Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, Non-U.S. Gov’t, Nuclear Medicine and Biology called Synthesis and pharmacological evaluation of a new series of radiolabeled ligands for 5-HT7 receptor PET neuroimaging, Author is Colomb, Julie; Becker, Guillaume; Forcellini, Elsa; Meyer, Sandra; Buisson, Lauriane; Zimmer, Luc; Billard, Thierry, which mentions a compound: 83435-58-9, SMILESS is O=C(N1[C@@H](CO)CCC1)OC(C)(C)C, Molecular C10H19NO3, Synthetic Route of C10H19NO3.
The brain serotonin-7 receptor (5-HT7) is the most recently discovered serotonin receptor. It is targeted by several drug-candidates in psychopharmacol. and neuropharmacol. In these fields, positron emission tomog. (PET) is a mol. imaging modality offering great promise for accelerating the development process from preclin. discovery to clin. phases. We recently described fluorinated 5-HT7 radioligands, inspired by the structure of SB269970, the prototypical 5-HT7 antagonist. Although these results were promising, it appeared that the radiotracer-candidates suffered, among other drawbacks, from too low a 5-HT7 receptor affinity. In the present study, seven structural analogs of SB269970 were synthesized using design strategies aiming to improve their radiopharmacol. properties. Their 5-HT7 binding properties were investigated by cellular functional assay. The nitro-precursors of the analogs were radiolabeled by [18 F-]nucleophilic substitution, and in vitro autoradiog. was performed in rat brain, followed by in vivo microPET. The chem. and radiochem. purity of the fluorine radiotracers was > 99% with specific activity in the 40-129 GBq/μmol range. The seven derivatives presented heterogeneous binding affinities toward 5-HT7 and 5-HT1A receptors. While [18 F]2F3P3 had promising characteristics in vitro, it showed poor brain penetration in vivo, partially reversed after pharmacol. inhibition of P-glycoprotein. These results indicated that, while chem. modification of these series improved several radiotracer-candidates in terms of 5-HT7 receptor affinity and specificity toward 5-HT1A receptors, other physicochem. modulations would be required in order to increase brain penetration.
This literature about this compound(83435-58-9)Synthetic Route of C10H19NO3has given us a lot of inspiration, and I hope that the research on this compound(Boc-D-Prolinol) can be further advanced. Maybe we can get more compounds in a similar way.
Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica