This month, Momelotinib (OJJAARA©) received FDA approval as a medicine for treating intermediate or high-risk myelofibrosis in adults with anemia. It acts as a selective inhibitor of Janus Kinase 1 and 2 (JAK1/JAK2), which contribute to the signaling pathways of several cytokines and growth factors that are important for hematopoiesis and immune function.

Momelotinib contains a morpholine moiety, which is popular in drug molecules but can exhibit some metabolic issues leading to undesirable adverse effects. The bioisosteric replacement of morpholine may profitably enhance the stability of both existing and prospective drugs.

 

We offer a set of morpholine bioisosteres, which could be a promising strategy in designing new drug candidates!

 

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