{"id":12275,"date":"2023-02-13T04:19:39","date_gmt":"2023-02-12T20:19:39","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=12275"},"modified":"2023-02-13T04:19:39","modified_gmt":"2023-02-12T20:19:39","slug":"eissa-ibrahim-h-et-al-published-their-research-in-european-journal-of-medicinal-chemistry-in-2017-cas-10199-53-8","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=12275","title":{"rendered":"Eissa, Ibrahim H. et al. published their research in European Journal of Medicinal Chemistry in 2017 | CAS: 10199-53-8"},"content":{"rendered":"<p>Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus was written by Eissa, Ibrahim H.;Mohammad, Haroon;Qassem, Omar A.;Younis, Waleed;Abdelghany, Tamer M.;Elshafeey, Ahmed;Abd Rabo Moustafa, Mahmoud M.;Seleem, Mohamed N.;Mayhoub, Abdelrahman S.. And the article was included in European Journal of Medicinal Chemistry in 2017.<a href=\"https:\/\/www.ambeed.com\/products\/10199-53-8.html\">Synthetic Route of C11H10N2O2<\/a> This article mentions the following:<\/p>\n<p>A new class of diphenylurea was identified as a novel antibacterial scaffold with an antibacterial spectrum that includes highly resistant staphylococcal isolates, namely methicillin- and vancomycin-resistant Staphylococcus aureus (MRSA &amp; VRSA). Starting with a lead compound that carries an aminoguanidine functionality from one side and a Bu moiety on the other ring, several analogs were prepared Considering the pharmacokinetic parameters as a key factor in structural optimization, the structure-activity-relationships (SARs) at the lipophilic side chain were rigorously examined leading to the discovery of the cycloheptyloxyl analog <strong>I<\/strong> as a potential drug-candidate. This compound has several notable advantages over vancomycin and linezolid including rapid killing kinetics against MRSA and the ability to target and reduce the burden of MRSA harboring inside immune cells (macrophages). Furthermore, the potent anti-MRSA activity of <strong>I<\/strong> was confirmed in vivo using a Caenorhabditis elegans animal model. The present study provides a foundation for further development of diphenylurea compounds as potential therapeutic agents to address the burgeoning challenge of bacterial resistance to antibiotics. In the experiment, the researchers used many compounds, for example, 1-Methyl-5-phenyl-1H-pyrazole-3-carboxylic acid (cas: 10199-53-8<a href=\"https:\/\/www.ambeed.com\/products\/10199-53-8.html\">Synthetic Route of C11H10N2O2<\/a>).<\/p>\n<p>1-Methyl-5-phenyl-1H-pyrazole-3-carboxylic acid (cas: 10199-53-8) belongs to pyrazole derivatives. Pyrazole has two ring nitrogen atoms in which N1 is pyrrolic and N2 is pyridine-like. The N1 nitrogen is not reactive but is deprotonated in the presence of a base-forming anion. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.<a href=\"https:\/\/www.ambeed.com\/products\/10199-53-8.html\">Synthetic Route of C11H10N2O2<\/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>1-Methyl-5-phenyl-1H-pyrazole-3-carboxylic acid (cas: 10199-53-8) belongs to pyrazole derivatives. Pyrazole has two ring nitrogen atoms in which N1 is pyrrolic and N2 is pyridine-like. The N1 nitrogen is not reactive but is deprotonated in the presence of a base-forming anion. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.<a href=\"https:\/\/www.ambeed.com\/products\/10199-53-8.html\">Synthetic Route of C11H10N2O2<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[836,131],"tags":[129],"class_list":["post-12275","post","type-post","status-publish","format-standard","hentry","category-10199-53-8","category-pyrazoles-derivatives","tag-200-300"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Eissa, Ibrahim H. et al. published their research in European Journal of Medicinal Chemistry in 2017 | CAS: 10199-53-8 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus was written by Eissa, Ibrahim H.;Mohammad, Haroon;Qassem, Omar A.;Younis, Waleed;Abdelghany, Tamer M.;Elshafeey, Ahmed;Abd Rabo Moustafa, Mahmoud M.;Seleem, Mohamed N.;Mayhoub, Abdelrahman S.. 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