Journal article Open Access

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

Kamlesh Kumar Pandey, Alok Pal Jain, Amit Nayak*


MARC21 XML Export

<?xml version='1.0' encoding='UTF-8'?>
<record xmlns="http://www.loc.gov/MARC21/slim">
  <leader>00000nam##2200000uu#4500</leader>
  <controlfield tag="005">20220705134841.0</controlfield>
  <controlfield tag="001">6798462</controlfield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">1490771</subfield>
    <subfield code="z">md5:085628f0b868b590a9504ef591e97a13</subfield>
    <subfield code="u">https://zenodo.org/record/6798462/files/8.Research Paper 1.pdf</subfield>
  </datafield>
  <datafield tag="542" ind1=" " ind2=" ">
    <subfield code="l">open</subfield>
  </datafield>
  <datafield tag="260" ind1=" " ind2=" ">
    <subfield code="c">2022-07-05</subfield>
  </datafield>
  <datafield tag="909" ind1="C" ind2="O">
    <subfield code="p">openaire</subfield>
    <subfield code="o">oai:zenodo.org:6798462</subfield>
  </datafield>
  <datafield tag="100" ind1=" " ind2=" ">
    <subfield code="a">Kamlesh Kumar Pandey, Alok Pal Jain, Amit Nayak*</subfield>
  </datafield>
  <datafield tag="245" ind1=" " ind2=" ">
    <subfield code="a">SYNTHESIS, CHARACTERIZATION AND PHARMACOLOGICAL EVALUATION OF NOVEL ISOXAZOLE BEARING PYRAZOLE DERIVATIVES FOR ANTIBACTERIAL ACTIVITY</subfield>
  </datafield>
  <datafield tag="540" ind1=" " ind2=" ">
    <subfield code="u">https://creativecommons.org/licenses/by/4.0/legalcode</subfield>
    <subfield code="a">Creative Commons Attribution 4.0 International</subfield>
  </datafield>
  <datafield tag="650" ind1="1" ind2="7">
    <subfield code="a">cc-by</subfield>
    <subfield code="2">opendefinition.org</subfield>
  </datafield>
  <datafield tag="520" ind1=" " ind2=" ">
    <subfield code="a">&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;</subfield>
  </datafield>
  <datafield tag="773" ind1=" " ind2=" ">
    <subfield code="n">doi</subfield>
    <subfield code="i">isVersionOf</subfield>
    <subfield code="a">10.5281/zenodo.6798461</subfield>
  </datafield>
  <datafield tag="024" ind1=" " ind2=" ">
    <subfield code="a">10.5281/zenodo.6798462</subfield>
    <subfield code="2">doi</subfield>
  </datafield>
  <datafield tag="980" ind1=" " ind2=" ">
    <subfield code="a">publication</subfield>
    <subfield code="b">article</subfield>
  </datafield>
</record>
8
8
views
downloads
All versions This version
Views 88
Downloads 88
Data volume 11.9 MB11.9 MB
Unique views 88
Unique downloads 88

Share

Cite as