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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
Author(s) -
Panchamukhi Shridhar I.,
Mulla Jameel Ahmed S.,
Shetty Nitinkumar S.,
Khazi Mohammed Iqbal A.,
Khan Ashraf Y.,
Kalashetti Mallikarjun B.,
Khazi Imitiyaz Ahmed M.
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000227
Subject(s) - differential scanning calorimetry , antimicrobial , chemistry , particle size , scanning electron microscope , solid lipid nanoparticle , nuclear chemistry , in vitro , thiophene , antibacterial activity , combinatorial chemistry , stereochemistry , organic chemistry , bacteria , materials science , biochemistry , physics , genetics , biology , composite material , thermodynamics
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.