Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazoleIn 2010 ,《Selective angiotensin II AT2 receptor agonists with reduced CYP 450 inhibition》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Mahalingam, A. K.; Wan, Yiqian; Murugaiah, A. M. S.; Wallinder, Charlotta; Wu, Xiongyu; Plouffe, Bianca; Botros, Milad; Nyberg, Fred; Hallberg, Anders; Gallo-Payet, Nicole; Alterman, Mathias. The article conveys some information:
Structural alterations to the benzylic position of the first drug-like selective angiotensin II AT2 receptor agonist (1) have been performed, with the emphasis to reduce the CYP 450 inhibitory property of the initial structure. The imidazole moiety, responsible for the CYP 450 inhibitory effect in 1, was replaced with various heterocycles. In addition, the modes of attachment of the heterocycles, i.e., carbon vs. nitrogen attachment, and introduction of carbonyl functionalities to the benzylic position have been evaluated. In all the three series, AT2 receptor ligands with affinity in the lower nanomolar range were identified. None of the analogs, regardless of the substituents, exhibited any affinity for the AT1 receptor. Compounds with substantially reduced inhibition of the CYP 450 enzymes were obtained. Among them the compound 60 was found to induce neurite elongation in NG 108-15 cells and served as potent AT2 selective agonist.3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazole) was used in this study.
3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazole
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Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics