Month: February 2023

Chemical Proteomic Profiling of Bromodomains Enables the Wide-Spectrum Evaluation of Bromodomain Inhibitors in Living Cells was written by Li, Xin;Wu, Yizhe;Tian, Gaofei;Jiang, Yixiang;Liu, Zheng;Meng, Xianbin;Bao, Xiucong;Feng, Ling;Sun, Hongyan;Deng, Haiteng;Li, Xiang David. And the article was included in Journal of the American Chemical Society in 2019.Synthetic Route of C4H3Cl2N3 This article mentions the following:

Bromodomains, epigenetic “readers” of lysine acetylation marks, exist in different nuclear proteins with diverse biol. functions in chromatin biol. Malfunctions of bromodomains are associated with the pathogenesis of human diseases, such as cancer. Bromodomains have therefore emerged as therapeutic targets for drug discovery. Given the high structural similarity of bromodomains, a critical step in the development of bromodomain inhibitors is the evaluation of their selectivity to avoid off-target effects. While numerous bromodomain inhibitors have been identified, new methods to evaluate the inhibitor selectivity toward endogenous bromodomains in living cells remain needed. Here we report the development of a photoaffinity probe, photo-bromosporine (photo-BS), that enables the wide-spectrum profiling of bromodomain inhibitors in living cells. Photo-BS allowed light-induced crosslinking of recombinant bromodomains and endogenous bromodomain-containing proteins (BCPs) both in vitro and in living cells. The photo-BS-induced labeling of the bromodomains was selectively competed by the corresponding bromodomain inhibitors. Proteomics anal. revealed that photo-BS captured 28 out of the 42 known BCPs from the living cells. Assessment of the two bromodomain inhibitors, bromosporine and GSK6853, resulted in the identification of known as well as previously uncharacterized bromodomain targets. Collectively, we established a chem. proteomics platform to comprehensively evaluate bromodomain inhibitors in terms of their selectivity against endogenous BCPs in living cells. In the experiment, the researchers used many compounds, for example, 4-Amino-3,6-dichloropyridazine (cas: 823-58-5Synthetic Route of C4H3Cl2N3).

4-Amino-3,6-dichloropyridazine (cas: 823-58-5) belongs to pyridazine derivatives. Pyridazines are rare in nature, possibly reflecting the scarcity of naturally occurring hydrazines, common building blocks for the synthesis of these heterocycles. The unsubstituted pyridazines are more resistant to eletrophilic substitution due to the nature of withdrawal of electron density from the ring by two heteroatoms, while the related electron deficiency of the ring makes pyridazine more easily attacked by nucleophiles.Synthetic Route of C4H3Cl2N3

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Highly efficient Pd-PEPPSI-IPr catalyst for N-(4-pyridazinyl)-bridged bicyclic sulfonamides via Suzuki-Miyaura coupling reaction was written by Sura, Mallikarhuna Reddy;Bijivemula, N. Reddy;Pogula, Sreekanth Reddy;Motakatla, Venkata Krishna Reddy;Madhvesh, Pathak;Peddiahgari, Vasu Govardhana Reddy. And the article was included in Applied Organometallic Chemistry in 2018.Product Details of 141-30-0 This article mentions the following:

A protocol for the Suzuki-Miyaura coupling of novel 2-(6-chloropyridazin-3-yl)-5-(aryl/heteroarylsulfonyl)-2,5-diazabicyclo[2.2.1]heptanes and heteroarylboronic acids to afford variety of coupled products was realized. Pd-PEPPSI-IPr catalyst was found to be a powerful and reusable catalyst under relatively mild reaction conditions. In the experiment, the researchers used many compounds, for example, 3,6-Dichloropyridazine (cas: 141-30-0Product Details of 141-30-0).

3,6-Dichloropyridazine (cas: 141-30-0) belongs to pyridazine derivatives. The pyridazine structure is a popular pharmacophore which is found within a number of herbicides such as credazine, pyridafol and pyridate. Pyridazine is bioavailable (especially in the CNS) and can reduce toxicity. Pyridazine is a component of several drug molecules, and the pyridazine pharmacophore has contributed to a variety of pharmacologically active compounds.Product Details of 141-30-0

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Synthesis of peptide nucleic acids containing pyridazine derivatives as cytosine and thymine analogs, and their duplexes with complementary oligodeoxynucleotides was written by Tomori, Takahito;Miyatake, Yuya;Sato, Yuta;Kanamori, Takashi;Masaki, Yoshiaki;Ohkubo, Akihiro;Sekine, Mitsuo;Seio, Kohji. And the article was included in Organic Letters in 2015.Application In Synthesis of 3-Aminopyridazine This article mentions the following:

Synthesis of peptide nucleic acids (PNAs) is reported with new pyridazine-type nucleobases: 3-aminopyridazine (aPz) and 1-aminophthalazine (aPh) as cytosine analogs, and pyridazin-3-one (Pz^O) and phthalazin-1-one (Ph^O) as thymine analogs. The PNAs having an aPz or a Pz^O formed duplexes with each complementary oligodeoxynucleotide forming a base pair with G or A, resp., as evaluated by using UV melting analyses and CD (CD) spectra. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Application In Synthesis of 3-Aminopyridazine).

3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. Pyridazine-based compounds continued to be a great source of biologically active compounds as evidenced by the number of publications which emerged in 2021. The unsubstituted pyridazines are more resistant to eletrophilic substitution due to the nature of withdrawal of electron density from the ring by two heteroatoms, while the related electron deficiency of the ring makes pyridazine more easily attacked by nucleophiles.Application In Synthesis of 3-Aminopyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Application of aza-transfer to organic compounds. Reactions between heterocyclic diazo compounds and hydrazines was written by Dezman, L.;Janezic, D.;Kokalj, M.;Kozak, E.;Primc, J.;Stanovnik, B.;Tisler, M.;Zaplotnik-Naglic, O.. And the article was included in Tetrahedron in 1977.Reference of 766-55-2 This article mentions the following:

Aza transfer reactions between heterocyclic hydrazines and diazonium salts or between heterocyclic diazo compounds and substituted hydrazines were studied. The reaction proceeds via intermediate tetrazenes and labeled compounds were used to elucidate the reaction mechanism. In the experiment, the researchers used many compounds, for example, Imidazo[1,2-b]pyridazine (cas: 766-55-2Reference of 766-55-2).

Imidazo[1,2-b]pyridazine (cas: 766-55-2) belongs to pyridazine derivatives. Pyridazine-based compounds continued to be a great source of biologically active compounds as evidenced by the number of publications which emerged in 2021. Pyridazine is bioavailable (especially in the CNS) and can reduce toxicity. Pyridazine is a component of several drug molecules, and the pyridazine pharmacophore has contributed to a variety of pharmacologically active compounds.Reference of 766-55-2

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Phosphodiesterase inhibitors. Part 3: Design, synthesis and structure-activity relationships of dual PDE3/4-inhibitory fused bicyclic heteroaromatic-dihydropyridazinones with anti-inflammatory and bronchodilatory activity was written by Ochiai, Koji;Takita, Satoshi;Eiraku, Tomohiko;Kojima, Akihiko;Iwase, Kazuhiko;Kishi, Tetsuya;Fukuchi, Kazunori;Yasue, Tokutaro;Adams, David R.;Allcock, Robert W.;Jiang, Zhong;Kohno, Yasushi. And the article was included in Bioorganic & Medicinal Chemistry in 2012.Application In Synthesis of 1,2-Dihydro-4-methyl-3,6-pyridazinedione This article mentions the following:

(-)-6-(7-Methoxy-2-trifluoromethylpyrazolo[1,5-a]pyridin-4-yl)-5-methyl-4,5-dihydro-3-(2H)-pyridazinone (KCA-1490) is a dual PDE3/4 inhibitor that exhibits potent combined bronchodilatory and anti-inflammatory activity. A survey of potential bicyclic heteroaromatic replacement subunits for the pyrazolo[1,5-a]pyridine core of KCA-1490 has identified the 4-methoxy-2-(trifluoromethyl)benzo[d]thiazol-7-yl and 8-methoxy-2-(trifluoromethyl)quinolin-5-yl analogs as dual PDE3/4-inhibitory compounds that potently suppress histamine-induced bronchoconstriction and exhibit anti-inflammatory activity in vivo. In the experiment, the researchers used many compounds, for example, 1,2-Dihydro-4-methyl-3,6-pyridazinedione (cas: 5754-18-7Application In Synthesis of 1,2-Dihydro-4-methyl-3,6-pyridazinedione).

1,2-Dihydro-4-methyl-3,6-pyridazinedione (cas: 5754-18-7) belongs to pyridazine derivatives. Pyridazine-based compounds continued to be a great source of biologically active compounds as evidenced by the number of publications which emerged in 2021. Pyridazine compounds have attracted interest in various fields like medicinal, industrial, and agricultural research as they are used for numerous biological activities and other applications.Application In Synthesis of 1,2-Dihydro-4-methyl-3,6-pyridazinedione

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Piperazin-1-ylpyridazine Derivatives Are a Novel Class of Human dCTP Pyrophosphatase 1 Inhibitors was written by Llona-Minguez, Sabin;Hoeglund, Andreas;Ghassemian, Artin;Desroses, Matthieu;Calderon-Montano, Jose Manuel;Burgos Moron, Estefania;Valerie, Nicholas C. K.;Wiita, Elisee;Almloef, Ingrid;Koolmeister, Tobias;Mateus, Andre;Cazares-Koerner, Cindy;Sanjiv, Kumar;Homan, Evert;Loseva, Olga;Baranczewski, Pawel;Darabi, Masoud;Mehdizadeh, Amir;Fayezi, Shabnam;Jemth, Ann-Sofie;Warpman Berglund, Ulrika;Sigmundsson, Kristmundur;Lundbaeck, Thomas;Jenmalm Jensen, Annika;Artursson, Per;Scobie, Martin;Helleday, Thomas. And the article was included in Journal of Medicinal Chemistry in 2017.Recommanded Product: 3,6-Dichloropyridazine This article mentions the following:

The dCTP pyrophosphatase 1 (dCTPase) is a nucleotide pool “housekeeping” enzyme responsible for the catabolism of canonical and noncanonical nucleoside triphosphates (dNTPs) and has been associated with cancer progression and cancer cell stemness. We have identified a series of piperazin-1-ylpyridazines as a new class of potent dCTPase inhibitors. Lead compounds increase dCTPase thermal and protease stability, display outstanding selectivity over related enzymes and synergize with a cytidine analog against leukemic cells. This new class of dCTPase inhibitors lays the first stone toward the development of drug-like probes for the dCTPase enzyme. In the experiment, the researchers used many compounds, for example, 3,6-Dichloropyridazine (cas: 141-30-0Recommanded Product: 3,6-Dichloropyridazine).

3,6-Dichloropyridazine (cas: 141-30-0) belongs to pyridazine derivatives. Pyridazine-based compounds continued to be a great source of biologically active compounds as evidenced by the number of publications which emerged in 2021. The unsubstituted pyridazines are more resistant to eletrophilic substitution due to the nature of withdrawal of electron density from the ring by two heteroatoms, while the related electron deficiency of the ring makes pyridazine more easily attacked by nucleophiles.Recommanded Product: 3,6-Dichloropyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Purine N-oxides. V. Oxides of adenine nucleotides was written by Stevens, Marcus A.;Smith, Herman W.;Brown, Geo. Bosworth. And the article was included in Journal of the American Chemical Society in 1959.Application of 61404-41-9 This article mentions the following:

The parent nucleotides (AMP-2′), (AMP-3′), and (AMP-5′) oxidized with H₂O₂-AcOH mixtures gave the 1-(N-oxides) of adenosine 2′-, 3′-, and 5′-phosphates and adenosine 5′-diphosphate (ADP), resp. The nucleotides oxidized with H₂O₂ alone gave chromatographic amounts of the 1-(N-oxides) of AMP-5′ and deoxyadenylic acid. These nucleotide oxides were characterized by hydrogenation to the parent nucleotide and by acid hydrolysis to 4-amino-5 imidazolecarboxamide oxime. Adenosine 1-(N-oxide) and the AMP-2′, AMP-3′-and AMP-5′ 1-(N-oxides) hydrolyzed with alkali gave the 1-ribosyl and 1-phosphoribosyl derivatives of 5-amino-4-imidazolecarboxamide oxime, resp. The nucleotide oxides in the solid state and in aqueous solution showed an instability which was not observed with adenosine 1-(N-oxide) or adenine 1-(N-oxide). AMP-3′ (500 mg.) in 25 ml. AcOH and 5 ml. 30% H₂O₂ kept 9 days, the solution treated 2 days with 10% Pd-C, evaporated to dryness in vacuo at room temperature, the residue in 6 l. H₂O₂ chromatographed on Dowex-1 formate, and eluted with 0.1M formate yielded AMP-2′, AMP-2′ 1-(N-oxide), AMP-3′, and AMP-3′ 1-(N-oxide). AMP-5′.2H₂O (333 mg.) kept 16 days in 2.6 ml. 30% H₂O₂, 0.7 ml. H₂O, and 3.3 ml. AcOH and the product chromatographed yielded 120 mg. AMP-5′ and 121 mg. AMP-5′ 1-(N-oxide), m. 183-5°. In the experiment, the researchers used many compounds, for example, Ethyl 6-chloro-3-hydroxypyridazine-4-carboxylate (cas: 61404-41-9Application of 61404-41-9).

Ethyl 6-chloro-3-hydroxypyridazine-4-carboxylate (cas: 61404-41-9) belongs to pyridazine derivatives. The pyridazine structure is also found within the structure of several drugs such as cefozopran, cadralazine, minaprine, pipofezine, and hydralazine. The unsubstituted pyridazines are more resistant to eletrophilic substitution due to the nature of withdrawal of electron density from the ring by two heteroatoms, while the related electron deficiency of the ring makes pyridazine more easily attacked by nucleophiles.Application of 61404-41-9

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Synthesis of pyridazine derivatives. XVI. Methyl-substituted imidazo[1,2-b]pyridazines by synthesis and homolytic methylation was written by Pollak, Alfred;Stanovnik, B.;Tisler, Miha. And the article was included in Tetrahedron in 1968.Computed Properties of C6H5N3 This article mentions the following:

Several Me substituted imidazo[1,2-b]pyridazines such as I, were synthesized and N.M.R. data for some of them are included and discussed. Homolytic methylation of imidazo[1,2-b]pyridazine revealed a marked selectivity and afforded a mixture of 7-methyl-, 8-methyl-, and 7,8-dimethylimidazo[1,2-b]pyridazine which could be separated by gas chromatog. 27 references. In the experiment, the researchers used many compounds, for example, Imidazo[1,2-b]pyridazine (cas: 766-55-2Computed Properties of C6H5N3).

Imidazo[1,2-b]pyridazine (cas: 766-55-2) belongs to pyridazine derivatives. The pyridazine structure is also found within the structure of several drugs such as cefozopran, cadralazine, minaprine, pipofezine, and hydralazine. In the past decade, X-ray data were reported with regard to the characterization and structural elucidation of a number of pyridazine-metal complexes, including pyridazine ligands with zinc, nickel, copper, cadmium and ruthenium.Computed Properties of C6H5N3

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Rational Design, Green Synthesis, and Initial Evaluation of a Series of Full-Color Tunable Fluorescent Dyes Enabled by the Copper-Catalyzed N-Arylation of 6-Phenyl Pyridazinones and Their Application in Cell Imaging was written by Liang, Lei;Wang, Wei;Wu, Jun;Xu, Fengrong;Niu, Yan;Xu, Bo;Xu, Ping. And the article was included in Chemistry – A European Journal in 2013.Category: pyridazine This article mentions the following:

There is widespread interest in the application, optimization, and evolution of the transition-metal-catalyzed arylation of N-heteroarenes to discover full-color tunable fluorescent core frameworks. Inspired by the versatile roles of pyridazinone in organic synthesis and medicinal chem., herein, we report a simple and efficient copper-catalyzed cross-coupling reaction for the N-functionalization of pyridazinones in neat water. To achieve the efficient conversion of pyridazinones and organic halides in aqueous phase, a series of copper-salen complexes composed of different Schiff base ligands were investigated by rational design. A final choice of fine-tuned hydrophilicity balanced with lipophilicity among the candidates was confirmed, which affords excellent activity towards the reaction of a wide range of pyridazinones and organic halides. More importantly, the products as N-substituted pyridazinones were synthesized rationally by this methodol. as full-color tunable fluorescent agents (426-612 nm). The N2 position of pyridazinones was modified by different aryl group such as benzothiazole, N,N-dimethylaniline, 3-quinoline, 4-isoquinoline and 2-thiophene, resulting in a series of full-color tunable fluorescent reagents. Meanwhile, the effects of electron-donating and electron-withdrawing groups of the 6-substituted Ph ring have also been investigated to optimize the fluorescent properties. These fluorescent core frameworks were studied in several cell lines as fluorescent dyes. Different colors from blue to red were observed by using fluorescence microscopy and confocal microscopy. In the experiment, the researchers used many compounds, for example, 6-(4-Chlorophenyl)pyridazin-3(2H)-one (cas: 2166-13-4Category: pyridazine).

6-(4-Chlorophenyl)pyridazin-3(2H)-one (cas: 2166-13-4) belongs to pyridazine derivatives. The pyridazine structure is also found within the structure of several drugs such as cefozopran, cadralazine, minaprine, pipofezine, and hydralazine. Pyridazine is bioavailable (especially in the CNS) and can reduce toxicity. Pyridazine is a component of several drug molecules, and the pyridazine pharmacophore has contributed to a variety of pharmacologically active compounds.Category: pyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Synthesis of pyrido[2′,1′:2,3]imidazo[4,5-b]quinoline and pyrido[1′,2′:1,2]imidazo[4,5-b]quinoline and their benzo and aza analogs via tandem catalysis was written by Loones, Kristof T. J.;Maes, Bert U. W.;Dommisse, Roger A.. And the article was included in Tetrahedron in 2007.Recommanded Product: 5469-70-5 This article mentions the following:

Regioselective tandem metal-catalyzed aminations on 2-chloro-3-iodoquinoline and 2,3-dibromoquinoline with amino(benzo)(di)azines are reported. Eight new heterocyclic scaffolds of the dipyridoimidazole type could be synthesized. By controlling the reaction temperature selective C-2 intermol. Pd-catalyzed amination on 2,3-dibromoquinoline with amino(benzo)(di)azines can be achieved. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Recommanded Product: 5469-70-5).

3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. The pyridazine structure is also found within the structure of several drugs such as cefozopran, cadralazine, minaprine, pipofezine, and hydralazine. Pyridazine is bioavailable (especially in the CNS) and can reduce toxicity. Pyridazine is a component of several drug molecules, and the pyridazine pharmacophore has contributed to a variety of pharmacologically active compounds.Recommanded Product: 5469-70-5

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem