So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Li, Yuanyuan; Zhang, Shengnan; Wang, Rong; Cui, Menghan; Liu, Wei; Yang, Qing; Kuang, Chunxiang researched the compound: Piperidine-3-carboxylic acid( cas:498-95-3 ).COA of Formula: C6H11NO2.They published the article 《Synthesis of novel tryptanthrin derivatives as dual inhibitors of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase》 about this compound( cas:498-95-3 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: tryptanthrin derivative preparation dual inhibitor indoleamine dioxygenase tryptophan dioxygenase; IDO1 inhibitor; IDO1/TDO dual inhibitor; Novel tryptanthrin derivative; TDO inhibitor; Water solubility. We’ll tell you more about this compound (cas:498-95-3).
Indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) are promising drug development targets due to their implications in pathologies such as cancer and neurodegenerative diseases. The search for IDO1 inhibitor has been intensely pursued but there is a paucity of potent TDO and IDO1/TDO dual inhibitors. Natural product tryptanthrin (indolo[2,1-b]quinazoline-6,12-dione) has been confirmed to bear IDO1 and/or TDO inhibitory activities. Herein, twelve novel tryptanthrin derivatives were synthesized and evaluated for the IDO1 and TDO inhibitory potency. All of the compounds were found to be IDO1/TDO dual inhibitors, in particular, compound I [R = (E)-CH:CHCO2Et, (E)-CH:CHCO2H] bore IDO1 inhibitory activity similar to that of INCB024360; and compound I [R = CHO, (E)-CH:CHCO2H] had remarkable TDO inhibitory activity superior to that of the well-known TDO inhibitor LM10. This work enriches the collection of IDO1/TDO dual inhibitors and provides chem. mols. for potential development into drugs.
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Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics