{"id":10704,"date":"2022-10-28T06:35:35","date_gmt":"2022-10-27T22:35:35","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10704"},"modified":"2022-10-28T06:35:35","modified_gmt":"2022-10-27T22:35:35","slug":"vekariya-rakesh-h-team-published-research-in-journal-of-medicinal-chemistry-in-2020-761446-44-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10704","title":{"rendered":"Vekariya, Rakesh H. team published research in Journal of Medicinal Chemistry in 2020 | 761446-44-0"},"content":{"rendered":"

Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. SDS of cas: 761446-44-0<\/a>.<\/p>\n

Vekariya, Rakesh H.;Lei, Wei;Ray, Abhisek;Saini, Surendra K.;Zhang, Sixue;Molnar, Gabriella;Barlow, Deborah;Karlage, Kelly L.;Bilsky, Edward J.;Houseknecht, Karen L.;Largent-Milnes, Tally M.;Streicher, John M.;Ananthan, Subramaniam research published \u300a Synthesis and Structure-Activity Relationships of 5′-Aryl-14-alkoxypyridomorphinans: Identification of a \u03bc Opioid Receptor Agonist\/\u03b4 Opioid Receptor Antagonist Ligand with Systemic Antinociceptive Activity and Diminished Opioid Side Effects\u300b, the research content is summarized as follows. We previously identified a pyridomorphinan (6, SRI-22138) possessing a 4-chlorophenyl substituent at the 5′-position on the pyridine and a 3-phenylpropoxy at the 14-position of the morphinan as a mixed \u03bc opioid receptor (MOR) agonist and \u03b4\/\u03ba opioid receptor (DOR\/KOR) antagonist with potent antinociceptive activity and diminished tolerance and dependence in rodents. Structural variations at the 5′- and 14-positions of this mol. gave insights into the structure-activity relationships for binding and functional activity. Subtle structural changes exerted significant influence, particularly on the ability of the compounds to function as agonists at the MOR. In vivo evaluation identified compound 20(I<\/strong>) (SRI-39067) as a MOR agonist\/DOR antagonist that produced systemically active potent antinociceptive activity in tail-flick assay in mice, with diminished tolerance, dependence\/withdrawal, reward liability, and respiratory depression vs. morphine. These results support the hypothesis that mixed MOR agonist\/DOR antagonist ligands may emerge as novel opioid analgesics with reduced side effects.<\/p>\n

SDS of cas: 761446-44-0<\/a>, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g\/mol. The purity is usually 95%., 761446-44-0.<\/p>\n

Referemce:
Pyrazole – Wikipedia<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

SDS of cas: 761446-44-0<\/a>, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g\/mol. The purity is usually 95%., 761446-44-0.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[733,131],"tags":[716],"class_list":["post-10704","post","type-post","status-publish","format-standard","hentry","category-761446-44-0","category-pyrazoles-derivatives","tag-m-w200-250"],"yoast_head":"\nVekariya, Rakesh H. team published research in Journal of Medicinal Chemistry in 2020 | 761446-44-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. 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