Reference of Methyl 5-(chlorosulfonyl)-1-methyl-1H-pyrrole-2-carboxylateOn October 31, 2020 ,《From orexin receptor agonist YNT-185 to novel antagonists with drug-like properties for the treatment of insomnia》 appeared in Bioorganic Chemistry. The author of the article were Mezeiova, Eva; Janockova, Jana; Konecny, Jan; Kobrlova, Tereza; Benkova, Marketa; Dolezal, Rafael; Prchal, Lukas; Karasova-Zdarova, Jana; Soukup, Ondrej; Korabecny, Jan. The article conveys some information:
YNT-185 is the first known small mol. acting as orexin 2 receptor (OX2R) agonist with implication to narcolepsy treatment, served as a template scaffold in generating a small set of seven compounds with predictive affinity to OX2R. The design of the new small mols. was driven mostly by improving physicochem. properties of the parent drug YNT-185 in parallel with in silico studies, later suggesting their favorable binding modes within the active site of OX2R. We obtained seven new potential OX2R binders that were evaluated in vitro for their CNS availability, cytotoxicity, and behavior pattern on OX2R. Out of them, I emerged as the most potent modulator of OX2R, which, contrary to YNT-185, displayed inverse mode of action, i.e. antagonist profile. I was also submitted to an in vivo experiment revealing its ability to permeate through BBB into the brain with a short half-life. In the experimental materials used by the author, we found Methyl 5-(chlorosulfonyl)-1-methyl-1H-pyrrole-2-carboxylate(cas: 306936-53-8Reference of Methyl 5-(chlorosulfonyl)-1-methyl-1H-pyrrole-2-carboxylate)
Methyl 5-(chlorosulfonyl)-1-methyl-1H-pyrrole-2-carboxylate(cas: 306936-53-8) belongs to pyrroles. Pyrroles are components of more complex macrocycles, including the porphyrinogens and products derived therefrom, including porphyrins of heme, the chlorins, bacteriochlorins, and chlorophylls. Porphobilinogen, a trisubstituted pyrrole, is the biosynthetic precursor to many natural products such as heme.Reference of Methyl 5-(chlorosulfonyl)-1-methyl-1H-pyrrole-2-carboxylate
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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics