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Benzothieno[3,2-e][1,2,4]triazolo[4,3-c]pyrimidines: synthesis, characterization, antimicrobial activity, and incorporation into solid lipid nanoparticles.

Authors
  • Panchamukhi, Shridhar I
  • Mulla, Jameel Ahmed S
  • Shetty, Nitinkumar S
  • Khazi, Mohammed Iqbal A
  • Khan, Ashraf Y
  • Kalashetti, Mallikarjun B
  • Khazi, Imitiyaz Ahmed M
Type
Published Article
Journal
Archiv der Pharmazie
Publisher
Wiley (John Wiley & Sons)
Publication Date
Jun 01, 2011
Volume
344
Issue
6
Pages
358–365
Identifiers
DOI: 10.1002/ardp.201000227
PMID: 21456079
Source
Medline
License
Unknown

Abstract

Fused triazolothienopyrimidines were prepared from the corresponding 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile. These precursors were intern prepared by employing the Gewald's reaction. All the newly synthesized compounds were characterized by spectral and analytical data. Title compounds displayed promising antibacterial and antifungal activities. Compound 3h which exhibited good antimicrobial activity was incorporated into SLN and characterized for particle size, entrapment efficiency (EE%), scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and in-vitro release studies. It showed narrow particle size distribution with high entrapment efficiency. In-vitro release study of compound loaded SLNs in phosphate buffer of pH 7.4, exhibited a biphasic pattern with an initial burst and prolonged release over 24 h.

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