Liu, Yugang et al. published their research in Organic Process Research & Development in 2008 | CAS: 5469-70-5

3-Aminopyridazine (cas: 5469-70-5) 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 and derivatives coordinate readily with transition metals to form complexes and catalysts with synthetic utility.Electric Literature of C4H5N3

Practical synthesis of a peptide deformylase (PDF) inhibitor was written by Liu, Yugang;Prashad, Mahavir;Ciszewski, Lech;Vargas, Kevin;Repic, Oljan;Blacklock, Thomas J.. And the article was included in Organic Process Research & Development in 2008.Electric Literature of C4H5N3 This article mentions the following:

A practical chromatog.-free synthesis of an N-formylated hydroxylamine peptide deformylase inhibitor LCD320 (I) is described. A diastereoselective Michael reaction of (4S)-3-[2-(cyclobutylmethyl)-1-oxo-2-propenyl]-4-(phenylmethyl)-2-oxazolidinone with O-benzyl hydroxylamine was used to establish the key stereogenic center. We found that traces of residual Li+ from a previous step had a great impact on the diastereoselectivity of this reaction. A very efficient amidation coupling reaction of proline derivative (2S,4R)-4-fluoro-1,2-pyrrolidinedicarboxylic acid 1,1-dimethylethyl ester with weakly nucleophilic 3-pyridazinamine using methanesulfonyl chloride in the presence of 1-methylimidazole in DMF was also developed that proceeded without racemization. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Electric Literature of C4H5N3).

3-Aminopyridazine (cas: 5469-70-5) 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 and derivatives coordinate readily with transition metals to form complexes and catalysts with synthetic utility.Electric Literature of C4H5N3

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Loones, Kristof T. J. et al. published their research in Journal of Organic Chemistry in 2006 | CAS: 5469-70-5

3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. Pyridazine and phthalazine have quite different spectroscopic properties compared with their isomers, pyrazine and quinoxaline. 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.Computed Properties of C4H5N3

Orthogonal and Auto-Tandem Catalysis: Synthesis of Dipyrido[1,2-a:2′,3′-d]imidazole and Its Benzo and Aza Analogues via Inter- and Intramolecular C-N Bond Formation was written by Loones, Kristof T. J.;Maes, Bert U. W.;Meyers, Caroline;Deruytter, Joke. And the article was included in Journal of Organic Chemistry in 2006.Computed Properties of C4H5N3 This article mentions the following:

The synthesis of dipyrido[1,2-a:2′,3′-d]imidazole and hitherto unknown benzo and aza analogs from 2,3-dibromopyridine and aminoazines is described. Mechanistically, the developed procedure involves orthogonal (Pd and Cu catalyst) or auto-tandem (Pd catalyst) catalysis via regioselective inter- and intramol. C-N bond formation. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Computed Properties of C4H5N3).

3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. Pyridazine and phthalazine have quite different spectroscopic properties compared with their isomers, pyrazine and quinoxaline. 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.Computed Properties of C4H5N3

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Wu, Qiqi et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2022 | CAS: 5469-70-5

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 activity depends upon the changes of substituted groups in the pyridazine ring system resulting in different biological activities. In addition, the natural pyrimidine bases uracil, thymine, and cytosine, which are constituents of the nucleic acids, are found to be the most important naturally occurring diazines.Safety of 3-Aminopyridazine

The discovery of a non-competitive GOT1 inhibitor, hydralazine hydrochloride, via a coupling reaction-based high-throughput screening assay was written by Wu, Qiqi;Sun, Zhongya;Chen, Zhifeng;Liu, Jingqiu;Ding, Hong;Luo, Cheng;Wang, Mingliang;Du, Daohai. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2022.Safety of 3-Aminopyridazine This article mentions the following:

Glutamate oxaloacetate transaminase 1 (GOT1) plays a key role in aberrant glutamine metabolism GOT1 suppression can arrest tumor growth and prevent the development of cancer, indicating GOT1 as a potential anticancer target. Reported GOT1 inhibitors, on the other hand, are quite restricted. Here, we developed and optimized a coupling reaction-based high-throughput screening assay for the discovery of GOT1 inhibitors. By using this screening assay, we found that the cardiovascular drug hydralazine hydrochloride inhibited GOT1 catalytic activity, with an IC50 of 26.62 ± 7.45 μM, in a non-competitive and partial-reversible manner. In addition, we determined the binding affinity of hydralazine hydrochloride to GOT1, with a Kd of 16.54 ± 8.59 μM, using a microscale thermophoresis assay. According to structure-activity relationship anal., the inhibitory activity of hydralazine hydrochloride is mainly derived from its hydrazine group. Furthermore, it inhibits the proliferation of cancer cells MCF-7 and MDA-MB-468 with a slight inhibitory effect compared to other tested cancer cells, highlighting GOT1 as a promising therapeutic target for the treatment of breast cancer. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Safety 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 activity depends upon the changes of substituted groups in the pyridazine ring system resulting in different biological activities. In addition, the natural pyrimidine bases uracil, thymine, and cytosine, which are constituents of the nucleic acids, are found to be the most important naturally occurring diazines.Safety of 3-Aminopyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

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Healthcare careers for chemists are once again largely based in laboratories, although increasingly there is opportunity to work at the point of care, helping with patient investigation. Product Details of 5469-70-5

The invention relates to a process for straightening keratin fibres, comprising: (i) a step in which a straightening composition containing at least two denaturing agents is applied to the keratin fibres, (ii) a step in which the temperature of the keratin fibres is raised, using a heating means, to a temperature of between 110 and 250 C.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N38 – PubChem

 

September 23, 2021 News New explortion of 5469-70-5

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The invention relates to guanidine compounds of general formula (I), corresponding enantiomeric, diastereomeric, and/or tautomeric forms thereof, and pharmaceutically acceptable salts thereof. The invention further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors in order to treat diseases modulated by 5-HT5 receptor activity, especially treat neurodegenerative and neuropsychiatric disorders and the signs, symptoms, and malfunctions associated therewith.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N36 – PubChem

 

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In the modern protocols of chemical protein syntheses, peptide-alpha-thioesters have been used as key components for the assembly of full-length polypeptides through chemoselective peptide coupling reactions. A variety of thioester precursors have been developed for the synthesis of the peptide-alpha-thioesters by Fmoc solid phase peptide synthesis (Fmoc-SPPS). Recently our group found a peptidyl-N-acetylguanidine as a new peptide-alpha-thioester precursor. This peptide derivative can be converted into a corresponding peptide-alpha-thioester only by treatment with an excess amount of a thiol in aqueous buffers at around neutral pH. This unique property allowed us to envision the practical use of the peptidyl-N-acetylguanidines for the chemical syntheses of proteins; however, an efficient synthetic method has been lacking. Herein, we report an efficient solid-phase synthesis of peptidyl-N-acetylguanidines. This new synthetic method employing selective activation and cleavage of a peptide bond successfully provided peptidyl-N-acetylguanidines from the on-resin protected peptides prepared by standard Fmoc-SPPS. We also evaluated the reactivity of a peptidyl-N-acetylguanidine in native chemical ligation through the synthesis of glucose-dependent insulinotropic polypeptide analogue.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N88 – PubChem

 

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A small molecular library of 40 pyrimidine, pyrazole, and isoxazole derivatives, bearing structural features for a promising binding of therapeutically interesting enzymes, was designed and prepared. An efficient and straightforward solid phase synthesis was envisaged and carried out on a Rink amide resin. The assistance of microwave heating in any step reduced the reaction time, increased the reaction yields, and allowed an easy work-up and purification of the targeted compounds.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N90 – PubChem

 

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A practical synthetic route to an important pharmaceutical intermediate 1-methyl-4-phenyl-1H-imidazol-2-amine, via a three-step sequence involving cyclisation, hydrolysis and methylation, is reported. In the process of optimisation, a novel chemical entity was isolated and confirmed to be 2,6-diphenyl-1H-imidazo[1,2-a]imidazole by MS, 1H NMR and 13C NMR. The scale-up experiment was carried out to provide 1-methyl-4-phenyl-1H-imidazol-2-amine in 27.4% total yield.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N102 – PubChem

 

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Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. A catalyst does not appear in the overall stoichiometry of the reaction it catalyzes. “Recommanded Product: 5469-70-5

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The present invention provides compounds of formula (I) and compositions thereof, methods of making them, and methods of using them to modulate alpha7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N21 – PubChem

 

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In this work, we demonstrate the existence of linear relationships between gas-phase equilibrium bond lengths of the guanidine skeleton of 2-(arylamino)imidazolines and their aqueous pKa value. For a training set of 22 compounds, in the most stable conformation of their lowest energy tautomeric form, three bonds were found to exhibit r2 and q2 values >0.95 and root-mean-squared-error of estimation values ?0.25 when regressed individually against pKa. The equations describing these one-bond-length linear relationships, in addition to a multiple linear regression model using all three bond lengths, were then used to predict the experimental pKa values of an external test set of further 27 derivatives. The optimal protocol we derive here shows an overall mean absolute error (MAE) of 0.20 and standard deviation of errors of 0.18 for the test set. Predictions for a second test set of diphenyl-based bis(2-iminoimidazolidines) yielded an MAE of 0.27 and a standard deviation of 0.10. The predictive power of the optimal model is further demonstrated by its ability to correct erroneously reported experimental values. Finally, a previously established guanidine model is recalibrated at a new level of theory, and predictions are made for novel phenylguanidine derivatives, showing an MAE of just 0.29. The protocols established and tested here pass both of Roy’s modern and stringent MAE-based criteria for a “good” quantitative structure-activity relationship/quantitative structure-property relationship model predictivity. Notably, the ab initio bond length high correlation subset protocol developed in this work demonstrates lower MAE values than the Marvin program by ChemAxon for all test sets.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N68 – PubChem