Aktywność biologiczna pochodnych tiazolo[4,5-d]pirymidyny
Journal Title: Wiadomości Chemiczne - Year 2013, Vol 67, Issue 11
Abstract
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].
Authors and Affiliations
Lilianna Becan
Keywords
Related Articles
- EP ID EP587070
- DOI -
- Views 137
- Downloads 0
Syntezy i aktywność biologiczna wybranych zasad Mannicha
The Mannich reaction is important for the synthesis and modification of biologically active compounds. Mannich bases – substituted products containing different heterocyclic system in their structures seem to be suitable...
Hiperwalentne związki siarki, selenu i telluru. Część 4. Selenurany i tellurany
In this part selenuranes (10-Se-4 and 10-Se-5) and perselenuranes 12-Se-6 as well as telluranes 10-Te-4 and pertelluranes 12-Te-6 will be presented. The main goal is to describe recent reports on the synthesis, chemical,...
Nanomaszyny molekularne
The work discusses the beginning of nanotechnology, mentions its creators and tells about breakthrough discoveries that contributed to its developments as a science. Next, the focus was on several of the most important n...
Analiza rozmieszczenia pierwiastków w badaniach archeometrycznych z zastosowaniem mikropróbkowania laserowego w spektrometrii mas z jonizacją w plazmie indukcyjnie sprzężonej
Laser Ablation Inductively Coupled Plasma Mass Spectrometry (LA-ICP-MS) is one of modern instrumental methods, which use in elemental analysis of cultural heritage objects has recently noticeably increased. The method re...
Równowagi asocjacyjne alkilopochodnych mocznika i tiomocznika
The studies and comparison of a series of molecular mono- and di-substituted derivatives of urea and thiourea in solvents of increasing polarity are presented [1–4]. These substances are characterized by a high tendency...