Download (6Mb) - Etheses - Saurashtra University

Chapter 2
Synthesis of substituted pyrimidines via Wittig
Padama shale et al. 23 have been reported Naphtho[2,1-b]furo[3,2-d]pyrimidine
and Carrageen induced rat paw edema method was employed for evaluating the antiinflammatory
activity. The compounds were given at a dose of 80 mg/kg body weight
in albino rats weighing between 150 and 200 g. The oedema was produced by
injecting carrageenan solution at the left hind paw (Figure-9).
O
N
N
R
R 1
Figure-9
Lee et al. 24 has synthesized some novel pyrimidines derivative having
thiazolidinedione. These compounds were evaluated for their glucose and lipid
lowering activity using pioglitazone and rosiglitazone as reference compound.
Desenko et al. 25 has synthesized azolopyrimidine derivatives and compounds were
evaluated for hypoglycemic activity (Figure-10).
N
N
N
Figure-10
Many pyrimidine ring containing drugs have exhibited antihypertensive
activity. A quinozoline derivative, prazosin, is a selective α1-adrenergic antagonist. 26
Its related analogues bunazosin, 27 trimazosin 28 and terazosin 29 are potent
antihypertensive agents(Figure-11).
O
O
NH 2
N
N
N
N R
Et
R= O
for Prazocin
R= CH 2 OOCH 2 COH(CH 3 ) 2 for Bunazosin
R= COCH 2 CH 2 CH 3 for Trimazosin
O
R=
O
for Terazosin
Figure-11
Ketanserin 30 has a similar effect and is an antagonist of both a1-adrenergic and
serotonin-S2 receptors. A triaminopyrimidine derivative, minoxidil,
Department of Chemistry, Saurashtra university, Rajkot-360005 48