Tag: 200-300

Safety of 2-Phenylpyrazolo[1,5-a]pyridine-3-carboxylic acidOn October 31, 1981 ,《1,3-Dipolar addition of pyridine N-imine to acetylenes and the use of carbon-13 NMR in several structural assignments》 appeared in Journal of Heterocyclic Chemistry. The author of the article were Anderson, Paul L.; Hasak, James P.; Kahle, Alicia D.; Paolella, Nicholas A.; Shapiro, Michael J.. The article conveys some information:

Addition of pyridine N-imine to EtO2CCCR (R = H, Me, Ph) or MeO2CCCCO2Me gave I (same R) or II, resp. Several of the 3-azapyrrocoline esters obtained were further converted into acids, amides and hydrazides. The experimental part of the paper was very detailed, including the reaction process of 2-Phenylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 80537-07-1Safety of 2-Phenylpyrazolo[1,5-a]pyridine-3-carboxylic acid)

2-Phenylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 80537-07-1) 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. Safety of 2-Phenylpyrazolo[1,5-a]pyridine-3-carboxylic acid

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

In 2012,Saini, Vaneet; Sigman, Matthew S. published 《Palladium-Catalyzed 1,1-Difunctionalization of Ethylene》.Journal of the American Chemical Society published the findings.Application of 847818-74-0 The information in the text is summarized as follows:

The 1,1-difunctionalization of ethylene, with aryl/vinyl/heteroaryl transmetalating agents and vinyl electrophiles, is reported. The reaction is high-yielding under a low pressure of ethylene, and regioselectivity is generally high for the 1,1-disubstituted product. The process is highlighted by the use of heteroaromatic cross-coupling reagents, which have not been competent reaction partners in previously reported efforts. The experimental process involved the reaction of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Application of 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, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Application of 847818-74-0

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

Kamal, Ahmed; Tamboli, Jaki R.; Vishnuvardhan, M. V. P. S.; Adil, S. F.; Nayak, V. Lakshma; Ramakrishna, S. published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Synthesis and anticancer activity of heteroaromatic linked 4β-amido podophyllotoxins as apoptotic inducing agents》.Computed Properties of C12H12N2O2 The author mentioned the following in the article:

A series of different heteroaromatic linked 4β-amidopodophyllotoxin conjugates were synthesized and evaluated for anticancer activity against five human cancer cell lines. Among the series, one of the compound I showed significant antiproliferative activity in A549 (lung cancer) cell line. Flow cytometric anal. showed that I arrested the cell cycle in the G2/M phase leading to caspase-3 dependent apoptotic cell death. Further, Hoechst 33258 staining and DNA fragmentation assay also suggests that I induces cell death by apoptosis. The experimental part of the paper was very detailed, including the reaction process of Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate(cas: 192701-73-8Computed Properties of C12H12N2O2)

Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate(cas: 192701-73-8) 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. Computed Properties of C12H12N2O2

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

Akiu, Mayuko; Tsuji, Takashi; Sogawa, Yoshitaka; Terayama, Koji; Yokoyama, Mika; Tanaka, Jun; Asano, Daigo; Sakurai, Ken; Sergienko, Eduard; Sessions, E. Hampton; Gardell, Stephen J.; Pinkerton, Anthony B.; Nakamura, Tsuyoshi published an article in 2021. The article was titled 《Discovery of 1-[2-(1-methyl-1H-pyrazol-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]-3-(pyridin-4-ylmethyl)urea as a potent NAMPT (nicotinamide phosphoribosyltransferase) activator with attenuated CYP inhibition》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.HPLC of Formula: 847818-74-0 The information in the text is summarized as follows:

Nicotinamide phosphoribosyltransferase (NAMPT) catalyzes the rate-limiting step of the NAD+ salvage pathway. Since NAD+ plays a pivotal role in many biol. processes including metabolism and aging, activation of NAMPT is an attractive therapeutic target for treatment of diverse array of diseases. Herein, we report the continued optimization of novel urea-containing derivatives which were identified as potent NAMPT activators. Early optimization of HTS hits afforded compound 12 (I) , with a triazolopyridine core, as a lead compound CYP direct inhibition (DI) was identified as an issue of concern, and was resolved through modulation of lipophilicity to culminate in 1-[2-(1-methyl-1H-pyrazol-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]-3-(pyridin-4-ylmethyl)urea (21, II), which showed potent NAMPT activity accompanied with attenuated CYP DI towards multiple CYP isoforms. The results came from multiple reactions, including the reaction of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0HPLC of Formula: 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. HPLC of Formula: 847818-74-0

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

Wang, Tianqi; Zhang, Rong; Liu, Yang; Fang, Zhen; Zhang, Hailin; Fan, Yan; Yang, Shengyong; Xiang, Rong published an article in 2021. The article was titled 《Discovery of a new class of JMJD6 inhibitors and structure-activity relationship study》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Computed Properties of C10H17BN2O2 The information in the text is summarized as follows:

JmjC domain-containing protein 6 (JMJD6) has been thought as a potential target for various diseases particularly cancer. However, few selective JMJD6 inhibitors have been reported. In this investigation, mol. docking and biol. activity evaluation were performed to retrieve new JMJD6 inhibitors, which led to the identification of a hit compound, J2. Further structural optimization and structure-activity relationship (SAR) anal. towards J2 were carried out, which gave a new potent JMJD6 inhibitor, 7p. This compound showed an IC50 value of 0.681μM against JMJD6, but displayed no activity against other tested JmjC domain-containing protein family members, indicating good selectivity (>100 fold). Collectively, this investigation offers a selective JMJD6 inhibitor, which could be taken as a lead compound for subsequent drug discovery targeting JMJD6. 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: 847818-74-0Computed Properties of C10H17BN2O2)

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, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, monoamine oxidase inhibitory, anti-inflammatory, antidiabetic and antibacterial activities. Computed Properties of C10H17BN2O2

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

In 2016,Tremmel, Tim; Puzik, Andreas; Gehring, Andre P.; Bracher, Franz published 《Canthin-4-ones as Novel Antibacterial Agents》.Archiv der Pharmazie (Weinheim, Germany) published the findings.Safety of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The information in the text is summarized as follows:

Based on the chemotype of canthin-4-one alkaloids with moderate antimicrobial activity, a collection of variously substituted canthin-4-ones and desaza analogs were synthesized. Key steps in the syntheses were regioselective halogenations of (desaza) canthin-4-one, followed by Pd-catalyzed cross-coupling reactions. The in vitro screening for antimicrobial activity revealed that two 5-substituted canthin-4-ones (3-pyridyl, 2-bromophenyl) exhibit significant activity against Streptococcus entericus, coupled with high selectivity and the lack of cytotoxicity against mammalian cells. The intact canthin-4-one ring system was demonstrated to be essential for antibacterial activity. In the experiment, the researchers used many compounds, for example, 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Safety of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole)

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, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, monoamine oxidase inhibitory, anti-inflammatory, antidiabetic and antibacterial activities. Safety of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

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

Sun, Lingyi; Bera, Hriday; Chui, Wai Keung published an article in European Journal of Medicinal Chemistry. The title of the article was 《Synthesis of pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors of thymidine phosphorylase》.Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine The author mentioned the following in the article:

Thymidine phosphorylase (TP) is an enzyme that promotes tumor growth and metastasis and therefore is an attractive druggable target. Using a reported TP inhibitor, 7-deazaxanthine (7DX), as the lead compound; this study was set up to evaluate whether pyrazolo[1,5-a][1,3,5]triazin-2,4-diones and pyrazolo[1,5-a][1,3,5]triazin-2-thioxo-4-ones would exhibit TP inhibitory activity. The pyrazolo[1,5-a][1,3,5]triazine nucleus was constructed using a reaction that annulated the 1,3,5-triazine ring onto a pyrazole scaffold. Among the 52 compounds synthesized and tested, it was found that 1,3-dihydro-pyrazolo[1,5-a][1,3,5]triazin-2-thioxo-4-ones exhibited various extent of inhibitory activity against TP. The best compound I, which bears a para-substituted pentafluorosulfur group, showed an IC50 value of 0.04 μM, which was around 800 times more potent than the 7DX (IC50 = 32 μM) under the same bioassay conditions. The results of the study suggested that a substituent with +σ and +π properties inserted at position 4 of a Ph ring that is attached to position 8 of the pyrazolo[1,5-a][1,3,5]triazin-2-thioxo-4-one scaffold would give excellent TP inhibitory action. In addition, I was found to be a non-competitive inhibitor thus suggested that it might interact with TP at a position different from the substrate binding site. In the experimental materials used by the author, we found 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine(cas: 1015845-73-4Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine)

4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine(cas: 1015845-73-4) belongs to anime. Amines characteristically form salts with acids; a hydrogen ion, H+, adds to the nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral electrophiles (compounds attracted to regions of negative charge) also react with amines; alkyl halides (R′X) and analogous alkylating agents are important examples of electrophilic reagents.Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine

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

Name: N,N-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-propanamineOn October 1, 2008 ,《Optimization of a series of multi-isoform PI3 kinase inhibitors》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Perry, Benjamin; Beevers, Rebekah; Bennett, Gavin; Buckley, George; Crabbe, Tom; Gowers, Lewis; James, Lynwen; Jenkins, Kerry; Lock, Chris; Sabin, Verity; Wright, Sara. The article contains the following contents:

Optimization of the cellular and pharmacol. activity of a novel series of PI3 kinase inhibitors targeting multiple isoforms is described. In addition to this study using N,N-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-propanamine, there are many other studies that have used N,N-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-propanamine(cas: 847818-72-8Name: N,N-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-propanamine) was used in this study.

N,N-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-propanamine(cas: 847818-72-8) 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. Name: N,N-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-propanamine

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

In 2009,Bethel, Paul A.; Gerhardt, Stefan; Jones, Emma V.; Kenny, Peter W.; Karoutchi, Galith I.; Morley, Andrew D.; Oldham, Keith; Rankine, Neil; Augustin, Martin; Krapp, Stephan; Simader, Hannes; Steinbacher, Stefan published 《Design of selective Cathepsin inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.Recommanded Product: 847818-74-0 The information in the text is summarized as follows:

A number of chiral N-[1-(cyanomethylaminocarbonyl)-2-arylethyl]arylamides were synthesized. The mol. recognition features of the products have been exploited in structure-based design of selective Cathepsin inhibitors. The experimental process involved the reaction 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, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, monoamine oxidase inhibitory, anti-inflammatory, antidiabetic and antibacterial activities. Recommanded Product: 847818-74-0

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