Category: 945376-95-4

Hu, Yue; Dong, Yao-Dong; Wu, Yan-Chao; Wang, Qiu-Xu; Nan, Xiang; Wang, Da-Li published their research in Bioorganic & Medicinal Chemistry on December 15 ,2021. The article was titled 《AMPK inhibitor BML-275 induces neuroprotection through decreasing cyt c and AIF expression after transient brain ischemia》.HPLC of Formula: 945376-95-4 The article contains the following contents:

Stroke is a major public health problem with an imperative need for a more effective and tolerated therapy. Neuroprotective therapy may be an effective therapeutic intervention for stroke. The morbidity and mortality of stroke-induced secondary brain injury is mainly caused by neuronal apoptosis, which can be executed in a caspase-dependent or apoptosis inducing factor (AIF)-dependent manner. As apoptosis is an energy-dependent process with a relative time delay, abnormal energy metabolism could be a significant and fundamental pathophysiol. basis of stroke. To our knowledge, convincible evidences that AMPK inhibition exerts neuroprotection in cerebral ischemia injury via anti-apoptosis remain to be investigated. Accordingly, the aims of this study were to investigate the protective effects of AMPK inhibitor BML-275 on cerebral ischemic/reperfusion (I/R) injury and to elucidate the underlying mechanisms. Cerebral ischemia was induced by transient middle cerebral artery occlusion (tMCAO) in male C57BL/6 mice. The therapeutic effects of BML-275 were evaluated by infarct sizes, neurol. scores and the proportion of apoptotic neurons after 24 h of reperfusion. The cell apoptosis markers cyt c and AIF were also evaluated. The results showed that i.p. administration of BML-275 alleviate the cerebral infarction, neurol. deficit and neuronal apoptosis induced by MCAO. BML-275 simultaneously induces anti-apoptosis and decreases the expression of cyt c and AIF. This study supports the hypothesis that anti-apoptosis is one of potential neuroprotective strategies for the treatment of stroke. In the experiment, the researchers used many compounds, for example, 4-(3-Bromopyrazolo[1,5-a]pyrimidin-6-yl)phenol(cas: 945376-95-4HPLC of Formula: 945376-95-4)

4-(3-Bromopyrazolo[1,5-a]pyrimidin-6-yl)phenol(cas: 945376-95-4) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. HPLC of Formula: 945376-95-4

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

《Design and Synthesis of Minimalist Terminal Alkyne-Containing Diazirine Photo-Crosslinkers and Their Incorporation into Kinase Inhibitors for Cell- and Tissue-Based Proteome Profiling》 was published in Angewandte Chemie, International Edition in 2013. These research results belong to Li, Zhengqiu; Hao, Piliang; Li, Lin; Tan, Chelsea Y. J.; Cheng, Xiamin; Chen, Grace Y. J.; Sze, Siu Kwan; Shen, Han-Ming; Yao, Shao Q.. COA of Formula: C12H8BrN3O The article mentions the following:

A minimalist clickable photo-crosslinker was incorporated with numerous small-mol. kinase inhibitors. The resulting probes were used for both in vitro (cell lysates) and in situ (live cells) proteome profiling, for large-scale identification of their potential cellular kinase targets and shows improved outcomes over previous probes. In the experimental materials used by the author, we found 4-(3-Bromopyrazolo[1,5-a]pyrimidin-6-yl)phenol(cas: 945376-95-4COA of Formula: C12H8BrN3O)

4-(3-Bromopyrazolo[1,5-a]pyrimidin-6-yl)phenol(cas: 945376-95-4) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. COA of Formula: C12H8BrN3O

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Synthetic Route of C12H8BrN3OOn November 15, 2010 ,《The rational design of a novel potent analogue of the 5′-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Machrouhi, Fouzia; Ouhamou, Nouara; Laderoute, Keith; Calaoagan, Joy; Bukhtiyarova, Marina; Ehrlich, Paula J.; Klon, Anthony E.. The article conveys some information:

We have designed and synthesized analogs of compound C, [4-(2-piperidinyl-1-ylethoxy)phenyl]-3-(4-pyridinyl)pyrazolo[1,5-a]pyrimidine, a non-specific inhibitor of 5′-AMP-activated protein kinase (AMPK), using a computational fragment-based drug design (FBDD) approach. Synthesizing only twenty-seven analogs yielded a compound that was equipotent to compound C in the inhibition of the human AMPK (hAMPK) α2 subunit in the heterotrimeric complex in vitro, exhibited significantly improved selectivity against a subset of relevant kinases, and demonstrated enhanced cellular inhibition of AMPK. The experimental process involved the reaction of 4-(3-Bromopyrazolo[1,5-a]pyrimidin-6-yl)phenol(cas: 945376-95-4Synthetic Route of C12H8BrN3O)

4-(3-Bromopyrazolo[1,5-a]pyrimidin-6-yl)phenol(cas: 945376-95-4) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Synthetic Route of C12H8BrN3O

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics