33149-25-6

Upstream product

• 29274-13-3 5-phenyl-4H-pyrazolo<1,5-a>pyrimidin-7-one 
• 94-02-0 ethyl 3-oxo-3-phenylpropionate 
• 1225387-53-0 3⁽⁵⁾-aminopyrazole 

Downstream Products

• 77493-98-2 5-Phenyl-4H-pyrazolo[1,5-a]pyrimidine-7-thione 
• 244127-47-7 4'-<(5-phenylpyrazolo<1,5-a>pyrimidin-7-yl)aminomethyl>biphenyl-2-carbonitrile 
• 672323-74-9 3-bromo-7-chloro-5-phenyl-pyrazolo[1,5-a]pyrimidine 
• 672325-78-9 C₁₈H₁₅N₅ 
• 672324-27-5 C₁₃H₈ClN₃O 
• 1112915-16-8 7-(1H-imidazol-4-yl)-5-phenyl-pyrazolo[1,5-a]pyrimidine 
• 1112915-10-2 7-(1H-indol-3-yl)-5-phenyl-pyrazolo[1,5-a]pyrimidine 
• 1112915-13-5 7-(1-methyl-1H-indol-3-yl)-5-phenyl-pyrazolo[1,5-a]pyrimidine 
• 1112914-98-3 5-methoxy-2-(5-phenyl-pyrazolo[1,5-a]pyrimidin-7-yl)-phenol 
• 1112914-91-6 5-phenyl-7-(2,4,6-trimethoxy-phenyl)-pyrazolo[1,5-a]pyrimidine 
• 1112915-04-4 4-(5-phenyl-pyrazolo[1,5-a]pyrimidin-7-yl)-naphthalen-1-ol 
• 1112914-93-8 2-methyl-4-(5-phenyl-pyrazolo[1,5-a]pyrimidin-7-yl)-benzene-1,3-diol 
• 1112915-07-7 7-(4-methoxy-naphthalen-1-yl)-5-phenyl-pyrazolo[1,5-a]pyrimidine 
• 1112915-01-1 7-(2,4-dimethoxy-phenyl)-5-phenyl-pyrazolo[1,5-a]pyrimidine 

Relevant academic research and scientific papers

Structural Insights into the Inhibition of Undecaprenyl Pyrophosphate Synthase from Gram-Positive Bacteria

The polyprenyl lipid undecaprenyl phosphate (C55P) is the universal carrier lipid for the biosynthesis of bacterial cell wall polymers. C55P is synthesized in its pyrophosphate form by undecaprenyl pyrophosphate synthase (UppS), an essentialcis-prenyltransferase that is an attractive target for antibiotic development. We previously identified a compound (MAC-0547630) that showed promise as a novel class of inhibitor and an ability to potentiate β-lactam antibiotics. Here, we provide a structural model for MAC-0547630’s inhibition of UppS and a structural rationale for its enhanced effect on UppS fromBacillus subtilisversusStaphylococcus aureus. We also describe the synthesis of a MAC-0547630 derivative (JPD447), show that it too can potentiate β-lactam antibiotics, and provide a structural rationale for its improved potentiation. Finally, we present an improved structural model of clomiphene’s inhibition of UppS. Taken together, our data provide a foundation for structure-guided drug design of more potent UppS inhibitors in the future.

In silico design of novel probes for the atypical opioid receptor MRGPRX2

The primate-exclusive MRGPRX2 G protein-coupled receptor (GPCR) has been suggested to modulate pain and itch. Despite putative peptide and small-molecule MRGPRX2 agonists, selective nanomolar-potency probes have not yet been reported. To identify a MRGPRX

The identification of GPR3 inverse agonist AF64394; The first small molecule inhibitor of GPR3 receptor function

The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported.

Evaluation of novel 7-(hetero)aryl-substituted pyrazolo[1, 5-a]pyrimidines as phosphodiesterase-4 inhibitors

A novel series of 7-(hetero)aryl substituted-pyrazolopyrimidines, prepared via an AlCl3 induced C-C bond forming reaction of 7-chloro-5-phenyl-pyrazolo[1,5-a]pyrimidine with arenes and heteroarenes have been investigated as PDE4 inhibitors. Amo

Reactivity of the -C(Cl){double bond, long}C-C{double bond, long}N- moiety towards AlCl3-induced C-C bond forming reactions: a new synthesis of 7-(hetero)aryl-substituted pyrazolo[1,5-a]pyrimidines

The reactivity of the -C(Cl){double bond, long}C-C{double bond, long}N- moiety towards an AlCl3-induced C-C bond forming reaction was investigated through the reaction of 7-chloro-5-phenyl-pyrazolo[1,5-a]pyrimidine with arenes and heteroarenes.

Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors

A series of four bicyclic cores were prepared and evaluated as cyclin-dependent kinase-2 (CDK2) inhibitors. From the in-vitro and cell-based analysis, the pyrazolo[1,5-a]pyrimidine core (represented by 9) emerged as the superior core for further elaboration in the identification of novel CDK2 inhibitors.

Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2

Properly substituted pyrazolo[1,5-a]pyrimidines are potent and selective CDK2 inhibitors. Compound 15j is orally available and showed efficacy in a mouse A2780 xenograft model.

PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.