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Chapter 6
Synthesis of benzodiazepines
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Figure-7
A series of 2,3-dihydro-1,5-benzodiazepines were synthesized and evaluated
for anti-inflammatory effects in microglia cells. 49 Among the 1,5-benzodiazepines
tested, compound (Figure-8) strongly inhibited LPS-induced nitric oxide (NO)
production, with an IC 50 value of 7.0 µM in the microglia cells.
Figure-8
A series of 2,3-dihydro-1H-thieno[2,3-e][1,4]diazepine (Figure-9) was
synthesized and evaluated for CNS activity. A new antianxiety screen for
benzodiazepine-like drugs was used along with the standard anticonvulsant test.
Structure activity relationships were discussed. 50
Figure-9
Walser A. et al. 51 have prepared [1,2,4]triazolo[4,3-a][1,4]benzodiazepines
bearing an ethynyl functionality at the 8-position and the isostericthieno[3,2-f]
[1,2,4]triazolo[4,3-a][1,4]diazepines (Figure-10) and evaluated as antagonists of
platelet activating factor.
Department of Chemistry, Saurashtra University, Rajkot-360005 205