pyrazoles-derivatives

In 2012,Manchester, John I.; Dussault, Daemian D.; Rose, Jonathan A.; Boriack-Sjodin, P. Ann; Uria-Nickelsen, Maria; Ioannidis, Georgine; Bist, Shanta; Fleming, Paul; Hull, Kenneth G. published 《Discovery of a novel azaindole class of antibacterial agents targeting the ATPase domains of DNA gyrase and Topoisomerase IV》.Bioorganic & Medicinal Chemistry Letters published the findings.Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazole The information in the text is summarized as follows:

The discovery and optimization of a series of bacterial topoisomerase inhibitors, e.g., I, is disclosed. Starting from a virtual screening hit, activity was optimized through a combination of structure-based design and phys. property optimization. Synthesis of fewer than a dozen compounds was required to achieve inhibition of the growth of methicillin-resistant Staphyloccus aureus at compound concentrations of 1.56 μM. These compounds simultaneously inhibit DNA gyrase and Topoisomerase IV at similar nanomolar concentrations, reducing the likelihood of the spontaneous occurrence of target-based mutations resulting in antibiotic resistance, an increasing threat in the treatment of serious infections. In the part of experimental materials, we found many familiar compounds, such as 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazole)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazole

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

In 2014,Chekler, Eugene L. Piatnitski; Unwalla, Rayomond; Khan, Taukeer A.; Tangirala, Raghuram S.; Johnson, Mark; St. Andre, Michael; Anderson, James T.; Kenney, Thomas; Chiparri, Sue; McNally, Chris; Kilbourne, Edward; Thompson, Catherine; Nagpal, Sunil; Weber, Gregory; Schelling, Scott; Owens, Jane; Morris, Carl A.; Powell, Dennis; Verhoest, Patrick R.; Gilbert, Adam M. published 《1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)indoline-4-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators》.Journal of Medicinal Chemistry published the findings.Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazole The information in the text is summarized as follows:

We present a novel series of selective androgen receptor modulators (SARMs) which shows excellent biol. activity and phys. properties. 1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)-indoline-4-carbonitriles showed potent binding to the androgen receptor (AR) and activated AR-mediated transcription in vitro. Representative compounds demonstrated diminished activity in promoting the intramol. interaction between the AR carboxyl (C) and amino (N) termini. This N/C-termini interaction is a biomarker assay for the undesired androgenic responses in vivo. In orchidectomized rats, daily administration of a lead compound from this series showed anabolic activity by increasing levator ani muscle weight Importantly, minimal androgenic effects (increased tissue weights) were observed in the prostate and seminal vesicles, along with minimal repression of circulating LH (LH) levels and no change in the lipid and triglyceride levels. This lead compound completed a two week rat toxicol. study, and was well tolerated at doses up to 100 mg/kg/day, the highest dose tested, for 14 consecutive days. In the experiment, the researchers used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazole)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazole

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

In 2015,Burdick, Daniel J.; Wang, Shumei; Heise, Christopher; Pan, Borlan; Drummond, Jake; Yin, JianPing; Goeser, Lauren; Magnuson, Steven; Blaney, Jeff; Moffat, John; Wang, Weiru; Chen, Huifen published 《Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.Reference of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The information in the text is summarized as follows:

A fragment-based lead discovery approach was used to discover novel ERK2 inhibitors. The crystal structure of N-benzyl-9H-purin-6-amine (compound 1) in complex with ERK2 elucidated its hinge-binding mode. In addition, the simultaneous binding of an imidazole mol. adjacent to (1) suggested a direction for fragment expansion. Structure-based core hopping applied to (1) led to 5H-pyrrolo[3,2-b]pyrazine that afforded direct vectors to probe the pockets of interest while retaining the essential hinge binding elements. Utilizing the new vectors for SAR exploration, the new core (I) was quickly optimized to 7-(1-benzyl-1H-pyrazol-4-yl)-2-(pyridin-4-yl)-5H-pyrrolo[3,2-b]pyrazine (compound 39) resulting in a greater than 6600-fold improvement in potency. In the part of experimental materials, we found many familiar compounds, such as 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Reference of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole)

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) 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. Reference of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

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

In 2018,International Journal of Molecular Sciences included an article by Dago, Camille D.; Le Maux, Paul; Roisnel, Thierry; Brigaudeau, Christophe; Bekro, Yves-Alain; Mignen, Olivier; Bazureau, Jean-Pierre. Related Products of 20154-03-4. The article was titled 《Preliminary structure-activity relationship (SAR) of a novel series of pyrazole SKF-96365 analogues as potential store-operated calcium entry (SOCE) inhibitors》. The information in the text is summarized as follows:

