Ledneczki, Istvan published the artcileDiscovery of novel steroidal histamine H3 receptor antagonists/inverse agonists, Application In Synthesis of 39546-32-2, the publication is Bioorganic & Medicinal Chemistry Letters (2017), 27(19), 4525-4530, database is CAplus and MEDLINE.
Emerging from an HTS campaign, novel steroid-based histamine H3 receptor antagonists were identified and characterized. Structural moieties of the hit compounds were combined to improve binding affinities which resulted in compound I as lead mol. During the lead optimization due to the versatile modifications of diamino steroid derivatives, several in vitro potent compounds with subnanomolar binding affinities to histamine H3 receptors were found. The unfavorable binding to rat muscarinic receptors was successfully reduced by tuning the basicity. Compound II showed significant in vivo activity in the rat dipsogenia model and could serve as a pharmacol. tool in the future.
Bioorganic & Medicinal Chemistry Letters published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Application In Synthesis of 39546-32-2.
Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem