{"id":11321,"date":"2022-11-23T03:41:00","date_gmt":"2022-11-22T19:41:00","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11321"},"modified":"2022-11-23T03:41:00","modified_gmt":"2022-11-22T19:41:00","slug":"brindani-nicolettas-team-published-research-in-journal-of-medicinal-chemistry-in-63-cas-890590-91-7","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11321","title":{"rendered":"Brindani, Nicoletta’s team published research in Journal of Medicinal Chemistry in 63 | CAS: 890590-91-7"},"content":{"rendered":"

Brindani, Nicoletta published the artcileIdentification, Structure-Activity Relationship, and Biological Characterization of 2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indoles as a Novel Class of CFTR Potentiators<\/i><\/b>, Synthetic Route of 890590-91-7<\/a>, the publication is Journal of Medicinal Chemistry (2020), 63(19), 11169-11194, database is CAplus and MEDLINE.<\/p>\n

Cystic fibrosis (CF) is a life-threatening autosomal recessive disease, caused by mutations in the CF transmembrane conductance regulator (CFTR) chloride channel. CFTR modulators have been reported to address the basic defects associated with CF-causing mutations, partially restoring the CFTR function in terms of protein processing and\/or channel gating. Small-mol. compounds, called potentiators, are known to ameliorate the gating defect. In this study, we describe the identification of the 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole core as a novel chemotype of potentiators. In-depth structure-activity relationship studies led to the discovery of enantiomerically pure I<\/strong> endowed with a good efficacy in rescuing the gating defect of F508del- and G551D-CFTR and a promising in vitro druglike profile. The in vivo characterization of \u03b3-carboline I<\/strong> showed considerable exposure levels and good oral bioavailability, with detectable distribution to the lungs after oral administration to rats. Overall, these findings may represent an encouraging starting point to further expand this chem. class, adding a new chemotype to the existing classes of CFTR potentiators.<\/p>\n

Journal of Medicinal Chemistry published new progress about 890590-91-7. 890590-91-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Carboxylic acid, name is 3-Isopropyl-1H-pyrazole-5-carboxylic acid, and the molecular formula is C7H10N2O2, Synthetic Route of 890590-91-7<\/a>.<\/p>\n

Referemce:
https:\/\/en.wikipedia.org\/wiki\/Pyrazole<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

Journal of Medicinal Chemistry published new progress about 890590-91-7. 890590-91-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Carboxylic acid, name is 3-Isopropyl-1H-pyrazole-5-carboxylic acid, and the molecular formula is C7H10N2O2, Synthetic Route of 890590-91-7<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[800,131],"tags":[717],"class_list":["post-11321","post","type-post","status-publish","format-standard","hentry","category-890590-91-7","category-pyrazoles-derivatives","tag-m-w150-200"],"yoast_head":"\nBrindani, Nicoletta's team published research in Journal of Medicinal Chemistry in 63 | CAS: 890590-91-7 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Brindani, Nicoletta published the artcileIdentification, Structure-Activity Relationship, and Biological Characterization of 2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indoles as a Novel Class of CFTR Potentiators, Synthetic Route of 890590-91-7, the publication is Journal of Medicinal Chemistry (2020), 63(19), 11169-11194, database is CAplus and MEDLINE.\" \/>\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=11321\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Brindani, Nicoletta's team published research in Journal of Medicinal Chemistry in 63 | CAS: 890590-91-7 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Brindani, Nicoletta published the artcileIdentification, Structure-Activity Relationship, and Biological Characterization of 2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indoles as a Novel Class of CFTR Potentiators, Synthetic Route of 890590-91-7, the publication is Journal of Medicinal Chemistry (2020), 63(19), 11169-11194, database is CAplus and MEDLINE.\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=11321\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-11-22T19:41:00+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=11321\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11321\",\"name\":\"Brindani, Nicoletta's team published research in Journal of Medicinal Chemistry in 63 | CAS: 890590-91-7 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-11-22T19:41:00+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Brindani, Nicoletta published the artcileIdentification, Structure-Activity Relationship, and Biological Characterization of 2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indoles as a Novel Class of CFTR Potentiators, Synthetic Route of 890590-91-7, the publication is Journal of Medicinal Chemistry (2020), 63(19), 11169-11194, database is CAplus and MEDLINE.\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11321#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=11321\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11321#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Brindani, Nicoletta’s team published research in Journal of Medicinal Chemistry in 63 | CAS: 890590-91-7\"}]},{\"@type\":\"WebSite\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/\",\"name\":\"pyrazoles-derivatives\",\"description\":\"Several pyrazole derivatives possess important pharmacological activities and they have been proved useful materials in drug research. 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