Journal article Open Access

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

Ashok Vishwakarma, Alok Pal Jain, Sandeep Patel


JSON Export

{
  "files": [
    {
      "links": {
        "self": "https://zenodo.org/api/files/e30270f2-70b3-4106-ad43-e88caf912bbd/2.Ashok.pdf"
      }, 
      "checksum": "md5:d2314feb95cb11ac5728c388a50ad502", 
      "bucket": "e30270f2-70b3-4106-ad43-e88caf912bbd", 
      "key": "2.Ashok.pdf", 
      "type": "pdf", 
      "size": 1040579
    }
  ], 
  "owners": [
    159385
  ], 
  "doi": "10.5281/zenodo.6798400", 
  "stats": {
    "version_unique_downloads": 10.0, 
    "unique_views": 8.0, 
    "views": 8.0, 
    "version_views": 8.0, 
    "unique_downloads": 10.0, 
    "version_unique_views": 8.0, 
    "volume": 10405790.0, 
    "version_downloads": 10.0, 
    "downloads": 10.0, 
    "version_volume": 10405790.0
  }, 
  "links": {
    "doi": "https://doi.org/10.5281/zenodo.6798400", 
    "conceptdoi": "https://doi.org/10.5281/zenodo.6798399", 
    "bucket": "https://zenodo.org/api/files/e30270f2-70b3-4106-ad43-e88caf912bbd", 
    "conceptbadge": "https://zenodo.org/badge/doi/10.5281/zenodo.6798399.svg", 
    "html": "https://zenodo.org/record/6798400", 
    "latest_html": "https://zenodo.org/record/6798400", 
    "badge": "https://zenodo.org/badge/doi/10.5281/zenodo.6798400.svg", 
    "latest": "https://zenodo.org/api/records/6798400"
  }, 
  "conceptdoi": "10.5281/zenodo.6798399", 
  "created": "2022-07-05T13:07:03.523439+00:00", 
  "updated": "2022-07-05T13:48:41.865919+00:00", 
  "conceptrecid": "6798399", 
  "revision": 2, 
  "id": 6798400, 
  "metadata": {
    "access_right_category": "success", 
    "doi": "10.5281/zenodo.6798400", 
    "description": "<p><strong><em>Objective:</em></strong><em> The objective of the paper is to design, synthesis and characterization of trisubstituted 4,5-dihydropyrazoles and evaluated for their antibacterial activity.</em></p>\n\n<p><strong><em>Material and methods:</em></strong><em> 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.</em></p>\n\n<p><strong><em>Result and Discussion:</em></strong><em> 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<sup>-1</sup>) at 3012 (C&ndash;H), 2912 (C&ndash;H), 1675 (C=C), 1595 (C-C), 1462 (C=N), 1308 (C-H<strong>), </strong>1512 (N=O), 1334 (N-O), 745 (C-Cl), 1018 (C-Br); 1102 (C-F).&nbsp; The 1HNMR spectra of synthesized compounds depicted the peak at &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<sub>2</sub>), 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. </em></p>\n\n<p><strong><em>Conclusion: </em></strong><em>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. </em></p>\n\n<p><strong>Keywords: </strong><em>Antimicrobial activity, disk diffusion method, antibacterial, pyrazole, gram positive</em></p>", 
    "license": {
      "id": "CC-BY-4.0"
    }, 
    "title": "DESIGN, SYNTHESIS, CHARACTERIZATION AND ANTIBACTERIAL EVALUATION OF TRISUBSTITUTED 4,5-DIHYDROPYRAZOLES DERIVATIVES", 
    "relations": {
      "version": [
        {
          "count": 1, 
          "index": 0, 
          "parent": {
            "pid_type": "recid", 
            "pid_value": "6798399"
          }, 
          "is_last": true, 
          "last_child": {
            "pid_type": "recid", 
            "pid_value": "6798400"
          }
        }
      ]
    }, 
    "publication_date": "2022-07-05", 
    "creators": [
      {
        "name": "Ashok Vishwakarma, Alok Pal Jain, Sandeep Patel"
      }
    ], 
    "access_right": "open", 
    "resource_type": {
      "subtype": "article", 
      "type": "publication", 
      "title": "Journal article"
    }, 
    "related_identifiers": [
      {
        "scheme": "doi", 
        "identifier": "10.5281/zenodo.6798399", 
        "relation": "isVersionOf"
      }
    ]
  }
}
8
10
views
downloads
All versions This version
Views 88
Downloads 1010
Data volume 10.4 MB10.4 MB
Unique views 88
Unique downloads 1010

Share

Cite as