Zhang, Xiaojun’s team published research in Journal of Medicinal Chemistry in 2016 | CAS: 847818-74-0

1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) 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. Recommanded Product: 847818-74-0

In 2016,Zhang, Xiaojun; Glunz, Peter W.; Johnson, James A.; Jiang, Wen; Jacutin-Porte, Swanee; Ladziata, Vladimir; Zou, Yan; Phillips, Monique S.; Wurtz, Nicholas R.; Parkhurst, Brandon; Rendina, Alan R.; Harper, Timothy M.; Cheney, Daniel L.; Luettgen, Joseph M.; Wong, Pancras C.; Seiffert, Dietmar; Wexler, Ruth R.; Priestley, E. Scott published 《Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex》.Journal of Medicinal Chemistry published the findings.Recommanded Product: 847818-74-0 The information in the text is summarized as follows:

Inhibitors of the tissue factor (TF)/factor VIIa complex (TF-FVIIa) are promising novel anticoagulants, which show excellent efficacy and minimal bleeding in preclin. models. Starting with an aminoisoquinoline P1-based macrocyclic inhibitor, optimization of the P’ groups led to a series of highly potent and selective TF-FVIIa inhibitors, which displayed poor permeability. Fluorination of the aminoisoquinoline reduced the basicity of the P1 group and significantly improved permeability. The resulting lead compound I was highly potent, selective, and achieved good pharmacokinetics in dogs with oral dosing. Moreover, it demonstrated robust antithrombotic activity in a rabbit model of arterial thrombosis. The experimental part of the paper was very detailed, including the reaction process of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Recommanded Product: 847818-74-0)

1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) 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. Recommanded Product: 847818-74-0

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