From a series of [β-(phenylalkoxy)-(phenethyl)]-1H-pyrazolium hydrochloride as new analogs of SKF-96365, one has an interesting effect for endoplasmic reticulum (ER) Ca2+ release and store-operated Ca2+ entry (SOCE)(IC50 25 μM) on the PLP-B lymphocyte cell line. A successful resolution of (±) 1-phenyl-2-(1H-pyrazol-1-yl)ethan-1-ol was developed by using the method of “”half-concentration”” in the presence of (+)-(1S)- or (-)-(1R)-CSA. After reading the article, we found that the author used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Related Products of 20154-03-4)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.Related Products of 20154-03-4

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

《Metabolically stable diphenylamine derivatives suppress androgen receptor and BET protein in prostate cancer》 was published in Biochemical Pharmacology (Amsterdam, Netherlands) in 2020. These research results belong to Yu, Jiang; Zhou, Peiting; Du, Wu; Xu, Ruixue; Yan, Guoyi; Deng, Yufang; Li, Xinghai; Chen, Yuanwei. Recommanded Product: 847818-74-0 The article mentions the following:

Androgen receptor (AR) is a crucial driver of prostate cancer (PC). AR-relevant resistance remains a major challenge in castration-resistant prostate cancer (CRPC). Bromodomain and extra-terminal domain (BET) family are critical AR coregulators. Here, we developed several diphenylamine derivatives and identified compound 7d that disrupted the functions of AR and BET family in prostate cancer and exhibited favorable metabolic stability in vitro and high drug exposure in vivo. We showed 7d not only bound to AR, suppressed transactivation of wild-type AR (wt-AR) and the mutant that mediates Enzalutamide resistance, but also reduced c-Myc protein expression through BET inhibition. In addition, 7d inhibited the proliferation of AR-pos. PC cells with favorable selectivity and suppressed AR-V7-expressing VCaP and 22Rv1 xenografts growth in vivo. Collectively, these results indicate the potential of lead compound 7d as an orally available AR and BET inhibitor to treat CRPC and overcome antiandrogen resistance. 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: 847818-74-0Recommanded 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, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Recommanded Product: 847818-74-0

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

HPLC of Formula: 20154-03-4In 2016 ,《Inhibitors of HIV-1 attachment: The discovery and structure-activity relationships of tetrahydroisoquinolines as replacements for the piperazine benzamide in the 3-glyoxylyl 6-azaindole pharmacophore》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Swidorski, Jacob J.; Liu, Zheng; Yin, Zhiwei; Wang, Tao; Carini, David J.; Rahematpura, Sandhya; Zheng, Ming; Johnson, Kim; Zhang, Sharon; Lin, Pin-Fang; Parker, Dawn D.; Li, Wenying; Meanwell, Nicholas A.; Hamann, Lawrence G.; Regueiro-Ren, Alicia. The article contains the following contents:

6,6-Fused ring systems including tetrahydroisoquinolines and tetrahydropyrido[3,4-d]pyrimidines have been explored as possible replacements for the piperazine benzamide portion of the HIV-1 attachment inhibitor BMS-663068. In initial studies, the tetrahydroisoquinoline compounds demonstrate sub-nanomolar activity in a HIV-1 pseudotype viral infection assay used as the initial screen for inhibitory activity. Anal. of SARs and approaches to optimization for an improved drug-like profile are examined herein. The results came from multiple reactions, including the reaction of 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4HPLC of Formula: 20154-03-4)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.HPLC of Formula: 20154-03-4

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

Recommanded Product: 844501-71-9In 2012 ,《Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Curtin, Michael L.; Frey, Robin R.; Heyman, H. Robin; Soni, Niru B.; Marcotte, Patrick A.; Pease, Lori J.; Glaser, Keith B.; Magoc, Terrance J.; Tapang, Paul; Albert, Daniel H.; Osterling, Donald J.; Olson, Amanda M.; Bouska, Jennifer J.; Guan, Zhiwen; Preusser, Lee C.; Polakowski, James S.; Stewart, Kent D.; Tse, Chris; Davidsen, Steven K.; Michaelides, Michael R.. The article contains the following contents:

In an effort to identify multi-targeted kinase inhibitors with a novel spectrum of kinase activity, a screen of Abbott proprietary KDR inhibitors against a broad panel of kinases was conducted and revealed a series of thienopyridine ureas with promising activity against the Aurora kinases. Modification of the di-Ph urea and C7 moiety of these compounds provided potent inhibitors with good pharmacokinetic profiles that were efficacious in mouse tumor models after oral dosing. Compound 2 (ABT-348) of this series is currently undergoing Phase I clin. trials in solid and hematol. cancer populations.3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Recommanded Product: 844501-71-9) was used in this study.

