11 0.025 0.050 From the structure activity-relationship (SAR) data of compounds 1 and 2a-2e, summarise what appear to be the most important features for MPO inhibitory activity. Provide reasons as to why these features may be important, using structures to assist you. (3 marks) Provide THREE structures that are logical extensions of the above SAR study that would allow you to understand these SAR data better. Justify your choice of structures. (3 marks)