{"id":11011,"date":"2022-11-16T03:23:12","date_gmt":"2022-11-15T19:23:12","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11011"},"modified":"2022-11-16T03:23:12","modified_gmt":"2022-11-15T19:23:12","slug":"khonde-lutete-peguys-team-published-research-in-journal-of-medicinal-chemistry-in-2021-09-09-cas-166196-54-9","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11011","title":{"rendered":"Khonde, Lutete Peguy’s team published research in Journal of Medicinal Chemistry in 2021-09-09 | CAS: 166196-54-9"},"content":{"rendered":"

Khonde, Lutete Peguy published the artcile1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis<\/i><\/b>, Application In Synthesis of 166196-54-9<\/a>, the main research area is diarylpyrazolyl acylsulfonamide preparation antituberculosis activity.<\/p>\n

Phenotypic whole cell high-throughput screening of a ~150,000 diverse set of compounds against Mycobacterium tuberculosis (Mtb) in cholesterol-containing media identified 1,3-diarylpyrazolyl-acylsulfonamide I as a moderately active hit. Structure-activity relationship (SAR) studies demonstrated a clear scope to improve whole cell potency to MIC values of <0.5\u03bcM, and a plausible pharmacophore model was developed to describe the chem. space of active compounds Compounds are bactericidal in vitro against replicating Mtb and retained activity against multidrug-resistant clin. isolates. Initial biol. triage assays indicated cell wall biosynthesis as a plausible mode-of-action for the series. However, no cross-resistance with known cell wall targets such as MmpL3, DprE1, InhA, and EthA was detected, suggesting a potentially novel mode-of-action or inhibition. The in vitro and in vivo drug metabolism and pharmacokinetics profiles of several active compounds from the series were established leading to the identification of a compound for in vivo efficacy proof-of-concept studies.\n\nJournal of Medicinal Chemistry published new progress about Homo sapiens. 166196-54-9 belongs to class pyrazoles-derivatives, name is 4-(4-Bromo-1H-pyrazol-3-yl)pyridine, and the molecular formula is C8H6BrN3, Application In Synthesis of 166196-54-9<\/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 Homo sapiens. 166196-54-9 belongs to class pyrazoles-derivatives, name is 4-(4-Bromo-1H-pyrazol-3-yl)pyridine, and the molecular formula is C8H6BrN3, Application In Synthesis of 166196-54-9<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[783,131],"tags":[716],"class_list":["post-11011","post","type-post","status-publish","format-standard","hentry","category-166196-54-9","category-pyrazoles-derivatives","tag-m-w200-250"],"yoast_head":"\nKhonde, Lutete Peguy's team published research in Journal of Medicinal Chemistry in 2021-09-09 | CAS: 166196-54-9 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Khonde, Lutete Peguy published the artcile1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis, Application In Synthesis of 166196-54-9, the main research area is diarylpyrazolyl acylsulfonamide preparation antituberculosis activity.\" \/>\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=11011\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Khonde, Lutete Peguy's team published research in Journal of Medicinal Chemistry in 2021-09-09 | CAS: 166196-54-9 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Khonde, Lutete Peguy published the artcile1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis, Application In Synthesis of 166196-54-9, the main research area is diarylpyrazolyl acylsulfonamide preparation antituberculosis activity.\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=11011\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-11-15T19:23:12+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<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\/\/schema.org\",\"@graph\":[{\"@type\":\"WebPage\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11011\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11011\",\"name\":\"Khonde, Lutete Peguy's team published research in Journal of Medicinal Chemistry in 2021-09-09 | CAS: 166196-54-9 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-11-15T19:23:12+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Khonde, Lutete Peguy published the artcile1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis, Application In Synthesis of 166196-54-9, the main research area is diarylpyrazolyl acylsulfonamide preparation antituberculosis activity.\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11011#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=11011\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11011#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Khonde, Lutete Peguy’s team published research in Journal of Medicinal Chemistry in 2021-09-09 | CAS: 166196-54-9\"}]},{\"@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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