Thiazolo[4,5-d]pyrimidine thiones and -ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists

Microwave-Assisted Synthesis of Bioactive Six-Membered Heterocycles and Their Fused Analogues

“…The use of MW activation improved the product yields and significantly shortened the reaction times related to a conventional heating. This green cyclization protocol required neither organic solvent for the reaction or purification of final compounds [158][159][160].…”

“…The use of MW activation improved the product yields and significantly shortened the reaction times related to a conventional heating. This green cyclization protocol required neither organic solvent for the reaction or purification of final compounds [158][159][160]. An elegant protocol for the synthesis of substituted 3,4-dihydropyrimidin-2(1H)-ones 167 under MW-irradiation has been highlighted by Varma et al [161].…”

The “homeostasis hormone” and its CRF1 receptor. From structure to function

“…114 Substitution of noncyclic diamino groups in R1 position was found to increase the binding affinity of CRF for the human CRF1 receptor compared to the cyclic amino group (e.g. morpholine).…”

Synthesis andin vitro evaluation of the anticancer activity of novel fluorinated thiazolo[4, 5-d]pyrimidines

“…Introduction Thiazolo[4,pyrimidines can be considered as thiaanalogues of the naturally occurring purine bases, adenine and guanine, due to the insertion of a sulphur atom in the place of the nitrogen atom at position 7 of the purine ring.These compounds have acquired a growing importance as anticancer immunotherapeutic agents [1], antiviral agents used in the treatment of human cytomegalovirus (HCMV) [2][3][4][5][6], antitumour [7] and antibacterial agents [8]. Recently they have been found to strongly antagonise the activity of the corticotropin releasing factor (CRF) and thus have the potential to be CNS active agents [9,10]. Thiazolo [4,5-d]pyrimidines have also been reported to have antidepressive activity [11].…”

“…Thiazolo [4,5-d]pyrimidines have also been reported to have antidepressive activity [11]. Many of these compounds are therefore of interest to major pharmaceutical companies [3][4][5][6][9][10][11]. …”