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.Do, Ha T.; Li, Huiying; Chreifi, Georges; Poulos, Thomas L.; Silverman, Richard B. researched the compound: Boc-D-Prolinol( cas:83435-58-9 ).Application of 83435-58-9.They published the article 《Optimization of Blood-Brain Barrier Permeability with Potent and Selective Human Neuronal Nitric Oxide Synthase Inhibitors Having a 2-Aminopyridine Scaffold》 about this compound( cas:83435-58-9 ) in Journal of Medicinal Chemistry. Keywords: blood brain barrier permeability nitric oxide synthase inhibitor. We’ll tell you more about this compound (cas:83435-58-9).
Effective delivery of therapeutic drugs into the human brain is one of the most challenging tasks in central nervous system drug development because of the blood-brain barrier (BBB). To overcome the BBB, both passive permeability and efflux transporter liability of a compound must be addressed. Herein, we report our optimization related to BBB penetration of neuronal nitric oxide synthase (nNOS) inhibitors toward the development of new drugs for neurodegenerative diseases. Various approaches, including enhancing lipophilicity and rigidity of new inhibitors and modulating the pKa of amino groups, have been employed. In addition to determining inhibitor potency and selectivity, crystal structures of most newly designed compounds complexed to various nitric oxide synthase isoforms have been determined We have discovered a new analog (21), which exhibits not only excellent potency (Ki < 30 nM) in nNOS inhibition but also a significantly low P-glycoprotein and breast-cancer-resistant protein substrate liability as indicated by an efflux ratio of 0.8 in the Caco-2 bidirectional assay. Here is just a brief introduction to this compound(83435-58-9)Application of 83435-58-9, more information about the compound(Boc-D-Prolinol) is in the article, you can click the link below.
Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica