Month: November 2022

Reduction of 1-substituted pyridinium salts was written by Acheson, R. Morrin;Paglietti, Giuseppe. And the article was included in Journal of the Chemical Society in 1976.Application In Synthesis of 1-Phenylpiperidine-3-carboxamide The following contents are mentioned in the article:

Addnl. data considered in abstracting and indexing are available from a source cited in the original document. Reduction of the pyridinium salts I (R = Ph, R1 = CONH2, R2 = H, X = Cl; R = Me, R1 = CN, R2 = H, X = I; R = Me, R1 = CONH2, R2 = H, X = MeSO4; R = PhCH2, R1 = H, R2 = Me, X = Br) with NaBH4 or Na2(S2O4) gave mixtures of mainly 1,2- and 1,4-dihydropyridines, which were analyzed by NMR. Pd-C-catalyzed hydrogenation of the dihydro derivatives gave isomerized products in some cases. This study involved multiple reactions and reactants, such as 1-Phenylpiperidine-3-carboxamide (cas: 58971-08-7Application In Synthesis of 1-Phenylpiperidine-3-carboxamide).

1-Phenylpiperidine-3-carboxamide (cas: 58971-08-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Application In Synthesis of 1-Phenylpiperidine-3-carboxamide

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis and FKBP binding of small molecule mimics of the tricarbonyl region of FK506 was written by Wang, Gary T.;Lane, Ben;Fesik, Stephen W.;Petros, Andrew;Luly, Jay;Krafft, Grant A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 1994.SDS of cas: 86069-86-5 The following contents are mentioned in the article:

Small acyclic model compounds were synthesized to examine the importance of the C(9) carbonyl group of FK506 for FKBP binding. 4-(4′-Methoxyphenyl)-1-Bu (3”,4”,5”-trimethoxyphenylglyoxyl)pipecolate, containing the N-(glyoxyl)pipecolate motif of FK506, was found to bind to FKBP with IC₅₀ of 16 μM. Replacement of the carbonyl group at the position corresponding to C(9) of FK506 with small nonpolar groups (hydrogen, methylene or Me group) significantly reduced the binding affinity. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5SDS of cas: 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.SDS of cas: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis and FKBP binding of small molecule mimics of the tricarbonyl region of FK506 was written by Wang, Gary T.;Lane, Ben;Fesik, Stephen W.;Petros, Andrew;Luly, Jay;Krafft, Grant A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 1994.Recommanded Product: 86069-86-5 The following contents are mentioned in the article:

Small acyclic model compounds were synthesized to examine the importance of the C(9) carbonyl group of FK506 for FKBP binding. 4-(4′-Methoxyphenyl)-1-Bu (3”,4”,5”-trimethoxyphenylglyoxyl)pipecolate, containing the N-(glyoxyl)pipecolate motif of FK506, was found to bind to FKBP with IC₅₀ of 16 μM. Replacement of the carbonyl group at the position corresponding to C(9) of FK506 with small nonpolar groups (hydrogen, methylene or Me group) significantly reduced the binding affinity. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Recommanded Product: 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Recommanded Product: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Total synthesis of the antifungal depsipeptide petriellin A was written by Sleebs, Marianne M.;Scanlon, Denis;Karas, John;Maharani, Rani;Hughes, Andrew B.. And the article was included in Journal of Organic Chemistry in 2011.HPLC of Formula: 86069-86-5 The following contents are mentioned in the article:

We report the solid-phase total synthesis of the antifungal highly modified cyclic depsipeptide petriellin A. The synthesis confirms earlier reports on the absolute configuration of the natural product. The solid-phase approach resulted in a protected linear precursor, which was cleaved from the solid support prior to cyclization and final deprotection. Use of advanced coupling agents for several hindered amides was a feature of the synthesis. The natural product was prepared in overall 5% yield. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5HPLC of Formula: 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.HPLC of Formula: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Total synthesis of the antifungal depsipeptide petriellin A was written by Sleebs, Marianne M.;Scanlon, Denis;Karas, John;Maharani, Rani;Hughes, Andrew B.. And the article was included in Journal of Organic Chemistry in 2011.Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

We report the solid-phase total synthesis of the antifungal highly modified cyclic depsipeptide petriellin A. The synthesis confirms earlier reports on the absolute configuration of the natural product. The solid-phase approach resulted in a protected linear precursor, which was cleaved from the solid support prior to cyclization and final deprotection. Use of advanced coupling agents for several hindered amides was a feature of the synthesis. The natural product was prepared in overall 5% yield. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

C-Terminal Residue Optimization and Fragment Merging: Discovery of a Potent Peptide-Hybrid Inhibitor of Dengue Protease was written by Behnam, Mira A. M.;Nitsche, Christoph;Vechi, Sergio M.;Klein, Christian D.. And the article was included in ACS Medicinal Chemistry Letters in 2014.Related Products of 86069-86-5 The following contents are mentioned in the article:

Dengue virus protease is a promising target for the development of antiviral drugs. We describe here a two-step rational optimization that led to the discovery of the potent inhibitor 35 with nanomolar binding affinity at dengue protease serotype 2 (IC₅₀ = 0.6 渭M, K_i = 0.4 渭M). First, a large number of natural and non-natural amino acids were screened at the C-terminal position of the previously reported, canonical peptide sequence (Cap-Arg-Lys-Nle-NH₂). Compared to the reference compound 1 (Bz-Arg-Lys-Nle-NH₂, IC₅₀ = 13.3 渭M), a 4-fold higher inhibitory potential was observed with the incorporation of a C-terminal phenylglycine (compound 9, IC₅₀ = 3.3 渭M). Second, we applied fragment merging of 9 with the previously reported thiazolidinedione peptide hybrid 33 (IC₅₀ = 2.5 渭M). This approach led to the fusion of two inhibitor-fragments with micromolar affinity into a 20-fold more potent, competitive inhibitor of dengue protease. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Related Products of 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Related Products of 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

C-Terminal Residue Optimization and Fragment Merging: Discovery of a Potent Peptide-Hybrid Inhibitor of Dengue Protease was written by Behnam, Mira A. M.;Nitsche, Christoph;Vechi, Sergio M.;Klein, Christian D.. And the article was included in ACS Medicinal Chemistry Letters in 2014.Electric Literature of C21H21NO4 The following contents are mentioned in the article:

Dengue virus protease is a promising target for the development of antiviral drugs. We describe here a two-step rational optimization that led to the discovery of the potent inhibitor 35 with nanomolar binding affinity at dengue protease serotype 2 (IC₅₀ = 0.6 渭M, K_i = 0.4 渭M). First, a large number of natural and non-natural amino acids were screened at the C-terminal position of the previously reported, canonical peptide sequence (Cap-Arg-Lys-Nle-NH₂). Compared to the reference compound 1 (Bz-Arg-Lys-Nle-NH₂, IC₅₀ = 13.3 渭M), a 4-fold higher inhibitory potential was observed with the incorporation of a C-terminal phenylglycine (compound 9, IC₅₀ = 3.3 渭M). Second, we applied fragment merging of 9 with the previously reported thiazolidinedione peptide hybrid 33 (IC₅₀ = 2.5 渭M). This approach led to the fusion of two inhibitor-fragments with micromolar affinity into a 20-fold more potent, competitive inhibitor of dengue protease. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Electric Literature of C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Electric Literature of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Neonicotine and isomeric pyridylpiperidines was written by Smith, C. R.. And the article was included in Journal of the American Chemical Society in 1931.Category: piperidines The following contents are mentioned in the article:

cf. C. A. 18, 2006. Details are given for the isolation of neonicotine (尾-pyridyl-伪-piperidine) (I) from the reaction product of C₅H₅N, Na and O; I b₇₇₅ 280-1掳 and yields a picrate, m. 213掳 (con.); this is probably not identical with nicotimine, isolated by Pictet and Rotschky (Ber. 34, 696(1901)) from the nicotine alkaloids. Reduction of I gives 伪,尾-dipiperidyl, b. 269-70掳. Reduction of 伪,尾-dipyridyl gives isoneonicotine (伪-pyridyl-尾-piperidine), b₇₆₀ 282掳, whose picrate m. 217-8掳 (corrected). 伪,伪-Pyridylpiperidyl, b₇₅₅ 265-6掳, whose picrate m. 187掳; the NO derivative is an oil. Isonicotine (纬,纬-pyridylpiperidine) b₇₆₀ 292掳; the picrate m. 215-8掳 (decomposition); the NO derivative m. 112掳. Nicotidine (尾,尾-pyridylpiperidine) b. 284-5掳; picrate m. about 206掳. 尾-Pyridyl-纬-piperidine yields a picrate, m. 240掳. The ease of reduction by Sn and HCl of the dipyridyls is in the order 纬,纬-, 尾,纬, 伪,伪- and 尾,尾, the first being the most easily reduced. This study involved multiple reactions and reactants, such as 3-(Piperidin-3-yl)pyridine (cas: 31251-28-2Category: piperidines).

3-(Piperidin-3-yl)pyridine (cas: 31251-28-2) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPAR纬 Modulator was written by Hartmann, Markus;Bibli, Sofia-Iris;Tews, Daniel;Ni, Xiaomin;Kircher, Theresa;Kramer, Jan S.;Kilu, Whitney;Heering, Jan;Hernandez-Olmos, Victor;Weizel, Lilia;Scriba, Gerhard K. E.;Krait, Sulaiman;Knapp, Stefan;Chaikuad, Apirat;Merk, Daniel;Fleming, Ingrid;Fischer-Posovszky, Pamela;Proschak, Ewgenij. And the article was included in Journal of Medicinal Chemistry in 2021.Category: piperidines The following contents are mentioned in the article:

The metabolic syndrome (MetS) is a constellation of cardiovascular and metabolic symptoms involving insulin resistance, steatohepatitis, obesity, hypertension, and heart disease, and patients suffering from MetS often require polypharmaceutical treatment. PPAR纬 agonists are highly effective oral antidiabetics with great potential in MetS, which promote adipocyte browning and insulin sensitization. However, the application of PPAR纬 agonists in clinics is restricted by potential cardiovascular adverse events. We have previously demonstrated that the racemic dual sEH/PPAR纬 modulator RB394 (3) simultaneously improves all risk factors of MetS in vivo. In this study, we identify and characterize (R)-3 (I), the eutomer of 3. We provide structural rationale for mol. recognition of the eutomer. Furthermore, we could show that the dual sEH/PPAR纬 modulator is able to promote adipocyte browning and simultaneously exhibits cardioprotective activity which underlines its exciting potential in treatment of MetS. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Category: piperidines).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Soluble epoxide hydrolase inhibitor, TPPU, increases regulatory T cells pathway in an arthritis model was written by Trindade-da-Silva, Carlos A.;Clemente-Napimoga, Juliana T.;Abdalla, Henrique B.;Rosa, Sergio Marcolino;Ueira-Vieira, Carlos;Morisseau, Christophe;Verri, Waldiceu A. Jr;Montalli, Victor Angelo Martins;Hammock, Bruce D.;Napimoga, Marcelo H.. And the article was included in FASEB Journal in 2020.Application of 1222780-33-7 The following contents are mentioned in the article:

Epoxyeicosatrienoic acids (EET) and related epoxy fatty acids (EpFA) are endogenous anti-inflammatory compounds, which are converted by the soluble epoxide hydrolase (sEH) to dihydroxylethersatrienoic acids (DHETs) with lessened biol. effects. Inhibition of sEH is used as a strategy to increase EET levels leading to lower inflammation. Rheumatoid arthritis is a chronic autoimmune disease that leads to destruction of joint tissues. This pathogenesis involves a complex interplay between the immune system, and environmental factors. Here, we investigate the effects of inhibiting sEH with 1-trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl) urea (TPPU) on a collagen-induced arthritis model. The treatment with TPPU ameliorates hyperalgesia, edema, and decreases the expression of important pro-inflammatory cytokines of Th1 and Th17 profiles, while increasing Treg cells. Considering the challenges to control RA, this study provides robust data supporting that inhibition of the sEH is a promising target to treat arthritis. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Application of 1222780-33-7).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Application of 1222780-33-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem