{"id":10023,"date":"2022-10-13T03:04:34","date_gmt":"2022-10-12T19:04:34","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10023"},"modified":"2022-10-13T03:04:34","modified_gmt":"2022-10-12T19:04:34","slug":"moya-garzon-maria-doloress-team-published-research-in-journal-of-medicinal-chemistry-in-2018-cas-847818-74-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10023","title":{"rendered":"Moya-Garzon, Maria Dolores’s team published research in Journal of Medicinal Chemistry in 2018 | CAS: 847818-74-0"},"content":{"rendered":"

Category: pyrazoles-derivatives<\/a>In 2018 ,\u300aSalicylic Acid Derivatives Inhibit Oxalate Production in Mouse Hepatocytes with Primary Hyperoxaluria Type 1\u300b was published in Journal of Medicinal Chemistry. The article was written by Moya-Garzon, Maria Dolores; Martin Higueras, Cristina; Penalver, Pablo; Romera, Manuela; Fernandes, Miguel X.; Franco-Montalban, Francisco; Gomez-Vidal, Jose A.; Salido, Eduardo; Diaz-Gavilan, Monica. The article contains the following contents:<\/p>\n

Primary hyperoxaluria type 1 (PH1) is a rare life-threatening genetic disease related to glyoxylate metabolism and characterized by accumulation of calcium oxalate crystals. Current therapies involve hepatic and\/or renal transplantation, procedures that have significant morbidity and mortality and require long-term immunosuppression. Thus, a pharmacol. treatment is urgently needed. We introduce here an unprecedented activity of salicylic acid derivatives as agents capable of decreasing oxalate output in hyperoxaluric hepatocytes at the low micromolar range, which means a potential use in the treatment of PH1. Though correlation of this phenotypic activity with glycolate oxidase (GO) inhibition is still to be verified, most of the salicylic acids described here are GO inhibitors with IC50 values down to 3 \u03bcM. Binding mode of salicylic acids inside GO has been studied using in silico methods, and preliminary structure-activity relationships have been established. The drug-like structure and ease of synthesis of our compounds make them promising hits for structural optimization. In the experiment, the researchers used 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Category: pyrazoles-derivatives<\/a>)<\/p>\n

1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Category: pyrazoles-derivatives<\/a><\/p>\n

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

1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Category: pyrazoles-derivatives<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[744,131],"tags":[129],"class_list":["post-10023","post","type-post","status-publish","format-standard","hentry","category-847818-74-0","category-pyrazoles-derivatives","tag-200-300"],"yoast_head":"\nMoya-Garzon, Maria Dolores's team published research in Journal of Medicinal Chemistry in 2018 | CAS: 847818-74-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Category: pyrazoles-derivativesIn 2018 ,\u300aSalicylic Acid Derivatives Inhibit Oxalate Production in Mouse Hepatocytes with Primary Hyperoxaluria Type 1\u300b was published in Journal of Medicinal Chemistry. 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