{"id":9930,"date":"2022-09-21T02:24:10","date_gmt":"2022-09-20T18:24:10","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=9930"},"modified":"2022-09-21T02:24:10","modified_gmt":"2022-09-20T18:24:10","slug":"li-jing-team-published-research-on-european-journal-of-medicinal-chemistry-in-2017-37622-90-5","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=9930","title":{"rendered":"Li, Jing team published research on European Journal of Medicinal Chemistry in 2017 | 37622-90-5"},"content":{"rendered":"

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 37622-90-5, formula is C6H8N2O2, Name is Ethyl 4-pyrazolecarboxylate. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 \u00b0C).Pyrazole used as a ligand to prepare organometallic compounds. Recommanded Product: Ethyl 4-pyrazolecarboxylate<\/a>.<\/p>\n

Li, Jing;Wu, Fangping;Liu, Xingguo;Zou, Yake;Chen, Huixiong;Li, Zheng;Zhang, Lei research published \u300a Synthesis and bioevaluation of 1-phenyl-pyrazole-4-carboxylic acid derivatives as potent xanthine oxidoreductase inhibitors\u300b, the research content is summarized as follows. A diverse library of 1-phenyl-pyrazole-4-carboxylic acid derivatives I<\/strong> [R = OCH2<\/sub>CH3<\/sub>, OCH2<\/sub>CH(CH3<\/sub>)2<\/sub>, N(CH3<\/sub>)2<\/sub>, pyrrolidin-1-yl, etc.; R1<\/sup> = H, CH3<\/sub>, CF3<\/sub>; R2<\/sup> = CN, NO2<\/sub>] was synthesized and evaluated for their inhibitory potency against xanthine oxidoreductase (XOR) in vitro and vivo, and the structure-activity relationship (SAR) analyses were also presented. Approx. half of the target compounds exhibited the inhibitory potency for XOR at the nanomolar level. Compounds I<\/strong> [R = N(CH3<\/sub>)CH2<\/sub>CH(CH3<\/sub>)2<\/sub>, pyrrolidin-1-yl, piperidin-1-yl; R1<\/sup> = H; R2<\/sup> = CN] emerged as the most potent xanthine oxidoreductase inhibitors with IC50<\/sub> values of 5.7, 5.7 and 4.2 nM, resp., in comparison to febuxostat (IC50<\/sub> of 5.4 nM). Steady-state kinetics measurements indicated that I<\/strong> [R = N(CH3<\/sub>)CH2<\/sub>CH(CH3<\/sub>)2<\/sub>, R1<\/sup> = H, R2<\/sup> = CN] is a mixed-type inhibitor. A computer mol. docking study of I<\/strong> [R = N(CH3<\/sub>)CH2<\/sub>CH(CH3<\/sub>)2<\/sub>, R1<\/sup> = H, R2<\/sup> = CN] bound to XOR was performed to gain an insight into its bind mode and SAR for the series. A potassium oxonate-hypoxanthine-induced hyperuricemia model in mice was chosen to further confirm the hypouricemic effects of I<\/strong> [R = N(CH3<\/sub>)CH2<\/sub>CH(CH3<\/sub>)2<\/sub>, piperidin-1-yl; R1<\/sup> = H; R2<\/sup> = CN] and the results demonstrated that I<\/strong> [R = N(CH3<\/sub>)CH2<\/sub>CH(CH3<\/sub>)2<\/sub>, R1<\/sup> = H, R2<\/sup> = CN] exhibits similar hypouricemic potency to febuxostat.<\/p>\n

37622-90-5, Ethyl 4-pyrazolecarboxylate, also known as Ethyl pyrazole-4-carboxylate, is a useful research compound. Its molecular formula is C6H8N2O2 and its molecular weight is 140.14 g\/mol. The purity is usually 95%.<\/p>\n

Ethyl pyrazole-4-carboxylate is a low yield, transition metal salt that is used in the synthesis of pyrazoles. It can be synthesized by the reaction of sodium ethoxide with ethyl chloroformate and a Grignard reagent. Sodium ethoxide is added to a suspension of sodium chloride and dried ethyl chloroformate, followed by addition of magnesium turnings. The mixture is refluxed for one hour, cooled, and filtered to give crystals. Ethyl pyrazole-4-carboxylate is used in the preparation of ethyl esters from aliphatic alcohols by reacting with boron trichloride or phosphorus pentachloride. It participates in certain chemical reactions as a byproduct and can damage equipment during chemical reactions. The yield of this compound can be increased by using an excess amount of Grignard reagent or adding hexamethylenetetramine to the reaction mixture, Recommanded Product: Ethyl 4-pyrazolecarboxylate<\/a><\/p>\n

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

37622-90-5, Ethyl 4-pyrazolecarboxylate, also known as Ethyl pyrazole-4-carboxylate, is a useful research compound. Its molecular formula is C6H8N2O2 and its molecular weight is 140.14 g\/mol. The purity is usually 95%.<\/p>\n

Ethyl pyrazole-4-carboxylate is a low yield, transition metal salt that is used in the synthesis of pyrazoles. It can be synthesized by the reaction of sodium ethoxide with ethyl chloroformate and a Grignard reagent. Sodium ethoxide is added to a suspension of sodium chloride and dried ethyl chloroformate, followed by addition of magnesium turnings. The mixture is refluxed for one hour, cooled, and filtered to give crystals. Ethyl pyrazole-4-carboxylate is used in the preparation of ethyl esters from aliphatic alcohols by reacting with boron trichloride or phosphorus pentachloride. It participates in certain chemical reactions as a byproduct and can damage equipment during chemical reactions. The yield of this compound can be increased by using an excess amount of Grignard reagent or adding hexamethylenetetramine to the reaction mixture, Recommanded Product: Ethyl 4-pyrazolecarboxylate<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[218,131],"tags":[732],"class_list":["post-9930","post","type-post","status-publish","format-standard","hentry","category-37622-90-5","category-pyrazoles-derivatives","tag-m-w100-150"],"yoast_head":"\nLi, Jing team published research on European Journal of Medicinal Chemistry in 2017 | 37622-90-5 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 37622-90-5, formula is C6H8N2O2, Name is Ethyl 4-pyrazolecarboxylate. 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