Abdul Hannan Khan, Muhammad Bilal, Abid Mahmood, Nasir Rasool, Muhammad Usman Qamar, Muhammad Imran, Sebastian Ionut Toma, Oana Andreescu
{"title":"N-(4-溴-3-甲基苯基)吡嗪-2-甲酰胺衍生物的简易合成、对临床分离的 XDR 伤寒杆菌的抗菌活性、碱性磷酸酶抑制活性以及对接研究。","authors":"Abdul Hannan Khan, Muhammad Bilal, Abid Mahmood, Nasir Rasool, Muhammad Usman Qamar, Muhammad Imran, Sebastian Ionut Toma, Oana Andreescu","doi":"10.3390/ph17091241","DOIUrl":null,"url":null,"abstract":"<p><p>The emergence of extensively drug-resistant <i>Salmonella</i> Typhi (XDR-<i>S. Typhi</i>) poses a grave public health threat due to its resistance to fluoroquinolones and third-generation cephalosporins. This resistance significantly complicates treatment options, underscoring the urgent need for new therapeutic strategies. In this study, we synthesized pyrazine carboxamides (<b>3, 5a</b>-<b>5d</b>) in good yields through the Suzuki reaction. Afterward, we evaluate their antibacterial activities against XDR-<i>S. Typhi</i> via the agar well diffusion method; <b>5d</b> has the strongest antibacterial activity with MIC 6.25 (mg/mL). Moreover, in vitro Alkaline Phosphatase inhibitor activity was also determined; <b>5d</b> is the most potent compound, with an IC<sub>50</sub> of 1.469 ± 0.02 µM. Further, in silico studies were performed to find the type of interactions between synthesized compounds and target proteins.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":null,"pages":null},"PeriodicalIF":4.3000,"publicationDate":"2024-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11434897/pdf/","citationCount":"0","resultStr":"{\"title\":\"Facile Synthesis of <i>N</i>-(4-Bromo-3-methylphenyl)pyrazine-2-carboxamide Derivatives, Their Antibacterial Activities against Clinically Isolated XDR <i>S. Typhi</i>, Alkaline Phosphatase Inhibitor Activities, and Docking Studies.\",\"authors\":\"Abdul Hannan Khan, Muhammad Bilal, Abid Mahmood, Nasir Rasool, Muhammad Usman Qamar, Muhammad Imran, Sebastian Ionut Toma, Oana Andreescu\",\"doi\":\"10.3390/ph17091241\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>The emergence of extensively drug-resistant <i>Salmonella</i> Typhi (XDR-<i>S. Typhi</i>) poses a grave public health threat due to its resistance to fluoroquinolones and third-generation cephalosporins. This resistance significantly complicates treatment options, underscoring the urgent need for new therapeutic strategies. In this study, we synthesized pyrazine carboxamides (<b>3, 5a</b>-<b>5d</b>) in good yields through the Suzuki reaction. Afterward, we evaluate their antibacterial activities against XDR-<i>S. Typhi</i> via the agar well diffusion method; <b>5d</b> has the strongest antibacterial activity with MIC 6.25 (mg/mL). Moreover, in vitro Alkaline Phosphatase inhibitor activity was also determined; <b>5d</b> is the most potent compound, with an IC<sub>50</sub> of 1.469 ± 0.02 µM. Further, in silico studies were performed to find the type of interactions between synthesized compounds and target proteins.</p>\",\"PeriodicalId\":20198,\"journal\":{\"name\":\"Pharmaceuticals\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":4.3000,\"publicationDate\":\"2024-09-20\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11434897/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmaceuticals\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.3390/ph17091241\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceuticals","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.3390/ph17091241","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Facile Synthesis of N-(4-Bromo-3-methylphenyl)pyrazine-2-carboxamide Derivatives, Their Antibacterial Activities against Clinically Isolated XDR S. Typhi, Alkaline Phosphatase Inhibitor Activities, and Docking Studies.
The emergence of extensively drug-resistant Salmonella Typhi (XDR-S. Typhi) poses a grave public health threat due to its resistance to fluoroquinolones and third-generation cephalosporins. This resistance significantly complicates treatment options, underscoring the urgent need for new therapeutic strategies. In this study, we synthesized pyrazine carboxamides (3, 5a-5d) in good yields through the Suzuki reaction. Afterward, we evaluate their antibacterial activities against XDR-S. Typhi via the agar well diffusion method; 5d has the strongest antibacterial activity with MIC 6.25 (mg/mL). Moreover, in vitro Alkaline Phosphatase inhibitor activity was also determined; 5d is the most potent compound, with an IC50 of 1.469 ± 0.02 µM. Further, in silico studies were performed to find the type of interactions between synthesized compounds and target proteins.
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