259103-38-3

Upstream product

• 259100-47-5 2-Amino-5-[(phenylmethyl)thio]thiazolo[4,5-d]pyrimidin-7(4H)-one 
• 100-39-0 benzyl bromide 
• 259103-40-7 6-amino-1,4-dihydro-4-oxo-2-[(phenylmethyl)thio]-5-pyrimidinyl ester thiocyanic acid 
• 37660-23-4 6-Amino-2-[(phenylmethyl)thio]-4(1H)-pyrimidinone 
• 259103-40-7 {[4-amino-2-(benzylsulfanyl)-6-hydroxypyrimidin-5-yl]sulfanyl}formonitrile 
• 259100-47-5 2-amino-5-(benzylsulfanyl)[1,3]thiazolo[4,5-d]pyrimidin-7-ol 
• 37660-23-4 4-amino-2-(benzylthio)-6-hydroxypyrimidine 

Downstream Products

• 849943-17-5 (2R)-2-{[2-amino-5-(benzylsulfanyl)-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino}pentan-1-ol 
• 259101-61-6 2-[[2-Amino-5-[(phenylmethyl)thio]thiazolo[4,5-d]pyrimidin-7-yl]amino]-2-methyl-1-propanol 
• 259102-55-1 2-Bromo-7-chloro-5-[(phenylmethyl)thio]-thiazolo[4,5-d]pyrimidine 
• 463954-22-5 C₁₉H₂₂N₆OS₂ 
• 849943-54-0 5-(benzylthio)-7-{[(1R)-1-(hydroxymethyl)-3-methylbutyl]amino}[1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one 
• 463954-10-1 C₁₉H₂₅N₅O₂S₂ 
• 463953-96-0 C₁₈H₂₂BrN₅OS₂ 
• 1429127-81-0 (2R)-2-{[5-(benzylsulfanyl)-2-chloro[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino}-4-methylpentan-1-ol 
• 849943-53-9 (2R)-2-{[5-(benzylsulfanyl)-2-methoxy[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino}-4-methylpentan-1-ol 
• 463954-25-8 C₁₉H₂₂N₆OS₂ 
• 463953-97-1 C₁₈H₂₂BrN₅OS₂ 
• 463954-19-0 C₁₉H₂₂N₆OS₂ 
• 463954-06-5 C₁₈H₂₁BrFN₅OS₂ 
• 849943-60-8 C₁₉H₂₅N₅OS₂ 

Relevant academic research and scientific papers

PB-10, a thiazolo[4,5-d] pyrimidine derivative, targets p21-activated kinase 4 in human colorectal cancer cells

Targeting p21-activated kinase 4 (PAK4) is a potential therapeutic strategy against human colorectal cancer (CRC). In this study, we synthesized a series of novel thiazolo[4,5-d]pyrimidine derivatives (PB-1–12) and identified PB-10 (PAK4 IC50 = 15.12 μM) as a potential and potent PAK4 inhibitor. Our results showed that PB-10 significantly suppressed the proliferation and colony formation of human CRC cells. PB-10 also arrested HCT-116 CRC cells at sub G0/G1 phase while promoting the expression of proapoptotic proteins. In addition, PB-10 inhibited migration, invasion, and adhesion as well as the PAK4 downstream signaling pathway in HCT-116 cells. Molecular docking analysis showed possible binding modes between PB-10 and PAK4. Our study provides a novel compound that may block the PAK4 signaling in CRC cells.

Synthesis and preliminary biological evaluation of [11C]methyl (2-amino-5-(benzylthio)thiazolo[4,5-d]pyrimidin-7-yl)-D-leucinate for the fractalkine receptor (CX3CR1)

The reference standard methyl (2-amino-5-(benzylthio)thiazolo[4,5-d]pyrimidin-7-yl)-D-leucinate (5) and its precursor 2-amino-5-(benzylthio)thiazolo[4,5-d]pyrimidin-7-yl)-D-leucine (6) were synthesized from 6-amino-2-mercaptopyrimidin-4-ol and BnBr with o

Substituted 7-amino-5-thio-thiazolo[4,5- d ]pyrimidines as potent and selective antagonists of the fractalkine receptor (CX3CR1)

We have developed two parallel series, A and B, of CX3CR1 antagonists for the treatment of multiple sclerosis. By modifying the substituents on the 7-amino-5-thio-thiazolo[4,5-d]pyrimidine core structure, we were able to achieve compounds with high selectivity for CX3CR1 over the closely related CXCR2 receptor. The structure-activity relationships showed that a leucinol moiety attached to the core-structure in the 7-position together with α-methyl branched benzyl derivatives in the 5-position displayed promising affinity, and selectivity as well as physicochemical properties, as exemplified by compounds 18a and 24h. We show the preparation of the first potent and selective orally available CX3CR1 antagonists.

NOVEL 5,7-DISUBSTITUTED [1,3]THIAZOLO[4,5-D]PYRIMIDIN-2(3H)-ONE DERIVATIVES

There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, R4 and R5 are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.

Hit-to-Lead studies: The discovery of potent, orally bioavailable thiazolopyrimidine CXCR2 receptor antagonists

A Hit-to-Lead optimisation programme was carried out on a high throughput screening hit, the thiazolopyrimidine 1, resulting in the discovery of the potent, orally bioavailable CXCR2 antagonist 29.

Thiazolo (4,5-D) pyrimidine compounds

The invention provides certain thiazolopyrimidine compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof; processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therap

Thiazolopyrimidines and thier use as modulators of chemokine receptor activity

The invention provides certain thiazolopyrimidine compound, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

NOVEL THIAZOLOPYRIMIDINE COMPOUNDS

The invention provides certain thiazolopyrimidine compounds, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.