Download (6Mb) - Etheses - Saurashtra University

Chapter 6
Synthesis of benzodiazepines
Figure-10
Nakanishi et al. 52 have reported the synthesis and pharmacological activity of
tetrazolo, oxadiazolo and imidazothienodiazepines derivatives (Figure-11). Some of
them were found as minor tranquilizers.
Figure-11
Malcolm et al. 53 have been synthesized acetamido-1,4-diazepine analogs
(Figure-12) which worked as inhibitor of respiratory syncytial virus(RSV) and
exhibited IC 50 in the range of 10-20 íM over all three assays routinely used. This
molecule also demonstrated excellent pharmacokinetic properties in the rat with a
half-life of approximately 6 hand an oral bioavailability of 76%. This suggested that
the core benzodiazepine was relatively stable to metabolism and a good starting point
for lead optimization.
Figure-12
Department of Chemistry, Saurashtra University, Rajkot-360005 206