Category: 149554-29-0

HPLC of Formula: 149554-29-0. 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: 6-(Piperazin-1-yl)nicotinonitrile, is researched, Molecular C10H12N4, CAS is 149554-29-0, about A therapeutic approach to pantothenate kinase associated neurodegeneration. Author is Sharma, Lalit Kumar; Subramanian, Chitra; Yun, Mi-Kyung; Frank, Matthew W.; White, Stephen W.; Rock, Charles O.; Lee, Richard E.; Jackowski, Suzanne.

Pantothenate kinase (PANK) is a metabolic enzyme that regulates cellular CoA (CoA) levels. There are three human PANK genes, and inactivating mutations in PANK2 lead to pantothenate kinase associated neurodegeneration (PKAN). Here we performed a library screen followed by chem. optimization to produce PZ-2891, an allosteric PANK activator that crosses the blood brain barrier. PZ-2891 occupies the pantothenate pocket and engages the dimer interface to form a PANK.ATP.Mg2+.PZ-2891 complex. The binding of PZ-2891 to one protomer locks the opposite protomer in a catalytically active conformation that is refractory to acetyl-CoA inhibition. Oral administration of PZ-2891 increases CoA levels in mouse liver and brain. A knockout mouse model of brain CoA deficiency exhibited weight loss, severe locomotor impairment and early death. Knockout mice on PZ-2891 therapy gain weight, and have improved locomotor activity and life span establishing pantazines as novel therapeutics for the treatment of PKAN.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 6-(Piperazin-1-yl)nicotinonitrile( cas:149554-29-0 ) is researched.Formula: C10H12N4.Ryu, Je Ho; Kim, Shinae; Lee, Jung A.; Han, Hye Young; Son, Hyun Joo; Lee, Hyun Jung; Kim, Yong Hyuk; Kim, Jae-Sun; Park, Hyeung-geun published the article 《Synthesis and optimization of picolinamide derivatives as a novel class of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors》 about this compound( cas:149554-29-0 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: picolinamide derivative synthesis optimization hydroxysteroid dehydrogenase inhibitor; 11β-HSD1 inhibitor; Diabetes; Hyperlipidemia; Metabolic syndrome; Picolinamide. Let’s learn more about this compound (cas:149554-29-0).

The synthesis and structure-activity relationship of a series of 6-substituted picolinamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1 are described. The optimization of the left-hand side of lead compound I resulted in the discovery of the highly potent, selective, and orally available inhibitor II, which demonstrated an excellent activity in a mouse ex vivo pharmacodynamic model. Moreover, II reduced the blood glucose and improved the lipid profiles in ob/ob mice after oral administration.

《Synthesis and optimization of picolinamide derivatives as a novel class of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(6-(Piperazin-1-yl)nicotinonitrile)Formula: C10H12N4.

Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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 Chemical Probe Identification Platform for Orphan GPCRs Using Focused Compound Screening: GPR39 as a Case Example, published in 2013-11-14, which mentions a compound: 149554-29-0, Name is 6-(Piperazin-1-yl)nicotinonitrile, Molecular C10H12N4, SDS of cas: 149554-29-0.

Orphan G protein-coupled receptors (oGPCRs) are a class of integral membrane proteins for which endogenous ligands or transmitters have not yet been discovered. Transgenic animal technologies have uncovered potential roles for many of these oGPCRs, providing new targets for the treatment of various diseases. Understanding signaling pathways of oGPCRs and validating these receptors as potential drug targets requires the identification of chem. probe compounds to be used in place of endogenous ligands to interrogate these receptors. A novel chem. probe identification platform was created in which GPCR-focused libraries were screened against sets of oGPCR targets, with a goal of discovering fit-for-purpose chem. probes for the more druggable members of the set. Application of the platform to a set of oGPCRs resulted in the discovery of the first reported small mol. agonists for GPR39, a receptor implicated in the regulation of insulin secretion and preservation of beta cells in the pancreas. Compound 1 stimulated intracellular calcium mobilization in recombinant and native cells in a GPR39-specific manner but did not potentiate glucose-stimulated insulin secretion in human islet preparations

The article 《Chemical Probe Identification Platform for Orphan GPCRs Using Focused Compound Screening: GPR39 as a Case Example》 also mentions many details about this compound(149554-29-0)SDS of cas: 149554-29-0, you can pay attention to it, because details determine success or failure

Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

HPLC of Formula: 149554-29-0. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 6-(Piperazin-1-yl)nicotinonitrile, is researched, Molecular C10H12N4, CAS is 149554-29-0, about Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst3 receptor antagonists. Author is Troxler, Thomas; Hurth, Konstanze; Schuh, Karl-Heinrich; Schoeffter, Philippe; Langenegger, Daniel; Enz, Albert; Hoyer, Daniel.

Starting from non-peptidic sst1-selective somatostatin receptor antagonists, first compounds with mixed sst1/sst3 affinity were identified by directed structural modifications. Systematic optimization of these initial leads afforded novel, enantiomerically pure, highly potent and sst3-subtype selective somatostatin antagonists, e.g. I (R = piperonyl, 6-methoxypyridin-3-yl, 6-quinoxalinyl, etc.), based on a (4S,4aS,8aR)-decahydroisoquinoline-4-carboxylic acid core moiety. These compounds can efficiently be synthesized and show promising PK properties in rodents.

After consulting a lot of data, we found that this compound(149554-29-0)HPLC of Formula: 149554-29-0 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 6-(Piperazin-1-yl)nicotinonitrile, is researched, Molecular C10H12N4, CAS is 149554-29-0, about The discovery of potent antagonists of NPBWR1 (GPR7).Application In Synthesis of 6-(Piperazin-1-yl)nicotinonitrile.

The synthesis and evaluation of small mol. antagonists of the G protein-coupled receptor NPBWR1 (GPR7) are reported for the first time. [4-(5-Chloropyridin-2-yl)piperazin-1-yl][(1S,2S,4R)-4-{[(1R)-1-(4-methoxyphenyl)ethyl]amino}-2-(thiophen-3-yl)cyclohexyl]methanone (I) emerged as a hit from a high-throughput screen. Examination of substituents that focused on replacing the 5-chloropyridine and 4-methoxybenzylamino groups of I led to the identification of compounds that exhibited subnanomolar potencies as low as 660 pM {II [X = NH]} in the functional assay and 200 pM in the binding assay {II [X = O]}.

In some applications, this compound(149554-29-0)Application In Synthesis of 6-(Piperazin-1-yl)nicotinonitrile is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 6-(Piperazin-1-yl)nicotinonitrile(SMILESS: N#CC1=CN=C(N2CCNCC2)C=C1,cas:149554-29-0) is researched.Application In Synthesis of (S)-5-(Hydroxymethyl)dihydrofuran-2(3H)-one. The article 《[(S)-γ-(4-Aryl-1-piperazinyl)-L-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors》 in relation to this compound, is published in Bioorganic & Medicinal Chemistry Letters. Let’s take a look at the latest research on this compound (cas:149554-29-0).

In the search for an inhibitor of dipeptidyl peptidase IV (DPP-IV) highly potent both in vitro and in vivo, a series of L-prolylthiazolidine-based DPP-IV inhibitors, e.g., I, having 4-arylpiperazine or 4-arylpiperidine at the γ-position of the proline structure was synthesized. Of these compounds, the 4-(5-nitro-2-pyridyl)piperazine analog I showed a sub-nanomolar (IC50 = 0.92 nmol/L) DPP-IV inhibitory activity and a long-lasting in vivo DPP-IV inhibition profile.

In some applications, this compound(149554-29-0)Synthetic Route of C10H12N4 is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 6-(Piperazin-1-yl)nicotinonitrile(SMILESS: N#CC1=CN=C(N2CCNCC2)C=C1,cas:149554-29-0) is researched.Recommanded Product: (S)-3-(Piperidin-2-yl)pyridine. The article 《Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1)》 in relation to this compound, is published in Bioorganic & Medicinal Chemistry Letters. Let’s take a look at the latest research on this compound (cas:149554-29-0).

The discovery of a novel series of pyrrolo[1,2-a]pyrazin-1(2H)-one PARP inhibitors is described. Optimization led to compounds that display excellent PARP-1 enzyme potency and inhibit the proliferation of BRCA deficient cells in the low double-digit nanomolar range showing excellent selectivity over BRCA proficient cancer cells.

As far as I know, this compound(149554-29-0)Formula: C10H12N4 can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.

Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

Lory, Pedro M. J.; Estrella-Jimenez, Maria E.; Shashack, Matthew J.; Lokesh, Ganesh L.; Natarajan, Amarnath; Gilbertson, Scott R. published the article 《Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides》. Keywords: thioxanthenone dioxide carbamoyl amino preparation BRCT hepatitis C inhibitor.They researched the compound: 6-(Piperazin-1-yl)nicotinonitrile( cas:149554-29-0 ).Quality Control of 6-(Piperazin-1-yl)nicotinonitrile. 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:149554-29-0) here.

Methods appropriate for the parallel synthesis of libraries based on the thioxanthen-9-one 10,10-dioxide scaffold are reported. The novel compounds were synthesized from previously reported 3-chlorothioxanthen-9-one-10,10-dioxide and com. available 3-carboxythioxanthen-9-one 10,10-dioxide. The library members were screened for activity in a fluorescence polarization assay for inhibitors of BRCT domains of breast cancer gene 1 and in cell-based secreted alk. phosphatase reported replicon system for activity against hepatitis C virus.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 6-(Piperazin-1-yl)nicotinonitrile( cas:149554-29-0 ) is researched.Name: 6-(Piperazin-1-yl)nicotinonitrile.Hurth, Konstanze; Enz, Albert; Floersheim, Philipp; Gentsch, Conrad; Hoyer, Daniel; Langenegger, Daniel; Neumann, Peter; Pfaeffli, Paul; Sorg, Dieter; Swoboda, Robert; Vassout, Annick; Troxler, Thomas published the article 《SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists》 about this compound( cas:149554-29-0 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: SAR structure arylpiperazine moiety obeline somatostatin sst receptor antagonist. Let’s learn more about this compound (cas:149554-29-0).

The SAR of over 50 derivatives of octahydrobenzo[g]quinoline (obeline)-type somatostatin sst1 receptor antagonist 1 is presented, focusing on the modification of its arylpiperazine moiety. Sst1 affinities in this series cover a range of five orders of magnitude with the best derivatives displaying subnanomolar sst1 affinities and >10,000-fold selectivities over the sst2 receptor subtype as well as promising pharmacokinetic properties.

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Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 6-(Piperazin-1-yl)nicotinonitrile, is researched, Molecular C10H12N4, CAS is 149554-29-0, about Design, Synthesis, Biological Screening, and Molecular Docking Studies of Piperazine-Derived Constrained Inhibitors of DPP-IV for the Treatment of Type 2 Diabetes, the main research direction is piperazine derivative preparation antidiabetic screening mol docking DPPIV inhibitor; antihyperglycemic; constrained DPP-IV inhibitor; dipeptidyl peptidyl-IV (DPP-IV) inhibitor; molecular docking; oral glucose tolerance test; piperazine.HPLC of Formula: 149554-29-0.

Novel piperazine-derived conformationally constrained compounds were designed, synthesized, and evaluated for in vitro Dipeptidyl peptidase-IV (DPP-IV) inhibitory activities. From a library of compounds synthesized, 1-(2-(4-(7-Chloro-4-quinolyl)piperazin-1-yl)acetyl)pyrrolidine (2g) was identified as a potential DPP-IV inhibitor exhibiting better inhibitory activity than P32/98, reference inhibitor. The in vivo studies carried out in STZ and db/db mice models indicated that the compound 2g showed moderate antihyperglycemic activity as compared to the marketed drug Sitagliptin. A two-week repeated dose study in db/db mice revealed that compound 2g significantly declined blood glucose levels with no evidence of hypoglycemia risk. Furthermore, it showed improvement in insulin resistance reversal and antidyslipidemic properties. Mol. docking studies established good binding affinity of compound 2g at the DPP-IV active site and are in favor of the observed biol. data. These data collectively suggest that compound 2g is a good lead mol. for further optimization studies.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI