Tag: 300-400

Analogues of arginine vasopressin modified in the N-terminal part of the molecule with pipecolic acid isomers was written by Sobolewski, Dariusz;Prahl, Adam;Slaninova, Jirina;Lammek, Bernard. And the article was included in Advances in Experimental Medicine and Biology in 2009.Synthetic Route of C21H21NO4 The following contents are mentioned in the article:

This study evaluated ten newly designed analogs of arginine vasopressin modified in the N-terminal part of the mol. with pipecolic acid (Pip) isomers. In general, the data was not impressive in terms of biol. activities of the reported analogs, but it provides important information on structure-activity relationships and response of the L- or D-Pip-containing peptides to standard trifluoroacetic acid cleavage conditions. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Synthetic Route of C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Synthetic Route of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Analogues of arginine vasopressin modified in the N-terminal part of the molecule with pipecolic acid isomers was written by Sobolewski, Dariusz;Prahl, Adam;Slaninova, Jirina;Lammek, Bernard. And the article was included in Advances in Experimental Medicine and Biology in 2009.Recommanded Product: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

This study evaluated ten newly designed analogs of arginine vasopressin modified in the N-terminal part of the mol. with pipecolic acid (Pip) isomers. In general, the data was not impressive in terms of biol. activities of the reported analogs, but it provides important information on structure-activity relationships and response of the L- or D-Pip-containing peptides to standard trifluoroacetic acid cleavage conditions. 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: (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. 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. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Recommanded Product: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Design and Application of a DNA-Encoded Macrocyclic Peptide Library was written by Zhu, Zhengrong;Shaginian, Alex;Grady, LaShadric C.;O’Keeffe, Thomas;Shi, Xiangguo E.;Davie, Christopher P.;Simpson, Graham L.;Messer, Jeffrey A.;Evindar, Ghotas;Bream, Robert N.;Thansandote, Praew P.;Prentice, Naomi R.;Mason, Andrew M.;Pal, Sandeep. And the article was included in ACS Chemical Biology in 2018.COA of Formula: C21H21NO4 The following contents are mentioned in the article:

A DNA-encoded macrocyclic peptide library was designed and synthesized with 2.4 × 10¹² members composed of 4-20 natural and non-natural amino acids. Affinity-based selection was performed against two therapeutic targets, VHL and RSV N protein. On the basis of selection data, some peptides were selected for resynthesis without a DNA tag, and their activity was confirmed. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5COA of Formula: C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.COA of Formula: C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Design and Application of a DNA-Encoded Macrocyclic Peptide Library was written by Zhu, Zhengrong;Shaginian, Alex;Grady, LaShadric C.;O’Keeffe, Thomas;Shi, Xiangguo E.;Davie, Christopher P.;Simpson, Graham L.;Messer, Jeffrey A.;Evindar, Ghotas;Bream, Robert N.;Thansandote, Praew P.;Prentice, Naomi R.;Mason, Andrew M.;Pal, Sandeep. And the article was included in ACS Chemical Biology in 2018.Synthetic Route of C21H21NO4 The following contents are mentioned in the article:

A DNA-encoded macrocyclic peptide library was designed and synthesized with 2.4 × 10¹² members composed of 4-20 natural and non-natural amino acids. Affinity-based selection was performed against two therapeutic targets, VHL and RSV N protein. On the basis of selection data, some peptides were selected for resynthesis without a DNA tag, and their activity was confirmed. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Synthetic Route of C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. 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.Synthetic Route of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Total synthesis of antascomicin B was written by Brittain, Dominic E. A.;Griffiths-Jones, Charlotte M.;Linder, Michael R.;Smith, Martin D.;McCusker, Catherine;Barlow, Jaqueline S.;Akiyama, Ryo;Yasuda, Kosuke;Ley, Steven V.. And the article was included in Angewandte Chemie, International Edition in 2005.Reference of 86069-86-5 The following contents are mentioned in the article:

The structurally enticing antascomicin B (I), which exhibits potent immunosuppressant-antagonizing properties, has a complex polyketide structure. Key steps in its enantioselective total synthesis include a transannular catechol-templated Dieckmann reaction to assemble the challenging tricarbonyl functionality and a butanediacetal-directed allylation. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Reference 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 saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Reference of 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Identification of the Key Residue of Calcitonin Gene Related Peptide (CGRP) 27-37 to Obtain Antagonists with Picomolar Affinity at the CGRP Receptor was written by Lang, Manja;De Pol, Silvia;Baldauf, Carsten;Hofmann, Hans-Joerg;Reiser, Oliver;Beck-Sickinger, Annette G.. And the article was included in Journal of Medicinal Chemistry in 2006.Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Calcitonin gene related peptide (CGRP) plays an important role in the CNS and in the cardiovascular system. To identify high-affinity antagonists in competitive binding studies, the authors identified a novel radioactive tracer, [³H-propionyl-K²⁴]-h伪CGRP 8-37, which was labeled in solution by a recently developed strategy using photolabile protecting groups at reactive side chains. This tracer was shown to be as potent as com. available ¹²⁵I-tracers for the determination of agonists and to have increased sensitivity for antagonists. The authors applied it to investigate the predicted turn structures centered at Pro²⁹ and Pro³⁴. The substitution at positions 29 and 34 by turn-inducing amino acid mimetica showed that these turns are highly diverse. At position 29, a hydrophobic residue is preferred that constricts the secondary structure, whereas position 34 is required to stabilize the conformation of the backbone. All high-affinity analogs showed antagonistic properties with potency similar to CGRP 8-37. 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 is a metabolite of cadaverine, a polyamine found in the human intestine. 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 In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Macrocyclic FKBP51 Ligands Define a Transient Binding Mode with Enhanced Selectivity was written by Voll, Andreas M.;Meyners, Christian;Taubert, Martha C.;Bajaj, Thomas;Heymann, Tim;Merz, Stephanie;Charalampidou, Anna;Kolos, Juergen;Purder, Patrick L.;Geiger, Thomas M.;Wessig, Pablo;Gassen, Nils C.;Bracher, Andreas;Hausch, Felix. And the article was included in Angewandte Chemie, International Edition in 2021.Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Subtype selectivity represents a challenge in many drug discovery campaigns. A typical example is the FK506 binding protein 51 (FKBP51), which has emerged as an attractive drug target. The most advanced FKBP51 ligands of the SAFit class are highly selective vs. FKBP52 but poorly discriminate against the homologs and off-targets FKBP12 and FKBP12.6. During a macrocyclization pilot study, we observed that many of these macrocyclic analogs have unanticipated and unprecedented preference for FKBP51 over FKBP12 and FKBP12.6. Structural studies revealed that these macrocycles bind with a new binding mode featuring a transient conformation, which is disfavored for the small FKBPs. Using a conformation-sensitive assay we show that this binding mode occurs in solution and is characteristic for this new class of compounds The discovered macrocycles are non-immunosuppressive, engage FKBP51 in cells, and block the cellular effect of FKBP51 on IKK伪. Our findings provide a new chem. scaffold for improved FKBP51 ligands and the structural basis for enhanced selectivity. 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. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. 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

Macrocyclic FKBP51 Ligands Define a Transient Binding Mode with Enhanced Selectivity was written by Voll, Andreas M.;Meyners, Christian;Taubert, Martha C.;Bajaj, Thomas;Heymann, Tim;Merz, Stephanie;Charalampidou, Anna;Kolos, Juergen;Purder, Patrick L.;Geiger, Thomas M.;Wessig, Pablo;Gassen, Nils C.;Bracher, Andreas;Hausch, Felix. And the article was included in Angewandte Chemie, International Edition in 2021.Electric Literature of C21H21NO4 The following contents are mentioned in the article:

Subtype selectivity represents a challenge in many drug discovery campaigns. A typical example is the FK506 binding protein 51 (FKBP51), which has emerged as an attractive drug target. The most advanced FKBP51 ligands of the SAFit class are highly selective vs. FKBP52 but poorly discriminate against the homologs and off-targets FKBP12 and FKBP12.6. During a macrocyclization pilot study, we observed that many of these macrocyclic analogs have unanticipated and unprecedented preference for FKBP51 over FKBP12 and FKBP12.6. Structural studies revealed that these macrocycles bind with a new binding mode featuring a transient conformation, which is disfavored for the small FKBPs. Using a conformation-sensitive assay we show that this binding mode occurs in solution and is characteristic for this new class of compounds The discovered macrocycles are non-immunosuppressive, engage FKBP51 in cells, and block the cellular effect of FKBP51 on IKK伪. Our findings provide a new chem. scaffold for improved FKBP51 ligands and the structural basis for enhanced selectivity. 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. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Electric Literature of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Brain-targeted chemical delivery of [Leu², Pip³]-TRH: synthesis and biological evaluation was written by Yoon, S.-H.;Wu, J.;Wu, W.-M.;Prokai, L.;Bodor, N.. And the article was included in Bioorganic & Medicinal Chemistry in 2000.Synthetic Route of C21H21NO4 The following contents are mentioned in the article:

A chem. targeting system for [Leu², Pip³]-TRH (Gln,Leu,Pip) was synthesized in order to allow its specific delivery to the central nervous system (CNS). Sequential metabolism of the obtained ‘packaged’ chem. delivery system, (CDS), DHT-Pro-Pro-Gln-Leu-Pip-OCh, should yield a ‘locked-in’ precursor following the oxidative conversion of the dihydrotrigonellyl (DHT) to the trigonellyl (T⁺) moiety, followed by removal of the cholesteryl function and cleavage of the T⁺-Pro-Pro by prolyl endopeptidase. The antagonism of barbiturate-induced sleeping time was used to assess the activity of the CDS. The sleeping time after administration of vehicle and [Leu²]-TRH was 100.5卤6.3 min, and 78.2卤4.7 min, resp. The [Leu², Pip³]-TRH-CDS showed a significant decrease in sleeping time (58.2卤3.4 min) compared to the vehicle or [Leu²]-TRH. These results indicate successful brain delivery of the precursor construct, and an effective release of the active GlnLeuPip in the brain. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Synthetic Route of C21H21NO4).

(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. 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.Synthetic Route of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Brain-targeted chemical delivery of [Leu², Pip³]-TRH: synthesis and biological evaluation was written by Yoon, S.-H.;Wu, J.;Wu, W.-M.;Prokai, L.;Bodor, N.. And the article was included in Bioorganic & Medicinal Chemistry in 2000.COA of Formula: C21H21NO4 The following contents are mentioned in the article:

A chem. targeting system for [Leu², Pip³]-TRH (Gln,Leu,Pip) was synthesized in order to allow its specific delivery to the central nervous system (CNS). Sequential metabolism of the obtained ‘packaged’ chem. delivery system, (CDS), DHT-Pro-Pro-Gln-Leu-Pip-OCh, should yield a ‘locked-in’ precursor following the oxidative conversion of the dihydrotrigonellyl (DHT) to the trigonellyl (T⁺) moiety, followed by removal of the cholesteryl function and cleavage of the T⁺-Pro-Pro by prolyl endopeptidase. The antagonism of barbiturate-induced sleeping time was used to assess the activity of the CDS. The sleeping time after administration of vehicle and [Leu²]-TRH was 100.5卤6.3 min, and 78.2卤4.7 min, resp. The [Leu², Pip³]-TRH-CDS showed a significant decrease in sleeping time (58.2卤3.4 min) compared to the vehicle or [Leu²]-TRH. These results indicate successful brain delivery of the precursor construct, and an effective release of the active GlnLeuPip in the brain. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5COA of Formula: C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.COA of Formula: C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem