Monn, James A.’s team published research in Journal of Medicinal Chemistry in 58 | CAS: 59032-27-8

Journal of Medicinal Chemistry published new progress about 59032-27-8. 59032-27-8 belongs to triazoles, auxiliary class Triazoles, name is Sodium 1,2,3-triazole-5-thiolate, and the molecular formula is C2H2N3NaS, Application of Sodium 1,2,3-triazole-5-thiolate.

Monn, James A. published the artcileSynthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812223), a Highly Potent, Functionally Selective mGlu2 Receptor Agonist, Application of Sodium 1,2,3-triazole-5-thiolate, the publication is Journal of Medicinal Chemistry (2015), 58(18), 7526-7548, database is CAplus and MEDLINE.

Identification of orthosteric mGlu2/3 receptor agonists capable of discriminating between individual mGlu2 and mGlu3 subtypes has been highly challenging owing to the glutamate-site sequence homol. between these proteins. Herein we detail the preparation and characterization of a series of mols. related to (1S,2S,5R,6S)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylate (LY354740) bearing C4-thiotriazole substituents. On the basis of second messenger responses in cells expressing other recombinant human mGlu2/3 subtypes, a number of high potency and efficacy mGlu2 receptor agonists exhibiting low potency mGlu3 partial agonist/antagonist activity were identified. From this, (1R,2S,4R,5R,6R)-2-amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY2812223, I) was further characterized. Cocrystn. of I with the amino terminal domains of hmGlu2 and hmGlu3 combined with site-directed mutation studies has clarified the underlying mol. basis of this unique pharmacol. Evaluation of I in a rat model responsive to mGlu2 receptor activation coupled with a measure of central drug disposition provides evidence that this mol. engages and activates central mGlu2 receptors in vivo.

Journal of Medicinal Chemistry published new progress about 59032-27-8. 59032-27-8 belongs to triazoles, auxiliary class Triazoles, name is Sodium 1,2,3-triazole-5-thiolate, and the molecular formula is C2H2N3NaS, Application of Sodium 1,2,3-triazole-5-thiolate.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics