Category: 136725-55-8

Application of 136725-55-8. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about Fluorine Substitution Induced High Tc of Enantiomeric Perovskite Ferroelectrics: (R)- and (S)-3-(Fluoropyrrolidinium)MnCl3. Author is Ai, Yong; Chen, Xiao-Gang; Shi, Ping-Ping; Tang, Yuan-Yuan; Li, Peng-Fei; Liao, Wei-Qiang; Xiong, Ren-Gen.

The past decade has witnessed much progress in designing mol. ferroelecs., whose intrinsic mech. flexibility, structural tunability, and easy processability are desirable for next-generation flexible and wearable electronic devices. However, an obstacle in expanding their promising applications in nonvolatile memory elements, capacitors, and sensors is effectively modulating the Curie temperature (Tc). Here, taking advantage of fluorine substitution on the reported mol. ferroelec., (pyrrolidinium)MnCl3, we present enantiomeric perovskite ferroelecs., namely, (R)- and (S)-3-(fluoropyrrolidinium)MnCl3. The close van der Waal’s radii and the similar steric parameters between H and F atoms ensure the min. disruption of the crystal structure, while their different electronegativity and polarizability can trigger significant changes in the phys. and chem. properties. As expected, the Tc gets successfully increased from 295 K in (pyrrolidinium)MnCl3 to 333 K in these two homochiral compounds Such a dramatic enhancement of 38 K signifies an important step toward designing high-Tc mol. ferroelecs. In the light of the conceptually new idea of fluorine substitution, one could look forward to a continuous succession of new mol. ferroelec. materials and technol. developments.

The article 《Fluorine Substitution Induced High Tc of Enantiomeric Perovskite Ferroelectrics: (R)- and (S)-3-(Fluoropyrrolidinium)MnCl3》 also mentions many details about this compound(136725-55-8)Application of 136725-55-8, you can pay attention to it, because details determine success or failure

Reference:
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Name: (R)-(-)-3-Fluoropyrrolidine Hydrochloride. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about Facile and efficient syntheses of novel (S)- and (R)-3-fluoropyrrolidines and 3,3-difluoropyrrolidine. Author is Giardina, Giuseppe; Dondio, Giulio; Grugni, Mario.

Novel enantiomeric 3-fluoropyrrolidines and 3,3-difluoropyrrolidine were obtained in high yield starting from the enantiomerically pure and com. available (2S,4R)-4-hydroxyproline. Spray-dried potassium fluoride and diethylaminosulfur trifluoride were used to introduce one or two fluorine atoms, resp.

After consulting a lot of data, we found that this compound(136725-55-8)Name: (R)-(-)-3-Fluoropyrrolidine Hydrochloride can be used in many types of reactions. And in most cases, this compound has more advantages.

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Henderson, Scott H.; Sorrell, Fiona; Bennett, James; Fedorov, Oleg; Hanley, Marcus T.; Godoi, Paulo H.; Ruela de Sousa, Roberta; Robinson, Sean; Ashall-Kelly, Alexander; Hopkins Navratilova, Iva; Walter, Daryl S.; Elkins, Jonathan M.; Ward, Simon E. published an article about the compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride( cas:136725-55-8,SMILESS:Cl.F[C@@H]1CCNC1 ).Formula: C4H9ClFN. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:136725-55-8) through the article.

Dual-specificity tyrosine-regulated kinase 1A (DYRK1A) regulates the proliferation and differentiation of neuronal progenitor cells during brain development. Consequently, DYRK1A has attracted interest as a target for the treatment of neurodegenerative diseases, including Alzheimer′s disease (AD) and Down′s syndrome. Recently, the inhibition of DYRK1A has been investigated as a potential treatment for diabetes, while DYRK1A′s role as a mediator in the cell cycle has garnered interest in oncol. indications. Structure-activity relationship (SAR) anal. in combination with high-resolution X-ray crystallog. leads to a series of pyrazolo[1,5-b]pyridazine inhibitors with excellent ligand efficiencies, good physicochem. properties, and a high degree of selectivity over the kinome. Compound 11 (I) exhibited good permeability and cellular activity without P-glycoprotein liability, extending the utility of 11 in an in vivo setting. These pyrazolo[1,5-b]pyridazines are a viable lead series in the discovery of new therapies for the treatment of diseases linked to DYRK1A function.

After consulting a lot of data, we found that this compound(136725-55-8)Formula: C4H9ClFN can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyridazine – Wikipedia,
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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Journal of Medicinal Chemistry called PI-2620 Lead Optimization Highlights the Importance of Off-Target Assays to Develop a PET Tracer for the Detection of Pathological Aggregated Tau in Alzheimer′s Disease and Other Tauopathies, Author is Kroth, Heiko; Oden, Felix; Molette, Jerome; Schieferstein, Hanno; Gabellieri, Emanuele; Mueller, Andre; Berndt, Mathias; Sreenivasachary, Nampally; Serra, Andreia Monica; Capotosti, Francesca; Schmitt-Willich, Heribert; Hickman, David; Pfeifer, Andrea; Dinkelborg, Ludger; Stephens, Andrew, which mentions a compound: 136725-55-8, SMILESS is Cl.F[C@@H]1CCNC1, Molecular C4H9ClFN, Quality Control of (R)-(-)-3-Fluoropyrrolidine Hydrochloride.

The first candidate PI-2014 was tested in healthy controls and subjects with Alzheimer′s disease (AD). As PI-2014 displayed off-target binding to monoamine oxidase A (MAO-A), a new lead with improved binding to Tau and decreased MAO-A binding was required. For compound optimization, Tau binding assays based on both human AD brain homogenate and Tau-paired helical filaments were employed. Furthermore, two MAO-A screening assays based on (1) human-recombinant MAO-A and (2) displacement of 2-fluoro-ethyl-harmine from mouse brain homogenate were employed. Removing the N-Me group from the tricyclic core resulted in compounds displaying improved Tau binding. For the final round of optimization, the cyclic amine substituents were replaced by pyridine derivatives PI-2620 (2-(2-fluoropyridin-4-yl)-9H-pyrrolo[2,3-b:4,5-c′]dipyridine) emerged as a best candidate displaying high Tau binding, low MAO-A binding, high brain uptake, and fast and complete brain washout. Furthermore, PI-2620 showed Tau binding on brain sections from corticobasal degeneration, progressive supranuclear palsy, and Pick′s disease.

Although many compounds look similar to this compound(136725-55-8)Quality Control of (R)-(-)-3-Fluoropyrrolidine Hydrochloride, numerous studies have shown that this compound(SMILES:Cl.F[C@@H]1CCNC1), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

HPLC of Formula: 136725-55-8. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about Fluorine in medicinal chemistry: β-fluorination of peripheral pyrrolidines attached to acridine ligands affects their interactions with G-quadruplex DNA. Author is Campbell, Nancy H.; Smith, Daniel L.; Reszka, Anthony P.; Neidle, Stephen; O’Hagan, David.

Comparative X-ray structure studies reveal that C-F bond incorporation into the peripheral pyrrolidine moieties of the G-quadruplex DNA binding ligand BSU6039 leads to a distinct pyrrolidine ring conformation, relative to the non-fluorinated analog, and with a different binding mode involving reversal of the pyrrolidinium N+-H orientation.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Related Products of 136725-55-8. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about Novel Human Neutral Sphingomyelinase 2 Inhibitors as Potential Therapeutics for Alzheimer’s Disease. Author is Sala, Michal; Hollinger, Kristen R.; Thomas, Ajit G.; Dash, Ranjeet P.; Tallon, Carolyn; Veeravalli, Vijayabhaskar; Lovell, Lyndah; Kogler, Martin; Hrebabecky, Hubert; Prochazkova, Eliska; Nesuta, Ondrej; Donoghue, Amanda; Lam, Jenny; Rais, Rana; Rojas, Camilo; Slusher, Barbara S.; Nencka, Radim.

Neutral sphingomyelinase 2 (nSMase2) catalyzes the cleavage of sphingomyelin to phosphorylcholine and ceramide, an essential step in the formation and release of exosomes from cells that is critical for intracellular communication. Chronic increase of brain nSMase2 activity and related exosome release has been implicated in various pathol. processes, including the progression of Alzheimer’s disease (AD), making nSMase2 a viable therapeutic target. Recently, we identified phenyl(R)-(1-(3-(3,4-dimethoxyphenyl)-2,6-dimethylimidazo[1,2-b] pyridazin-8-yl) pyrrolidin-3-yl)-carbamate 1 (PDDC)(I), the first nSMase2 inhibitor which possesses both favorable pharmacodynamics and pharmacokinetic (PK) parameters, including substantial oral bioavailability, brain penetration and significant inhibition of exosome release from the brain in vivo. Herein we demonstrate efficacy of 1 (PDDC) in a mouse model of AD and detail extensive structure-activity relationship (SAR) studies with 70 analogs, unveiling several that exert similar or higher activity against nSMase2 with favorable pharmacokinetic properties.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Discovery of Potent N-Ethylurea Pyrazole Derivatives as Dual Inhibitors of Trypanosoma brucei and Trypanosoma cruzi, published in 2020-03-12, which mentions a compound: 136725-55-8, Name is (R)-(-)-3-Fluoropyrrolidine Hydrochloride, Molecular C4H9ClFN, Recommanded Product: (R)-(-)-3-Fluoropyrrolidine Hydrochloride.

Trypanosoma brucei (T. brucei) and Trypanosoma cruzi (T. cruzi) are causative agents of parasitic diseases known as human African trypanosomiasis and Chagas disease, resp. Together, these diseases affect 68 million people around the world. Current treatments are unsatisfactory, frequently associated with intolerable side-effects, and generally inadequate in treating all stages of disease. In this paper, we report the discovery of N-ethylurea pyrazoles that potently and selectively inhibit the viability of T. brucei and T. cruzi. Sharp and logical SAR led to the identification of 54 as the best compound, with an in vitro IC50 of 9 nM and 16 nM against T. b. brucei and T. cruzi, resp. Compound 54 demonstrates favorable physicochem. properties and was efficacious in a murine model of Chagas disease, leading to undetectable parasitemia within 6 days when CYP metabolism was inhibited.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Highest-Tc organic enantiomeric ferroelectrics obtained by F/H substitution, published in 2020, which mentions a compound: 136725-55-8, Name is (R)-(-)-3-Fluoropyrrolidine Hydrochloride, Molecular C4H9ClFN, Safety of (R)-(-)-3-Fluoropyrrolidine Hydrochloride.

Through the strategy of F/H substitution, we precisely designed the highest-Tc (phase transition temperature) organic enantiomeric ferroelecs., (R)- and (S)-(N,N-dimethyl-3-fluoropyrrolidinium) iodide, of which the Tc reaches up to 470 K, far beyond those of other enantiomeric ferroelecs. and also the com. ferroelec. BaTiO3.

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Pyridazine – Wikipedia,
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Kroth, Heiko; Oden, Felix; Molette, Jerome; Schieferstein, Hanno; Gabellieri, Emanuele; Mueller, Andre; Berndt, Mathias; Sreenivasachary, Nampally; Serra, Andreia Monica; Capotosti, Francesca; Schmitt-Willich, Heribert; Hickman, David; Pfeifer, Andrea; Dinkelborg, Ludger; Stephens, Andrew published the article 《PI-2620 Lead Optimization Highlights the Importance of Off-Target Assays to Develop a PET Tracer for the Detection of Pathological Aggregated Tau in Alzheimer′s Disease and Other Tauopathies》. Keywords: PET imaging tracer preparation Tau aggregation Alzheimer’s palsy Pick’s.They researched the compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride( cas:136725-55-8 ).Related Products of 136725-55-8. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:136725-55-8) here.

The first candidate PI-2014 was tested in healthy controls and subjects with Alzheimer′s disease (AD). As PI-2014 displayed off-target binding to monoamine oxidase A (MAO-A), a new lead with improved binding to Tau and decreased MAO-A binding was required. For compound optimization, Tau binding assays based on both human AD brain homogenate and Tau-paired helical filaments were employed. Furthermore, two MAO-A screening assays based on (1) human-recombinant MAO-A and (2) displacement of 2-fluoro-ethyl-harmine from mouse brain homogenate were employed. Removing the N-Me group from the tricyclic core resulted in compounds displaying improved Tau binding. For the final round of optimization, the cyclic amine substituents were replaced by pyridine derivatives PI-2620 (2-(2-fluoropyridin-4-yl)-9H-pyrrolo[2,3-b:4,5-c′]dipyridine) emerged as a best candidate displaying high Tau binding, low MAO-A binding, high brain uptake, and fast and complete brain washout. Furthermore, PI-2620 showed Tau binding on brain sections from corticobasal degeneration, progressive supranuclear palsy, and Pick′s disease.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Product Details of 136725-55-8. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about Discovery of a pyrazolo[1,5-a]pyrimidine derivative (MT-3014) as a highly selective PDE10A inhibitor via core structure transformation from the stilbene moiety. Author is Koizumi, Yuuki; Tanaka, Yoshihito; Matsumura, Takehiko; Kadoh, Yoichi; Miyoshi, Haruko; Hongu, Mitsuya; Takedomi, Kei; Kotera, Jun; Sasaki, Takashi; Taniguchi, Hiroyuki; Watanabe, Yumi; Takakuwa, Misae; Kojima, Koki; Baba, Nobuyuki; Nakamura, Itsuko; Kawanishi, Eiji.

We have developed a new class of PDE10A inhibitor, a pyrazolo[1,5-a]pyrimidine derivative MT-3014 (1, I). A previous compound introduced was deprioritized due to concerns for E/Z-isomerization and glutathione-adduct formation at the core stilbene structure. We discovered pyrazolo [1,5-a] pyrimidine as a new lead scaffold by structure-based drug design utilizing a co-crystal structure with PDE10A. The lead compound was optimized for in vitro activity, solubility, and selectivity against human ether-a-́go-go related gene cardiac channel binding. We observed that I shows excellent efficacy in rat conditioned avoidance response test and suitable pharmacokinetic properties in rats, especially high brain penetration.

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