{"id":10498,"date":"2022-10-21T06:59:36","date_gmt":"2022-10-20T22:59:36","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10498"},"modified":"2022-10-21T06:59:36","modified_gmt":"2022-10-20T22:59:36","slug":"diaz-jose-luiss-team-published-research-in-medchemcomm-in-2017-cas-847818-74-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10498","title":{"rendered":"Diaz, Jose Luis’s team published research in MedChemComm in 2017 | CAS: 847818-74-0"},"content":{"rendered":"

In 2017,Diaz, Jose Luis; Corbera, Jordi; Martinez, Daniel; Bordas, Magda; Sicre, Cristina; Pascual, Rosalia; Pretel, Ma Jose; Marin, Ana Paz; Montero, Ana; Dordal, Albert; Alvarez, Ines; Almansa, Carmen published \u300aPyrazolo[3,4-d]pyrimidines as sigma-1 receptor ligands for the treatment of pain. Part 2: Introduction of cyclic substituents in position 4\u300b.MedChemComm published the findings.Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/a> The information in the text is summarized as follows:<\/p>\n

The replacement of acylamino group by cyclic substituents in the position 4 of the pyrazolo[3,4-d]pyrimidine scaffold I [R = Ph, pyridin-3-yl, 1-methyl-1H-pyrazol-5-yl, etc.], led to highly active sigma-1 receptor (\u03c31R) ligands. Ph or pyrazolyl groups were the best in terms of affinity for the \u03c31R and the compound I [R = 1-methyl-1H-pyrazol-5-yl], was the most selective. Compound I [R = 1-methyl-1H-pyrazol-5-yl] was also one of the best \u03c31R ligands ever described in terms of lipophilic ligand efficiency, which translated into a good physicochem. and ADMET profile. In addition, compound I [R = 1-methyl-1H-pyrazol-5-yl] was identified as an antagonist of the \u03c31R in view of its potent antinociceptive profile in several pain models in mice.1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/a>) was used in this study.<\/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, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/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, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/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-10498","post","type-post","status-publish","format-standard","hentry","category-847818-74-0","category-pyrazoles-derivatives","tag-200-300"],"yoast_head":"\nDiaz, Jose Luis's team published research in MedChemComm in 2017 | CAS: 847818-74-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"In 2017,Diaz, Jose Luis; Corbera, Jordi; Martinez, Daniel; Bordas, Magda; Sicre, Cristina; Pascual, Rosalia; Pretel, Ma Jose; Marin, Ana Paz; Montero, Ana; Dordal, Albert; Alvarez, Ines; Almansa, Carmen published \u300aPyrazolo[3,4-d]pyrimidines as sigma-1 receptor ligands for the treatment of pain. Part 2: Introduction of cyclic substituents in position 4\u300b.MedChemComm published the findings.Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The information in the text is summarized as follows:\" \/>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/www.pyrazoles-derivatives.com\/?p=10498\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Diaz, Jose Luis's team published research in MedChemComm in 2017 | CAS: 847818-74-0 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"In 2017,Diaz, Jose Luis; Corbera, Jordi; Martinez, Daniel; Bordas, Magda; Sicre, Cristina; Pascual, Rosalia; Pretel, Ma Jose; Marin, Ana Paz; Montero, Ana; Dordal, Albert; Alvarez, Ines; Almansa, Carmen published \u300aPyrazolo[3,4-d]pyrimidines as sigma-1 receptor ligands for the treatment of pain. Part 2: Introduction of cyclic substituents in position 4\u300b.MedChemComm published the findings.Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The information in the text is summarized as follows:\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=10498\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-10-20T22:59:36+00:00\" \/>\n<meta name=\"author\" content=\"Jessica.F\" \/>\n<meta name=\"twitter:card\" content=\"summary_large_image\" \/>\n<meta name=\"twitter:label1\" content=\"Written by\" \/>\n\t<meta name=\"twitter:data1\" content=\"Jessica.F\" \/>\n\t<meta name=\"twitter:label2\" content=\"Est. reading time\" \/>\n\t<meta name=\"twitter:data2\" content=\"1 minute\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\/\/schema.org\",\"@graph\":[{\"@type\":\"WebPage\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10498\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10498\",\"name\":\"Diaz, Jose Luis's team published research in MedChemComm in 2017 | CAS: 847818-74-0 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-10-20T22:59:36+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"In 2017,Diaz, Jose Luis; Corbera, Jordi; Martinez, Daniel; Bordas, Magda; Sicre, Cristina; Pascual, Rosalia; Pretel, Ma Jose; Marin, Ana Paz; Montero, Ana; Dordal, Albert; Alvarez, Ines; Almansa, Carmen published \u300aPyrazolo[3,4-d]pyrimidines as sigma-1 receptor ligands for the treatment of pain. 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