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Recommanded Product: 844501-71-9

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

Electric Literature of C12H13N3O2On May 15, 2015 ,《Synthetic studies of five-membered heteroaromatic derivatives as potassium-competitive acid blockers (P-CABs)》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Arikawa, Yasuyoshi; Hasuoka, Atsushi; Nishida, Haruyuki; Hirase, Keizo; Inatomi, Nobuhiro; Takagi, Terufumi; Tarui, Naoki; Kawamoto, Makiko; Imanishi, Akio; Itoh, Fumio; Kajino, Masahiro. The article conveys some information:

On the basis of a series of novel and potent potassium-competitive acid blockers represented by 1-sulfonylpyrrole derivative I, we prepared several five-membered heterocyclic analogs II [Ht = S, N, O containing heterocycle] and evaluated their H+,K+-ATPase activities in vitro. We also assessed the role of the methylaminomethyl side chain by comparison with methylamino and ethylamino derivatives We observed that the five-membered core ring and its orientation affect inhibitory activity and that the methylaminomethyl moiety is the best side chain. On the basis of potency and ligand-lipophilicity efficiency, compound I remains the most drug-like of the compounds studied to date. This study revealed the factors necessary for potent H+,K+-ATPase inhibition, such as differences in electron d., the properties of the lone pair at each apical position of the heteroaromatic ring, and the geometry of the substituents. After reading the article, we found that the author used Ethyl 5-amino-1-phenyl-1H-pyrazole-3-carboxylate(cas: 866837-96-9Electric Literature of C12H13N3O2)

Ethyl 5-amino-1-phenyl-1H-pyrazole-3-carboxylate(cas: 866837-96-9) belongs to anime. Reaction with nitrous acid (HNO2), which functions as an acylating agent that is a source of the nitrosyl group (―NO), converts aliphatic primary amines to nitrogen and mixtures of alkenes and alcohols corresponding to the alkyl group in a complex process. This reaction has been used for analytical determination of primary amino groups in a procedure known as the Van Slyke method.Electric Literature of C12H13N3O2

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

In 2014,Ojeda-Gomez, Claudia; Pessoa-Mahana, Hernan; Iturriaga-Vasquez, Patricio; Pessoa-Mahana, Carlos David; Recabarren-Gajardo, Gonzalo; Mendez-Rojas, Claudio published 《Synthesis and Biological Screening of Novel Indolalkyl Arenes Targeting the Serotonin Transporter》.Archiv der Pharmazie (Weinheim, Germany) published the findings.Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazole The information in the text is summarized as follows:

A series of functionalized indolylalkylarenes were synthesized and their affinities for the serotonin transporter were investigated in vitro. Compounds I (R = H, F; R’ = 4-CF3Ph, 2-FBn, PhCH2CH2) were obtained by nucleophilic substitution of 3-(1H-indol-3-yl)propyl-4-methylbenzenesulfonates with a series of azaheterocycles. Compounds II (R = H, F; R’ = H, Cl, NO2) were prepared in a two-step sequence by reaction of 3-(1H-indol-3-yl)-2-methylpropanal with substituted 1,2-phenylenediamines. Compounds I (R = F; R’ = 4-CF3Ph, 2-FBn, PhCH2CH2) showed good binding affinities (Ki = 33.0, 48.0, and 17 nM, resp.). The other synthesized compounds showed moderate or no affinity in the binding studies. The experimental part of the paper was very detailed, including the reaction process of 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazole)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Recommanded Product: 3-(Trifluoromethyl)-1H-pyrazole

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

In 2015,Parsy, Christophe C.; Alexandre, Francois-Rene; Bidau, Valerie; Bonnaterre, Florence; Brandt, Guillaume; Caillet, Catherine; Cappelle, Sylvie; Chaves, Dominique; Convard, Thierry; Derock, Michel; Gloux, Damien; Griffon, Yann; Lallos, Lisa B.; Leroy, Frederic; Liuzzi, Michel; Loi, Anna-Giulia; Moulat, Laure; Chiara, Musiu; Roques, Virginie; Rosinovsky, Elodie; Savin, Simon; Seifer, Maria; Standring, David; Surleraux, Dominique published 《Discovery and structural diversity of the hepatitis C virus NS3/4A serine protease inhibitor series leading to clinical candidate IDX320》.Bioorganic & Medicinal Chemistry Letters published the findings.Electric Literature of C4H3F3N2 The information in the text is summarized as follows:

Exploration of the P2 region by mimicking the proline motif found in BILN2061 resulted in the discovery of two series of potent HCV NS3/4A protease inhibitors. X-ray crystal structure of the ligand in contact with the NS3/4A protein and modulation of the quinoline heterocyclic region by structure based design and modeling allowed for the optimization of enzyme potency and cellular activity. This research led to the selection of clin. candidate IDX320 having good genotype coverage and pharmacokinetic properties in various species. After reading the article, we found that the author used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Electric Literature of C4H3F3N2)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Electric Literature of C4H3F3N2

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