Category: 96651-85-3

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 96651-85-3, is researched, Molecular C13H18ClN, about Spirovesamicols: Conformationally Restricted Analogs of 2-(4-Phenylpiperidino)cyclohexanol (Vesamicol, AH5183) as Potential Modulators of Presynaptic Cholinergic Function, the main research direction is spirovesamicol preparation vesamicol receptor ligand structure; cholinergic neurotransmission spirovesamicol vesamicol receptor ligand.SDS of cas: 96651-85-3.

In an effort to develop selective inhibitors of vesicular acetylcholine storage, the authors have synthesized a series of semirigid vesamicol receptor ligands based on the structure of 2-(4-phenylpiperidino)cyclohexanol (vesamicol, AH5183). In these compounds, the planes of the Ph and piperidyl moieties of the parent ligand vesamicol are held at right angles by vinyl, ethylene, and propylene bridges to form N-substituted derivatives of spiro[indene-1,4′-piperidine], 2,3-dihydrospiro[indene-1,4′-piperidine], and 3,4-dihydrospiro[naphthalene-1(2H),4′-piperidine], resp. Preliminary evaluation of these compounds in elec. organ synaptic vesicles revealed several potent vesamicol receptor ligands, such as1′-(2-hydroxy-1,2,3,4-tetrahydronaphth-3-yl)spiro[1H-indene-1,4′-piperidine] and 1′-(2-hydroxy-1,2,3,4-tetrahydronaphth-3-yl)spiro[2-bromo-1H-indene-1,4′-piperidine], which display subnanomolar affinity for this receptor. In general, the vinyl and ethylene bridges yielded the most potent analogs while the propylene-bridged analogs were among the least potent compounds The increased rigidity of these spiro-fused compounds, relative to the corresponding simple 4-phenylpiperidine derivatives of vesamicol, is expected to confer greater selectivity for the vesamicol receptor.

This compound(2,3-Dihydrospiro[indene-1,4′-piperidine] hydrochloride)SDS of cas: 96651-85-3 was discussed at the molecular level, the effects of temperature and reaction time on the properties of the compound were discussed, and the optimum reaction conditions were selected.

Reference:
Benzoxazole – Wikipedia,
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Hayashi, Shigeo; Ohashi, Katsuyo; Mihara, Sachiko; Nakata, Eriko; Emoto, Chie; Ohta, Atsuko published an article about the compound: 2,3-Dihydrospiro[indene-1,4′-piperidine] hydrochloride( cas:96651-85-3,SMILESS:Cl.C1CC2(CCNCC2)C2=CC=CC=C12 ).Synthetic Route of C13H18ClN. 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:96651-85-3) through the article.

A series of (4-arylpiperidine substituted-methyl)-[bicyclic (hetero)cycloalkanobenzene] analogs, e.g., I was designed, synthesized, and biol. evaluated in vitro to seek and identify potent and selective small-mols. of nonpeptide NOP receptor antagonists, which resulted in the discovery of novel potent small-mol. II with high human NOP receptor selectivity over human μ receptor. The structure-activity relationship of the potency and selectivity, structure-metabolic stability relationship, and SAR of hERG (human ether-a-go-go related gene) potassium ion channel binding affinity for the analogs in the present studies in vitro provided significant and/or useful structural determinants and insights for the resp. purposes. The superior profiles of compound II were discussed with a viewpoint of multisite interactions between ligand and NOP receptor, together with the results of previous NOP receptor agonist/antagonist studies.

《Discovery of small-molecule nonpeptide antagonists of nociceptin/orphanin FQ receptor: The studies of design, synthesis, and structure-activity relationships for (4-arylpiperidine substituted-methyl)-[bicyclic (hetero)cycloalkanobenzene] derivatives》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(2,3-Dihydrospiro[indene-1,4′-piperidine] hydrochloride)Synthetic Route of C13H18ClN.

Reference:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 96651-85-3, is researched, SMILESS is Cl.C1CC2(CCNCC2)C2=CC=CC=C12, Molecular C13H18ClNJournal, Bioorganic & Medicinal Chemistry Letters called Peptidomimetic growth hormone secretagogues: synthesis and biological activities of analogs varied at the indole nucleus of the prototypical spiropiperidine L-162,752, Author is Nargund, Ravi P.; Chen, Meng-Hsin; Johnston, David B. R.; Barakat, Khaled J.; Tata, James R.; Cheng, Kang; Jacks, Thomas M.; Chan, Wanda W.-S.; Wei, Liente, the main research direction is spiropiperidine preparation growth hormone secretagogue; structure activity spiropiperidine growth hormone secretagogue; L 162752 analog growth hormone secretagogue.Product Details of 96651-85-3.

SAR studies around the indole nucleus of the prototypical peptidomimetic L-162,752 (I; R = 3-indolyl) revealed that the D-Trp residue could be replaced with 3-phenylpropyl-D-glycine and O-benzyl-D-serine to provide secretagogues I (R = PhCH2CH2, PhCH2O) with comparable intrinsic activity but with significantly better and oral activity in dogs. Use of dimethyl-β-alanine amino side chains led to considerable loss of activity in the D-homophenylalanine and O-benzyl-D-serine series II [R = PhCH2CH2, PhCH2O; R1 = H. CH2CH(OH)Me, CH2CH(OH)CH2OH] .

The article 《Peptidomimetic growth hormone secretagogues: synthesis and biological activities of analogs varied at the indole nucleus of the prototypical spiropiperidine L-162,752》 also mentions many details about this compound(96651-85-3)Product Details of 96651-85-3, you can pay attention to it, because details determine success or failure

Reference:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 96651-85-3, is researched, Molecular C13H18ClN, about Spiropiperidines as high-affinity, selective σ ligands., the main research direction is spiropiperidine selective sigma ligand; tetralin spiropiperidino selective sigma ligand; indan spiropiperidino selective sigma ligand; benzocycloheptane spiropiperidino selective sigma ligand; radioligand displacement spiropiperidinobenzocycloalkane; structure activity spiropiperidinobenzocycloalkane receptor binding.Related Products of 96651-85-3.

A variety of achiral conformationally restricted spirocyclic piperidines were prepared in an attempt to investigate the functional role of the central σ recognition site. All compounds possessed a lipophilic N-substituent incorporating either a tetralin (I; n = 2, R = PhCH2, Bu, hexyl, 2-picolyl, cyclohexylmethyl, CH2CH:CH2, 2-furylmethyl, 2-thienylmethyl, CH2CH:CMe2, etc.), indan (I; n = 1, R = PhCH2, PhCH2CH2, CH2CH:CMe2, Bu, etc.), or benzocycloheptane skeleton (I; n = 3, R = PhCH2, Bu). Their in vitro affinity at the σ site was assessed in radioligand displacement experiments with guinea pig cerebellum homogenates using the σ-specific radioligand N,N-di-o-[5-3H]-tolylguanidine (II). A study of the structure-activity relationships identified the N-Bu and N-dimethylallyl substituents as the optimum groups for high affinity and selectivity at the σ site, e.g., I (n = 1, R = CH2CH:CMe2), pIC50 = 8.9 vs II and >10,000-fold selective over the dopamine D2 receptor. Such compounds are amongst the highest affinity σ ligands reported to date, with excellent selectivity over the dopamine D2 receptor, and may serve as a useful tool for exploring the physiol. role of the σ site.

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Reference:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – 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.Efange, Simon M. N.; Kamath, Ashok P.; Khare, Anil B.; Kung, Mei-Ping; Mach, Robert H.; Parsons, Stanley M. researched the compound: 2,3-Dihydrospiro[indene-1,4′-piperidine] hydrochloride( cas:96651-85-3 ).Application of 96651-85-3.They published the article 《N-Hydroxyalkyl Derivatives of 3β-Phenyltropane and 1-Methylspiro[1H-indoline-3,4′-piperidine]: Vesamicol Analogs with Affinity for Monoamine Transporters》 about this compound( cas:96651-85-3 ) in Journal of Medicinal Chemistry. Keywords: monoamine transporter phenyltropane derivative preparation structure; methylspiro indolinepiperidine preparation monoamine transporter structure. We’ll tell you more about this compound (cas:96651-85-3).

As part of our ongoing structure-activity studies of the vesicular acetylcholine transporter ligand 2-(4-phenylpiperidino)cyclohexanol (vesamicol), N-hydroxy(phenyl)alkyl derivatives of 3β-phenyltropane, and 1-methylspiro[1H-indoline-3,4′-piperidine] were synthesized and tested for binding in vitro. Although a few compounds displayed moderately high affinity for the vesicular acetylcholine transporter, no compound was more potent than the prototypical vesicular acetylcholine transporter ligand vesamicol. However, a few compounds displayed higher affinity for the dopamine transporter than cocaine. We conclude that modification of the piperidyl fragment of vesamicol will not lead to more potent vesicular acetylcholine transporter ligands.

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Reference:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – 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 The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470), published in 2016-12-22, which mentions a compound: 96651-85-3, mainly applied to GPR40 agonist diabetes, Category: benzoxazole.

