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DESIGN, SYNTHESIS, CHARACTERIZATION AND ANTIBACTERIAL EVALUATION OF TRISUBSTITUTED 4,5-DIHYDROPYRAZOLES DERIVATIVES

Ashok Vishwakarma, Alok Pal Jain, Sandeep Patel


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  <identifier identifierType="DOI">10.5281/zenodo.6798400</identifier>
  <creators>
    <creator>
      <creatorName>Ashok Vishwakarma, Alok Pal Jain, Sandeep Patel</creatorName>
    </creator>
  </creators>
  <titles>
    <title>DESIGN, SYNTHESIS, CHARACTERIZATION AND ANTIBACTERIAL EVALUATION OF TRISUBSTITUTED 4,5-DIHYDROPYRAZOLES DERIVATIVES</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/6798400</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsVersionOf">10.5281/zenodo.6798399</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 is to design, synthesis and characterization of trisubstituted 4,5-dihydropyrazoles and evaluated for their antibacterial activity.&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 derivatives have been synthesized by the two steps process, in first step 1-(4-aminophenyl)ethan-1-one (0.002M) (1) react with 4-substituted benzaldehyde (2) to form (E)-1-(4-substituted phenyl)-3-(p-substituted)prop-2-en-1-one [3]. The final compound (4), 1-(4-substitutedphenyl)-3-(4-substitutedphenyl)-5-(p-substituted)-4,5-dihydro-1H-pyrazole was synthesized by the reaction of compound 3 with different (4-fluorophenyl) hydrazine and (4-chlorophenyl) hydrazine. Total Sixteen compounds have been synthesized and characterized by physicochemical and spectral analysis. The final compounds (TDHP-1 to TDHP-16) have been evaluated for antibacterial activity by disk diffusion method.&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 synthesized compounds have characterized by the IR, 1HNMR and mass spectral analysis. The IR spectrum of the compounds has shown the characteristics peak (cm&lt;sup&gt;-1&lt;/sup&gt;) at 3012 (C&amp;ndash;H), 2912 (C&amp;ndash;H), 1675 (C=C), 1595 (C-C), 1462 (C=N), 1308 (C-H&lt;strong&gt;), &lt;/strong&gt;1512 (N=O), 1334 (N-O), 745 (C-Cl), 1018 (C-Br); 1102 (C-F).&amp;nbsp; The 1HNMR spectra of synthesized compounds depicted the peak at &amp;delta;7.23-8.62 (m, 4H, CH=CH-CH=CH), 7.03-8.80 (m, 3H, Ar-H), 3.08, 2.47 (d, 2H, CH&lt;sub&gt;2&lt;/sub&gt;), 3.42 (d, 1H, C-5, CH), 11.431 (s, 1H, NH). The Data of antibacterial activity against the gram-positive bacterial strains (Bacillus subtilis and Staphylococcus aureus) suggested that among substituted pyrazoline derivatives (TDHP-1 to TDHP-16), compound TDHP-2, TDHP-3, TDHP-4, TDHP-5, TDHP-6, TDHP-7, TDHP-8 have shown best activity against gram positive bacteria and The Data of antibacterial activity against the gram-negative bacterial strains (Salmonella typhimurium and Pseudomonas aeruginosa) suggested that among substituted pyrazoline derivatives (TDHP-1 to TDHP-16), compound TDHP-1, TDHP-2, TDHP-3, TDHP-4, TDHP-5 TDHP-6, TDHP-7, TDHP-8 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;In general, trisubstituted 4,5-dihydropyrazoles derivatives having amine termination has shown the better anti-microbial activity as compared to standard drug. There is a need in drug design strategy to achieve more anti-microbial potency in different bacterial strain on novel future synthetic heterocyclic compounds. &lt;/em&gt;&lt;/p&gt;

&lt;p&gt;&lt;strong&gt;Keywords: &lt;/strong&gt;&lt;em&gt;Antimicrobial activity, disk diffusion method, antibacterial, pyrazole, gram positive&lt;/em&gt;&lt;/p&gt;</description>
  </descriptions>
</resource>
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