Thiazolo[4,5-d]pyrimidine is one of the six structural isomers of the bicyclic
ring system containing thiazole moiety fused with the pyrimidine. There are
six structural isomers depending on the position of the nitrogen atoms. The isomer
[4,5-d] does not contain the bridge-head nitrogen and can be considered as
7-thio analogue of the natural purine bases such as guanine and adenine. Due
to the great of their biological potential the newly synthesized compounds are
evaluated for various pharmacological activities. This review presents numerous
thiazolo[4,5-d]pyrimidine derivatives reported for their interesting biological activity
including antibacterial [2, 3, 5, 7, 8, 10, 19], antifungal [2–6, 9, 10], antiviral
[11–13], analgesic [18, 19], antidepressant [17] and anticancer properties [23–26].
Some urea and thiourea derivatives exhibited significant antiparkinsonian activity
[14–16]. Tumor necrosis factor (TNF) promotes an inflammatory response, which
in turn causes many of the clinical problems associated with autoimmune disorders.
Ethyl 4-(2-amino-5,7-dioxo-3,4,5,7-tetrahydro-thiazolo[4,5-d]pyrimidin-
6(2H)-yl)butanoate derivatives 29 (Fig. 24) as a TNFα inhibitors have a potential
use in the treatment of diseases such as refractory asthma, psoriasis, rheumatoid
arthritis, irritable bowel syndrome, and other [21]. Blocade of the CXCR2 receptor
by thiazolo[4,5-d]pyrimidine-2(3H)-ones also represents an attractive strategy
for treatment of inflammatory diseases [20]. Recently there have been developed
CX3CR1 receptor antagonists for the treatment of multiple sclerosis [22]. Isatoribine,
5-amino-3-β-D-ribofuranosyl-3H-thiazolo[4,5-d]pyrimidin-2-one (20) (Fig.
15) is a small molecule toll-like receptor 7 (TLR7) agonist and an activator of innate
immunity. Its orally bioavailable analogue ANA 975 (Fig. 16) has been reported for
probable use in treating disease states associated with abnormal cell growth, such
as cancer and has anti HCV activity [13]. Thiazolo[4,5-d]pyrimidines inhibit the
growth of the weeds which implies that they have a potential as herbicides [27].
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