{"id":11203,"date":"2022-11-21T05:05:22","date_gmt":"2022-11-20T21:05:22","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11203"},"modified":"2022-11-21T05:05:22","modified_gmt":"2022-11-20T21:05:22","slug":"sijm-maartens-team-published-research-in-chemmedchem-in-15-cas-763120-58-7","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11203","title":{"rendered":"Sijm, Maarten&#8217;s team published research in ChemMedChem  in 15 | CAS: 763120-58-7"},"content":{"rendered":"<p>Sijm, Maarten published the artcile<b><i>Identification of Phenylphthalazinones as a New Class of Leishmania infantum Inhibitors<\/i><\/b>,  <a href=\"https:\/\/www.ambeed.com\/products\/763120-58-7.html\">Computed Properties of  763120-58-7<\/a>,  the publication is  ChemMedChem (2020), 15(2), 219-227, database is CAplus and MEDLINE.<\/p>\n<p>Leishmaniasis is a neglected parasitic disease caused by over 20 different Leishmania species. Current treatments often rely on harsh regimes of pentavalent antimonials such as sodium stibogluconate, while more recent drugs suffer other shortcomings such as low stability and rapid emergence of treatment failure, amongst others. Furthermore, the effectiveness of drugs varies depending on the infecting Leishmania species, thus there is an urgent need for new and effective anti-leishmanial drugs. Screening of an inhouse compound library identified the hexahydrophthalazinone NPD-2942 as a low micromolar hit with a pIC<sub>50<\/sub> of 5.8 against L. infantum and a pIC<sub>50<\/sub> of 4.6 for cytotoxicity against human MRC-5 fibroblasts. To derive structure-activity relationships, we modified the cyclohexyl ring of the hexahydrophthalazinone scaffold and 1,2,3-triazoles were attempted as replacement for the pyrazole ring, amongst others. Ultimately, the 2,3-pyrazole-substituted hexahydrophthalazinone NPD-1289 was identified as the most potent analog in this series with a pIC<sub>50<\/sub> of 6.3, although some cytotoxicity toward MRC-5 cells (pIC<sub>50<\/sub>=5.1) was recorded as well. Replacement of the unsubstituted 2,3-pyrazole with 1,2,3-triazoles led to compounds with lower anti-leishmanial activity. The current scaffold is a valuable new starting point for optimization toward novel anti-leishmanial drugs.<\/p>\n<p>ChemMedChem published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C10H13NO2, <a href=\"https:\/\/www.ambeed.com\/products\/763120-58-7.html\">Computed Properties of  763120-58-7<\/a>.<\/p>\n<p>Referemce:<br \/><a href=\"https:\/\/en.wikipedia.org\/wiki\/Pyrazole\">https:\/\/en.wikipedia.org\/wiki\/Pyrazole<\/a>,<br \/><a href=\"Pyrazole - Wikipedia\">Pyrazoles &#8211; an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>ChemMedChem published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C10H13NO2, <a href=\"https:\/\/www.ambeed.com\/products\/763120-58-7.html\">Computed Properties of  763120-58-7<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[131],"tags":[732],"class_list":["post-11203","post","type-post","status-publish","format-standard","hentry","category-pyrazoles-derivatives","tag-m-w100-150"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - 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