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Synthesis and evaluation of pyrazolines bearing benzothiazole as anti-inflammatory agents.
Kharbanda, Chetna; Alam, Mohammad Sarwar; Hamid, Hinna; Javed, Kalim; Bano, Sameena; Dhulap, Abhijeet; Ali, Yakub; Nazreen, Syed; Haider, Saqlain.
Affiliation
  • Kharbanda C; Department of Chemistry, Faculty of Science, Hamdard University, New Delhi 110 062, India.
  • Alam MS; Department of Chemistry, Faculty of Science, Hamdard University, New Delhi 110 062, India. Electronic address: msalam@jamiahamdard.ac.in.
  • Hamid H; Department of Chemistry, Faculty of Science, Hamdard University, New Delhi 110 062, India.
  • Javed K; Department of Chemistry, Faculty of Science, Hamdard University, New Delhi 110 062, India.
  • Bano S; Department of Chemistry, Faculty of Science, Hamdard University, New Delhi 110 062, India.
  • Dhulap A; CSIR Unit for Research and Development of Information Products, Pune 411038, India.
  • Ali Y; Department of Chemistry, Faculty of Science, Hamdard University, New Delhi 110 062, India.
  • Nazreen S; Department of Chemistry, Faculty of Science, Hamdard University, New Delhi 110 062, India.
  • Haider S; Department of Chemistry, Faculty of Science, Hamdard University, New Delhi 110 062, India.
Bioorg Med Chem ; 22(21): 5804-12, 2014 Nov 01.
Article in En | MEDLINE | ID: mdl-25311566
The present study aims at the synthesis of pyrazolines bearing benzothiazole and their evaluation as anti-inflammatory agents. The synthesized compounds were evaluated for their anti-inflammatory potential using carrageenan induced paw edema model. Two compounds 5a and 5d alleviated inflammation more than the standard drug celecoxib. Eight compounds 5 b, 5 c, 5 e, 5 g, 5 h, 6 b, 6 e and 6 f showed anti-inflammatory activity comparable to celecoxib. To understand the mode of action, COX-2 enzyme assay and TNF-α assay were carried out. All the active compounds were assessed for their cytotoxicity. The ulcerogenic risk evaluation was performed on the active compounds that were not found to be cytotoxic. Out of ten active compounds, two compounds (5 d and 6 f) were finally found to be the most potent anti-inflammatory agents attributing to the suppression of the COX-2 enzyme activity and TNF-α production without being either cytotoxic or ulcerogenic.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrazoles / Benzothiazoles / Anti-Inflammatory Agents Type of study: Prognostic_studies Limits: Animals Language: En Journal: Bioorg Med Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2014 Document type: Article Affiliation country: India Country of publication: United kingdom

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrazoles / Benzothiazoles / Anti-Inflammatory Agents Type of study: Prognostic_studies Limits: Animals Language: En Journal: Bioorg Med Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2014 Document type: Article Affiliation country: India Country of publication: United kingdom