The G protein-coupled receptor 40 (GPR40) also known as Free Fatty Acid Receptor 1 (FFAR1) is highly expressed in pancreatic, islet β-cells and responds to endogenous fatty acids resulting in amplification of insulin secretion only in the presence of elevated glucose levels. Hypothesis driven structural modifications to endogenous FFAs, focused on breaking planarity and reducing lipophilicity, led to the identification of spiropiperidine and tetrahydroquinoline acid derivatives as GPR40 agonists with unique pharmacol., selectivity and pharmacokinetic properties. Compounds 1 (LY2881835), 2 (LY2922083) and 3 (LY2922470) demonstrated potent, efficacious and durable dose dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion during preclin. testing. A clin. study with 3 administered to subjects with T2DM provided proof of concept of 3 as a potential glucose-lowering therapy. This manuscript summarizes the scientific rationale, medicinal chem., preclin. and early development data of this new class of GPR40 agonists.

If you want to learn more about this compound(2,3-Dihydrospiro[indene-1,4′-piperidine] hydrochloride)Category: benzoxazole, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(96651-85-3).

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Recommanded Product: 2,3-Dihydrospiro[indene-1,4′-piperidine] hydrochloride. 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: 2,3-Dihydrospiro[indene-1,4′-piperidine] hydrochloride, is researched, Molecular C13H18ClN, CAS is 96651-85-3, about Indolyl Azaspiroketal Mannich Bases Are Potent Antimycobacterial Agents with Selective Membrane Permeabilizing Effects and in Vivo Activity.

The inclusion of an azaspiroketal Mannich base in the membrane targeting antitubercular 6-methoxy-1-n-octyl-1H-indole scaffold resulted in analogs with improved selectivity and submicromolar activity against Mycobacterium tuberculosis H37Rv. The potency enhancing properties of the spiro-ring fused motif was affirmed by SAR and validated in a mouse model of tuberculosis. As expected for membrane inserting agents, the indolyl azaspiroketal Mannich bases perturbed phospholipid vesicles, permeabilized bacterial cells and induced the mycobacterial cell envelope stress reporter promoter piniBAC. Surprisingly, their membrane disruptive effects did not appear to be associated with bacterial membrane depolarization. This profile was not uniquely associated with azaspiroketal Mannich bases but was characteristic of indolyl Mannich bases as a class. Whereas resistant mycobacteria could not be isolated for a less potent indolyl Mannich base, the more potent azaspiroketal analog displayed low spontaneous resistance mutation frequency of 10-8/CFU. This may indicate involvement of an addnl. envelope-related target in its mechanism of action.

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Reference:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Name: 2,3-Dihydrospiro[indene-1,4′-piperidine] hydrochloride. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 2,3-Dihydrospiro[indene-1,4′-piperidine] hydrochloride, is researched, Molecular C13H18ClN, CAS is 96651-85-3, about Efficient design, synthesis and structure-activity relationship studies of 1-(3′-substituted propyl)-4-arylpiperidines as non-peptide antagonists of nociceptin/orphanin FQ receptor: biological activities, metabolic stabilities and hERG channel bindings. Author is Hayashi, Shigeo; Ohashi, Katsuyo; Nakata, Eriko; Emoto, Chie.

Nociceptin/orphanin FQ (N/OFQ) is an endogenous heptadecapeptide that is a metabolite of precursor polypeptide (prepro-N/OFQ), and N/OFQ peptide (NOP) receptor (or opioid-receptor-like-1 receptor) is a G-protein-coupled receptor (GPCR) that is distinct from classical opioid peptide receptors, whereas the receptors share high sequence-similarities. As well, [35S]-guanosine 5′-(γ-thiotriphosphate) binding that was stimulated by N/OFQ-NOP receptor binding was not affected by various GPCR antagonists including opioid receptor antagonists. N/OFQ and NOP receptor are located in the spinal cord, the peripheral nervous systems and other peripheral tissues that are related to pain-inhibitory signal transmissions, and in the corticolimbic regions that are involved in the integration of the emotional components. Indeed, potent and selective new-class NOP receptor agonists as systemically potent analgesic against neuropathic pain and as orally potent anxiolytic with resp. unique safe-profiles have been discovered in our studies. Besides, the blockade of N/OFQ actions via N/OFQ-NOP receptor system has been displayed as anti-depression effect, anti-hyperplasia effect and anti-hypotension effect in animal model studies, which might show potential utilities of NOP receptor antagonists to modulate/attenuate N/OFQ activity for regulation of human physiologies in pharmacol. and clin. viewpoints. Hence, the design, synthesis, structure-activity relationship in vitro and structure-metabolic stability relationship in vitro of various 1-(3′-substituted propyl)-4-arylpiperidine derivatives, e.g., I, were investigated to seek and identify potent and selective new-class NOP receptor antagonists with metabolic stabilities and little hERG ion channel binding affinities by multi-viewpoint and integrated drug-design strategies, with clarifying structural features and physicochem. properties as key factors for the purposes. The unique and efficient studies, and their exclusive results and findings for the analogs are described herein.

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Reference:
Benzoxazole – Wikipedia,
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