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SYNTHESIS, CHARACTERIZATION AND PHARMACOLOGICAL EVALUATION OF NOVEL ISOXAZOLE BEARING PYRAZOLE DERIVATIVES FOR ANTIBACTERIAL ACTIVITY

Kamlesh Kumar Pandey, Alok Pal Jain, Amit Nayak*


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  <identifier identifierType="DOI">10.5281/zenodo.6798462</identifier>
  <creators>
    <creator>
      <creatorName>Kamlesh Kumar Pandey, Alok Pal Jain, Amit Nayak*</creatorName>
    </creator>
  </creators>
  <titles>
    <title>SYNTHESIS, CHARACTERIZATION AND PHARMACOLOGICAL EVALUATION OF NOVEL ISOXAZOLE BEARING PYRAZOLE DERIVATIVES FOR ANTIBACTERIAL ACTIVITY</title>
  </titles>
  <publisher>Zenodo</publisher>
  <publicationYear>2022</publicationYear>
  <dates>
    <date dateType="Issued">2022-07-05</date>
  </dates>
  <resourceType resourceTypeGeneral="JournalArticle"/>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://zenodo.org/record/6798462</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsVersionOf">10.5281/zenodo.6798461</relatedIdentifier>
  </relatedIdentifiers>
  <rightsList>
    <rights rightsURI="https://creativecommons.org/licenses/by/4.0/legalcode">Creative Commons Attribution 4.0 International</rights>
    <rights rightsURI="info:eu-repo/semantics/openAccess">Open Access</rights>
  </rightsList>
  <descriptions>
    <description descriptionType="Abstract">&lt;p&gt;&lt;strong&gt;&lt;em&gt;Objective:&lt;/em&gt;&lt;/strong&gt;&lt;em&gt; The objective of the paper was to synthesis and characterization of new &lt;em&gt;isoxazole bearing pyrazole derivatives and evaluate them for antibacterial activity.&lt;/em&gt;&lt;/em&gt;&lt;/p&gt;

&lt;p&gt;&lt;strong&gt;&lt;em&gt;Material and methods:&lt;/em&gt;&lt;/strong&gt;&lt;em&gt; The isoxazole bearing pyrazole derivatives have been synthesized by the utilize the four-step process. Total Ten compounds have been synthesized and characterized by IR, &lt;sup&gt;1&lt;/sup&gt;HNMR, elemental and mass spectral analysis. The final compounds (PIA-1 to PIA-10) have been evaluated for antibacterial activity by disk diffusion method using sulfamethoxazole as standard drug.&lt;/em&gt;&lt;/p&gt;

&lt;p&gt;&lt;strong&gt;&lt;em&gt;Result and Discussion:&lt;/em&gt;&lt;/strong&gt;&lt;em&gt; The IR spectra of compound PIA-1 to PIA-10 shown the characteristics peak at 3052 (N-H), 2964 (C-H), 1628 (C=O), 1448 (C=N), 1625 (C=C), 1126 (C-O); 1015 (C-Br); 850 (C-Cl) and 1102 (C-F).&amp;nbsp; The 1HNMR spectrum show the characteristics peak &amp;delta; 6.68-6.70 (d, 2H, Ar-Fluorine), 7.14-7.16 (d, 1H, Ar-chlorine), 7.28-7.30 (m, 5H, Ar-H), 7.58-8.00 (d, 2H, Ar-Chlorine), 7.75-7.78 (d, 2H, Ar-Fluorine), 8.25 (s, 1H, Ar-H isoxazole), 10.97 (s, 1H, -Ar-H pyrazole); 7.26 (s, 1H, Ar-Cl). The antibacterial evaluation of the synthesized compounds stated that Isoxazole-pyrazole derivatives exhibit considerable inhibitory effect on all bacteria strains at both 50 &amp;micro;g/ml and 100 &amp;micro;g/ml dosing levels. PIA-1, PIA-2, PIA-3, PIA-4 had the highest activity in gram positive bacterial stains and PIA-1, PIA-3, PIA-4 and PIA-10 have shown best activity against gram negative bacteria.&lt;/em&gt;&lt;/p&gt;

&lt;p&gt;&lt;strong&gt;&lt;em&gt;Conclusion&lt;/em&gt;&lt;/strong&gt;&lt;em&gt;: The antibacterial activity of the synthesized compounds (PIA-1, PIA-3, PIA-4 and PIA-5) was significantly similar or better than that of standard Drug used for comparison. These Isoxazole bearing pyrazole compounds have demonstrated potency as a superior antibacterial agent, although more in-vivo research on the efficacy and dosage regimen of the compounds is needed.&lt;/em&gt;&lt;/p&gt;

&lt;p&gt;&lt;strong&gt;Keywords: &lt;/strong&gt;&lt;em&gt;Antibacterial activity, Pyrazole, Isoxazole, sulfamethoxazole, disk diffusion&lt;/em&gt;&lt;/p&gt;</description>
  </descriptions>
</resource>
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