{"id":10839,"date":"2022-11-02T10:56:54","date_gmt":"2022-11-02T02:56:54","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10839"},"modified":"2022-11-02T10:56:54","modified_gmt":"2022-11-02T02:56:54","slug":"venkatesan-aranapakam-m-et-al-published-their-research-in-journal-of-medicinal-chemistry-in-2006-cas-153597-59-2-2","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10839","title":{"rendered":"Venkatesan, Aranapakam M. et al. published their research in Journal of Medicinal Chemistry in 2006 |CAS: 153597-59-2"},"content":{"rendered":"<p>On July 27, 2006, Venkatesan, Aranapakam M.; Agarwal, Atul; Abe, Takao; Ushirogochi, Hideki; Yamamura, Itsuka; Ado, Mihira; Tsuyoshi, Takasaki; Dos Santos, Osvaldo; Gu, Yansong; Sum, Fuk-Wah; Li, Zhong; Francisco, Gerry; Lin, Yang-I.; Petersen, Peter J.; Yang, Youjun; Kumagai, Toshio; Weiss, William J.; Shlaes, David M.; Knox, James R.; Mansour, Tarek S. published an article.<a href=\"https:\/\/www.ambeed.com\/products\/153597-59-2.html\">COA of Formula: C9H12N2O3<\/a> The title of the article was Structure-Activity Relationship of 6-Methylidene Penems Bearing 6,5 Bicyclic Heterocycles as Broad-Spectrum \u03b2-Lactamase Inhibitors: Evidence for 1,4-Thiazepine Intermediates with C7 R Stereochemistry by Computational Methods. And the article contained the following:<\/p>\n<p>The design and synthesis of a series of 6-methylidene penems containing [6,5]-fused bicycles (thiophene, imidazole, or pyrazle-fused system) as novel class A, B, and C \u03b2-lactamase inhibitors is described. These penems proved to be potent inhibitors of the TEM-1 (class A) and AmpC (class C) \u03b2-lactamases and less so against the class B metallo-\u03b2-lactamase CcrA. Their in vitro and in vivo activities in combination with piperacillin are discussed. On the basis of the crystallog. structures of a serine-bound reaction intermediate of imidazo[2,1-c]oxazine I with SHV-1 (class A) and GC1 (class C) enzymes, compounds II (R = Q, Q1, Q2, etc.) were designed and synthesized. Penems are proposed to form a seven-membered 1,4 thiazepine ring in both class A and C \u03b2-lactamases. The interaction energy calculation for the enzyme-bound intermediates favor the formation of the C7 R enantiomer over the S enantiomer of the 1,4-thiazepine in both \u03b2-lactamases, which is consistent with those obtained from the crystal structure of I with SHV-1 and GC1. The experimental process involved the reaction of Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate(cas: 153597-59-2).<a href=\"https:\/\/www.ambeed.com\/products\/153597-59-2.html\">COA of Formula: C9H12N2O3<\/a><\/p>\n<p>The Article related to methylidene penem preparation beta lactamase inhibitor structure activity, bactericide methylidene penem structure activity, Biomolecules and Their Synthetic Analogs: Beta-Lactam Fungal Metabolites and other aspects.<a href=\"https:\/\/www.ambeed.com\/products\/153597-59-2.html\">COA of Formula: C9H12N2O3<\/a><\/p>\n<p>Referemce:<br \/><a href=\"https:\/\/en.wikipedia.org\/wiki\/Pyrazole\">Pyrazole &#8211; Wikipedia<\/a>,<br \/><a href=\"https:\/\/www.sciencedirect.com\/topics\/chemistry\/pyrazoles\">Pyrazoles &#8211; an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>The Article related to methylidene penem preparation beta lactamase inhibitor structure activity, bactericide methylidene penem structure activity, Biomolecules and Their Synthetic Analogs: Beta-Lactam Fungal Metabolites and other aspects.<a href=\"https:\/\/www.ambeed.com\/products\/153597-59-2.html\">COA of Formula: C9H12N2O3<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[760,131],"tags":[128],"class_list":["post-10839","post","type-post","status-publish","format-standard","hentry","category-153597-59-2","category-pyrazoles-derivatives","tag-100-200"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Venkatesan, Aranapakam M. et al. published their research in Journal of Medicinal Chemistry in 2006 |CAS: 153597-59-2 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"On July 27, 2006, Venkatesan, Aranapakam M.; Agarwal, Atul; Abe, Takao; Ushirogochi, Hideki; Yamamura, Itsuka; Ado, Mihira; Tsuyoshi, Takasaki; Dos Santos, Osvaldo; Gu, Yansong; Sum, Fuk-Wah; Li, Zhong; Francisco, Gerry; Lin, Yang-I.; Petersen, Peter J.; Yang, Youjun; Kumagai, Toshio; Weiss, William J.; Shlaes, David M.; Knox, James R.; Mansour, Tarek S. published an article.COA of Formula: C9H12N2O3 The title of the article was Structure-Activity Relationship of 6-Methylidene Penems Bearing 6,5 Bicyclic Heterocycles as Broad-Spectrum \u03b2-Lactamase Inhibitors: Evidence for 1,4-Thiazepine Intermediates with C7 R Stereochemistry by Computational Methods. And the article contained the following:\" \/>\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=10839\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Venkatesan, Aranapakam M. et al. published their research in Journal of Medicinal Chemistry in 2006 |CAS: 153597-59-2 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"On July 27, 2006, Venkatesan, Aranapakam M.; Agarwal, Atul; Abe, Takao; Ushirogochi, Hideki; Yamamura, Itsuka; Ado, Mihira; Tsuyoshi, Takasaki; Dos Santos, Osvaldo; Gu, Yansong; Sum, Fuk-Wah; Li, Zhong; Francisco, Gerry; Lin, Yang-I.; Petersen, Peter J.; Yang, Youjun; Kumagai, Toshio; Weiss, William J.; Shlaes, David M.; Knox, James R.; Mansour, Tarek S. published an article.COA of Formula: C9H12N2O3 The title of the article was Structure-Activity Relationship of 6-Methylidene Penems Bearing 6,5 Bicyclic Heterocycles as Broad-Spectrum \u03b2-Lactamase Inhibitors: Evidence for 1,4-Thiazepine Intermediates with C7 R Stereochemistry by Computational Methods. 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