Tag: M.W:200-300

Category: benzothiophene. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 5-Amino-1-(2-bromophenyl)-1H-pyrazole-4-carbonitrile, is researched, Molecular C10H7BrN4, CAS is 71856-54-7, about Synthesis and adenosine receptor affinity of a series of pyrazolo[3,4-d]pyrimidine analogs of 1-methylisoguanosine.

Two series of pyrazolo[3,4-d]pyrimidine analogs I (R = Ph, substituted Ph; R1 = Me; R = Ph, R1 = Et, Pr, Bu, Ph; R = 3-ClC6H4, R1 = Et, Pr, Bu) of 1-methylisoguanosine have been synthesized. All I were tested for A1 adenosine receptor affinity by using a (R)-{3H}-N6-(phenylisopropyl)adenosine binding assay. The 3-chlorophenyl group showed the greatest activity in the N1-position and the Bu group produced the greatest activity in the N5-position. Combination of the best substituent in each of these positions enhanced the overall activity. The most potent compound was I (R = 3-C6H4Cl, R1 = Bu) (II) with an IC50 of 6.4 × 10-6M. Selectivity at the receptor subclasses was examined by performing an A2 adenosine receptor affinity assay with [3H]CGS 21680. This series of compounds were slightly less potent at A2 receptors. II was the most potent compound with an IC50 of 19.2 × 10-6M.

《Synthesis and adenosine receptor affinity of a series of pyrazolo[3,4-d]pyrimidine analogs of 1-methylisoguanosine》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(5-Amino-1-(2-bromophenyl)-1H-pyrazole-4-carbonitrile)Category: benzothiophene.

Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Harden, Fiona A.; Quinn, Ronald J.; Scammells, Peter J. researched the compound: 5-Amino-1-(2-bromophenyl)-1H-pyrazole-4-carbonitrile( cas:71856-54-7 ).Reference of 5-Amino-1-(2-bromophenyl)-1H-pyrazole-4-carbonitrile.They published the article 《Synthesis and adenosine receptor affinity of a series of pyrazolo[3,4-d]pyrimidine analogs of 1-methylisoguanosine》 about this compound( cas:71856-54-7 ) in Journal of Medicinal Chemistry. Keywords: methylisoguanosine analog pyrazolopyrimidine; aminoalkylarylpyrazolopyrimidinone preparation adenosine receptor affinity. We’ll tell you more about this compound (cas:71856-54-7).

Two series of pyrazolo[3,4-d]pyrimidine analogs I (R = Ph, substituted Ph; R1 = Me; R = Ph, R1 = Et, Pr, Bu, Ph; R = 3-ClC6H4, R1 = Et, Pr, Bu) of 1-methylisoguanosine have been synthesized. All I were tested for A1 adenosine receptor affinity by using a (R)-{3H}-N6-(phenylisopropyl)adenosine binding assay. The 3-chlorophenyl group showed the greatest activity in the N1-position and the Bu group produced the greatest activity in the N5-position. Combination of the best substituent in each of these positions enhanced the overall activity. The most potent compound was I (R = 3-C6H4Cl, R1 = Bu) (II) with an IC50 of 6.4 × 10-6M. Selectivity at the receptor subclasses was examined by performing an A2 adenosine receptor affinity assay with [3H]CGS 21680. This series of compounds were slightly less potent at A2 receptors. II was the most potent compound with an IC50 of 19.2 × 10-6M.

《Synthesis and adenosine receptor affinity of a series of pyrazolo[3,4-d]pyrimidine analogs of 1-methylisoguanosine》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(5-Amino-1-(2-bromophenyl)-1H-pyrazole-4-carbonitrile)Reference of 5-Amino-1-(2-bromophenyl)-1H-pyrazole-4-carbonitrile.

Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Reference of tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate. 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: tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate, is researched, Molecular C13H24N2O3, CAS is 254905-58-3, about The influence of conformational restriction in the C-terminus of growth hormone secretagogues on their potency. Author is Peschke, Bernd; Ankersen, Michael; Bauer, Michael; Hansen, Thomas Kruse; Hansen, Birgit Sehested; Nielsen, Karin Kramer; Raun, Kirsten; Richter, Lutz; Westergaard, Lisbet.

In order to obtain more potent growth hormone secretagogues, a comparison of ipamorelin and NN703 suggested the addition of a polar group at the C-terminus of NN703. A study was conducted using constrained amines for this purpose. Here, substituted 4-piperidinylamino- and 4-dimethylaminopiperidino-substituents were found to give the most active compounds A replacement of the 4-dimethylaminopiperidino-substituent with 4-hydroxypiperidino resulted in a series of compounds, which showed in vitro activity with EC50 values in the low nanomolar range, and favorable kinetic properties, such as 40% oral bioavailability. The most promising compound was also tested in a swine in vivo model, resulting in a growth hormone level with a Cmax of over 40 ng mL-1.

《The influence of conformational restriction in the C-terminus of growth hormone secretagogues on their potency》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate)Reference of tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate.

Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Mallinger, Aurelie; Crumpler, Simon; Pichowicz, Mark; Waalboer, Dennis; Stubbs, Mark; Adeniji-Popoola, Olajumoke; Wood, Bozena; Smith, Elizabeth; Thai, Ching; Henley, Alan T.; Georgi, Katrin; Court, William; Hobbs, Steve; Box, Gary; Ortiz-Ruiz, Maria-Jesus; Valenti, Melanie; De Haven Brandon, Alexis; Te Poele, Robert; Leuthner, Birgitta; Workman, Paul; Aherne, Wynne; Poeschke, Oliver; Dale, Trevor; Wienke, Dirk; Esdar, Christina; Rohdich, Felix; Raynaud, Florence; Clarke, Paul A.; Eccles, Suzanne A.; Stieber, Frank; Schiemann, Kai; Blagg, Julian researched the compound: tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate( cas:254905-58-3 ).Product Details of 254905-58-3.They published the article 《Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen》 about this compound( cas:254905-58-3 ) in Journal of Medicinal Chemistry. Keywords: trisubstituted pyridine preparation bioavailability WNT signaling inhibitor antitumor. We’ll tell you more about this compound (cas:254905-58-3).

WNT signaling is frequently deregulated in malignancy, particularly in colon cancer, and plays a key role in the generation and maintenance of cancer stem cells. The authors report the discovery and optimization of a 3,4,5-trisubstituted pyridine, 1-(3,5-Dichloropyridin-4-yl)piperidine-4-carboxamide (9), using a high-throughput cell-based reporter assay of WNT pathway activity. The authors demonstrate a twisted conformation about the pyridine-piperidine bond of (9) by small-mol. x-ray crystallog. Medicinal chem. optimization to maintain this twisted conformation, cognisant of physicochem. properties likely to maintain good cell permeability, led to 8-[3-Chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]pyridin-4-yl]-2,8-diazaspiro[4,5]decan-1-one (74) (CCT251545), a potent small-mol. inhibitor of WNT signaling with good oral pharmacokinetics. The authors demonstrate inhibition of WNT pathway activity in a solid human tumor xenograft model with evidence for tumor growth inhibition following oral dosing. This work provides a successful example of hypothesis-driven medicinal chem. optimization from a singleton hit against a cell-based pathway assay without knowledge of the biochem. target.

Different reactions of this compound(tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate)Product Details of 254905-58-3 require different conditions, so the reaction conditions are very important.

Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

HPLC of Formula: 254905-58-3. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate, is researched, Molecular C13H24N2O3, CAS is 254905-58-3, about The influence of conformational restriction in the C-terminus of growth hormone secretagogues on their potency. Author is Peschke, Bernd; Ankersen, Michael; Bauer, Michael; Hansen, Thomas Kruse; Hansen, Birgit Sehested; Nielsen, Karin Kramer; Raun, Kirsten; Richter, Lutz; Westergaard, Lisbet.

In order to obtain more potent growth hormone secretagogues, a comparison of ipamorelin and NN703 suggested the addition of a polar group at the C-terminus of NN703. A study was conducted using constrained amines for this purpose. Here, substituted 4-piperidinylamino- and 4-dimethylaminopiperidino-substituents were found to give the most active compounds A replacement of the 4-dimethylaminopiperidino-substituent with 4-hydroxypiperidino resulted in a series of compounds, which showed in vitro activity with EC50 values in the low nanomolar range, and favorable kinetic properties, such as 40% oral bioavailability. The most promising compound was also tested in a swine in vivo model, resulting in a growth hormone level with a Cmax of over 40 ng mL-1.

Different reactions of this compound(tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate)HPLC of Formula: 254905-58-3 require different conditions, so the reaction conditions are very important.

Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

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, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen, published in 2015-02-26, which mentions a compound: 254905-58-3, Name is tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate, Molecular C13H24N2O3, Product Details of 254905-58-3.

WNT signaling is frequently deregulated in malignancy, particularly in colon cancer, and plays a key role in the generation and maintenance of cancer stem cells. The authors report the discovery and optimization of a 3,4,5-trisubstituted pyridine, 1-(3,5-Dichloropyridin-4-yl)piperidine-4-carboxamide (9), using a high-throughput cell-based reporter assay of WNT pathway activity. The authors demonstrate a twisted conformation about the pyridine-piperidine bond of (9) by small-mol. x-ray crystallog. Medicinal chem. optimization to maintain this twisted conformation, cognisant of physicochem. properties likely to maintain good cell permeability, led to 8-[3-Chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]pyridin-4-yl]-2,8-diazaspiro[4,5]decan-1-one (74) (CCT251545), a potent small-mol. inhibitor of WNT signaling with good oral pharmacokinetics. The authors demonstrate inhibition of WNT pathway activity in a solid human tumor xenograft model with evidence for tumor growth inhibition following oral dosing. This work provides a successful example of hypothesis-driven medicinal chem. optimization from a singleton hit against a cell-based pathway assay without knowledge of the biochem. target.

Different reactions of this compound(tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate)Product Details of 254905-58-3 require different conditions, so the reaction conditions are very important.

Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Category: benzothiophene. 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: tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate, is researched, Molecular C13H24N2O3, CAS is 254905-58-3, about The influence of conformational restriction in the C-terminus of growth hormone secretagogues on their potency. Author is Peschke, Bernd; Ankersen, Michael; Bauer, Michael; Hansen, Thomas Kruse; Hansen, Birgit Sehested; Nielsen, Karin Kramer; Raun, Kirsten; Richter, Lutz; Westergaard, Lisbet.

In order to obtain more potent growth hormone secretagogues, a comparison of ipamorelin and NN703 suggested the addition of a polar group at the C-terminus of NN703. A study was conducted using constrained amines for this purpose. Here, substituted 4-piperidinylamino- and 4-dimethylaminopiperidino-substituents were found to give the most active compounds A replacement of the 4-dimethylaminopiperidino-substituent with 4-hydroxypiperidino resulted in a series of compounds, which showed in vitro activity with EC50 values in the low nanomolar range, and favorable kinetic properties, such as 40% oral bioavailability. The most promising compound was also tested in a swine in vivo model, resulting in a growth hormone level with a Cmax of over 40 ng mL-1.

Different reactions of this compound(tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate)Category: benzothiophene require different conditions, so the reaction conditions are very important.

Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Product Details of 254905-58-3. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate, is researched, Molecular C13H24N2O3, CAS is 254905-58-3, about Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen.

WNT signaling is frequently deregulated in malignancy, particularly in colon cancer, and plays a key role in the generation and maintenance of cancer stem cells. The authors report the discovery and optimization of a 3,4,5-trisubstituted pyridine, 1-(3,5-Dichloropyridin-4-yl)piperidine-4-carboxamide (9), using a high-throughput cell-based reporter assay of WNT pathway activity. The authors demonstrate a twisted conformation about the pyridine-piperidine bond of (9) by small-mol. x-ray crystallog. Medicinal chem. optimization to maintain this twisted conformation, cognisant of physicochem. properties likely to maintain good cell permeability, led to 8-[3-Chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]pyridin-4-yl]-2,8-diazaspiro[4,5]decan-1-one (74) (CCT251545), a potent small-mol. inhibitor of WNT signaling with good oral pharmacokinetics. The authors demonstrate inhibition of WNT pathway activity in a solid human tumor xenograft model with evidence for tumor growth inhibition following oral dosing. This work provides a successful example of hypothesis-driven medicinal chem. optimization from a singleton hit against a cell-based pathway assay without knowledge of the biochem. target.

After consulting a lot of data, we found that this compound(254905-58-3)Product Details of 254905-58-3 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Synthesis and adenosine receptor affinity of a series of pyrazolo[3,4-d]pyrimidine analogs of 1-methylisoguanosine, published in 1991-09-30, which mentions a compound: 71856-54-7, mainly applied to methylisoguanosine analog pyrazolopyrimidine; aminoalkylarylpyrazolopyrimidinone preparation adenosine receptor affinity, Application In Synthesis of 5-Amino-1-(2-bromophenyl)-1H-pyrazole-4-carbonitrile.

Two series of pyrazolo[3,4-d]pyrimidine analogs I (R = Ph, substituted Ph; R1 = Me; R = Ph, R1 = Et, Pr, Bu, Ph; R = 3-ClC6H4, R1 = Et, Pr, Bu) of 1-methylisoguanosine have been synthesized. All I were tested for A1 adenosine receptor affinity by using a (R)-{3H}-N6-(phenylisopropyl)adenosine binding assay. The 3-chlorophenyl group showed the greatest activity in the N1-position and the Bu group produced the greatest activity in the N5-position. Combination of the best substituent in each of these positions enhanced the overall activity. The most potent compound was I (R = 3-C6H4Cl, R1 = Bu) (II) with an IC50 of 6.4 × 10-6M. Selectivity at the receptor subclasses was examined by performing an A2 adenosine receptor affinity assay with [3H]CGS 21680. This series of compounds were slightly less potent at A2 receptors. II was the most potent compound with an IC50 of 19.2 × 10-6M.

After consulting a lot of data, we found that this compound(71856-54-7)Application In Synthesis of 5-Amino-1-(2-bromophenyl)-1H-pyrazole-4-carbonitrile can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Related Products of 254905-58-3. 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: tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate, is researched, Molecular C13H24N2O3, CAS is 254905-58-3, about Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations. Author is de la Fuente Revenga, Mario; Balle, Thomas; Jensen, Anders A.; Froelund, Bente.

Exploration of small selective ligands for the nicotinic acetylcholine receptors (nAChRs) based on acetylcholine (ACh) has led to the development of potent agonists with clear preference for the α4β2 nAChR, the most prevalent nAChR subtype in the central nervous system. In this work the authors present the continuation of these efforts aimed at increasing this subtype selectivity by introduction of conformational restriction in the carbamoylcholine homolog, 3-(dimethylaminobutyl) dimethylcarbamate (DMABC). The results highlight the importance of the N-carbamoyl substitution in α4β2-subtype selectivity. Moreover, the authors have confirmed the non-linear conformation of DMABC bound to nAChRs suggested by recent crystal structures of the compound in complex with the Lymnaea stagnalis ACh binding protein.

Although many compounds look similar to this compound(254905-58-3)Related Products of 254905-58-3, numerous studies have shown that this compound(SMILES:O=C(N1CCC(C(N(C)C)=O)CC1)OC(C)(C)C), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem