{"id":9966,"date":"2022-10-12T07:02:02","date_gmt":"2022-10-11T23:02:02","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=9966"},"modified":"2022-10-12T07:02:02","modified_gmt":"2022-10-11T23:02:02","slug":"klug-dana-ms-team-published-research-in-journal-of-medicinal-chemistry-in-2021-07-08-1046832-21-6","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=9966","title":{"rendered":"Klug, Dana M’s team published research in Journal of Medicinal Chemistry in 2021-07-08 | 1046832-21-6"},"content":{"rendered":"

Klug, Dana M.; Mavrogiannaki, Eftychia M.; Forbes, Katherine C.; Silva, Lisseth; Diaz-Gonzalez, Rosario; Perez-Moreno, Guiomar; Ceballos-Perez, Gloria; Garcia-Hernandez, Raquel; Bosch-Navarrete, Cristina; Cordon-Obras, Carlos; Gomez-Linan, Claudia; Saura, Andreu; Momper, Jeremiah D.; Martinez-Martinez, Maria Santos; Manzano, Pilar; Syed, Ali; El-Sakkary, Nelly; Caffrey, Conor R.; Gamarro, Francisco; Ruiz-Perez, Luis Miguel; Gonzalez Pacanowska, Dolores; Ferrins, Lori; Navarro, Miguel; Pollastri, Michael P. published the artcile< Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis>, Product Details of C11H19BN2O2<\/a>, the main research area is human African trypanosomiasis Trypanosoma brucei inhibitor BBB antitrypanosomal pharmacokinetic.<\/p>\n

Neglected tropical diseases such as human African trypanosomiasis (HAT) are prevalent primarily in tropical climates and among populations living in poverty. Historically, the lack of economic incentive to develop new treatments for these diseases has meant that existing therapeutics have serious shortcomings in terms of safety, efficacy, and administration, and better therapeutics are needed. We now report a series of 3,5-disubstituted-7-azaindoles identified as growth inhibitors of Trypanosoma brucei, the parasite that causes HAT, through a high-throughput screen. We describe the hit-to-lead optimization of this series and the development and preclin. investigation of 29d (I), a potent antitrypanosomal compound with promising pharmacokinetic (PK) parameters. This compound was ultimately not progressed beyond in vivo PK studies due to its inability to penetrate the blood-brain barrier (BBB), critical for stage 2 HAT treatments.<\/p>\n

Journal of Medicinal Chemistry published new progress about Blood-brain barrier. 1046832-21-6 belongs to class pyrazoles-derivatives, and the molecular formula is C11H19BN2O2, Product Details of C11H19BN2O2<\/a>.<\/p>\n

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

Journal of Medicinal Chemistry published new progress about Blood-brain barrier. 1046832-21-6 belongs to class pyrazoles-derivatives, and the molecular formula is C11H19BN2O2, Product Details of C11H19BN2O2<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[737,131],"tags":[716],"class_list":["post-9966","post","type-post","status-publish","format-standard","hentry","category-1046832-21-6","category-pyrazoles-derivatives","tag-m-w200-250"],"yoast_head":"\nKlug, Dana M's team published research in Journal of Medicinal Chemistry in 2021-07-08 | 1046832-21-6 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Klug, Dana M.; Mavrogiannaki, Eftychia M.; Forbes, Katherine C.; Silva, Lisseth; Diaz-Gonzalez, Rosario; Perez-Moreno, Guiomar; Ceballos-Perez, Gloria; Garcia-Hernandez, Raquel; Bosch-Navarrete, Cristina; Cordon-Obras, Carlos; Gomez-Linan, Claudia; Saura, Andreu; Momper, Jeremiah D.; Martinez-Martinez, Maria Santos; Manzano, Pilar; Syed, Ali; El-Sakkary, Nelly; Caffrey, Conor R.; Gamarro, Francisco; Ruiz-Perez, Luis Miguel; Gonzalez Pacanowska, Dolores; Ferrins, Lori; Navarro, Miguel; Pollastri, Michael P. published the artcile< Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis>, Product Details of C11H19BN2O2, the main research area is human African trypanosomiasis Trypanosoma brucei inhibitor BBB antitrypanosomal pharmacokinetic.\" \/>\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=9966\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Klug, Dana M's team published research in Journal of Medicinal Chemistry in 2021-07-08 | 1046832-21-6 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Klug, Dana M.; Mavrogiannaki, Eftychia M.; Forbes, Katherine C.; Silva, Lisseth; Diaz-Gonzalez, Rosario; Perez-Moreno, Guiomar; Ceballos-Perez, Gloria; Garcia-Hernandez, Raquel; Bosch-Navarrete, Cristina; Cordon-Obras, Carlos; Gomez-Linan, Claudia; Saura, Andreu; Momper, Jeremiah D.; Martinez-Martinez, Maria Santos; Manzano, Pilar; Syed, Ali; El-Sakkary, Nelly; Caffrey, Conor R.; Gamarro, Francisco; Ruiz-Perez, Luis Miguel; Gonzalez Pacanowska, Dolores; Ferrins, Lori; Navarro, Miguel; Pollastri, Michael P. published the artcile< Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis>, Product Details of C11H19BN2O2, the main research area is human African trypanosomiasis Trypanosoma brucei inhibitor BBB antitrypanosomal pharmacokinetic.\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=9966\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-10-11T23:02:02+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=9966\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=9966\",\"name\":\"Klug, Dana M's team published research in Journal of Medicinal Chemistry in 2021-07-08 | 1046832-21-6 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-10-11T23:02:02+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Klug, Dana M.; Mavrogiannaki, Eftychia M.; Forbes, Katherine C.; Silva, Lisseth; Diaz-Gonzalez, Rosario; Perez-Moreno, Guiomar; Ceballos-Perez, Gloria; Garcia-Hernandez, Raquel; Bosch-Navarrete, Cristina; Cordon-Obras, Carlos; Gomez-Linan, Claudia; Saura, Andreu; Momper, Jeremiah D.; Martinez-Martinez, Maria Santos; Manzano, Pilar; Syed, Ali; El-Sakkary, Nelly; Caffrey, Conor R.; Gamarro, Francisco; Ruiz-Perez, Luis Miguel; Gonzalez Pacanowska, Dolores; Ferrins, Lori; Navarro, Miguel; Pollastri, Michael P. published the artcile< Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis>, Product Details of C11H19BN2O2, the main research area is human African trypanosomiasis Trypanosoma brucei inhibitor BBB antitrypanosomal pharmacokinetic.\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=9966#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=9966\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=9966#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Klug, Dana M’s team published research in Journal of Medicinal Chemistry in 2021-07-08 | 1046832-21-6\"}]},{\"@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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