Day: November 25, 2022

Synthesis and SAR of substituted tetrahydrocarbazole derivatives as new NPY-1 antagonists was written by Di Fabio, Romano;Giovannini, Riccardo;Bertani, Barbara;Borriello, Manuela;Bozzoli, Andrea;Donati, Daniele;Falchi, Alessandro;Ghirlanda, Damiano;Leslie, Colin P.;Pecunioso, Angelo;Rumboldt, Giovanna;Spada, Simone. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2006.Product Details of 882033-93-4 The following contents are mentioned in the article:

The SAR of a new series of tetrahydrocarbazole derivatives I [R¹ = Me, 3-(1-piperidinyl)propyl, piperidin-4-ylmethyl, etc.; R² = H, 4-morpholinyl, 1-piperidinyl, 4-methyl-1-piperazinyl, etc.] is evaluated: the appropriate decoration of this template led to the identification of a new class of NPY-1 antagonists showing good in vitro potency and a promising in vivo pharmacokinetic profile in rat. This study involved multiple reactions and reactants, such as (3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4Product Details of 882033-93-4).

(3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4) 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. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Product Details of 882033-93-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Development of single and mixed isoform selectivity PI3Kδ inhibitors by targeting Asn836 of PI3Kδ was written by Miller, Michelle S.;Mountford, Simon J.;Pinson, Jo-Anne;Zheng, Zhaohua;Kunzli, Marco;Patel, Vanit;Hogg, Simon J.;Shortt, Jake;Jennings, Ian G.;Thompson, Philip E.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2016.Recommanded Product: 86069-86-5 The following contents are mentioned in the article:

A series of PI3Kδ inhibitors derived from the pan-PI3K inhibitor ZSTK474 was prepared that target a non-conserved region of the catalytic site. Dependent upon the substituents present, these analogs show different levels of isoform selectivity and sensitivity to the mutation N836D in PI3Kδ. As a marker of ‘on-target’ activity and permeability, a selection of the most potent PI3Kδ inhibitors were shown to inhibit pAkt production in the Nawalma Burkitt lymphoma cell line. 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. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. 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.Recommanded Product: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Development of single and mixed isoform selectivity PI3Kδ inhibitors by targeting Asn836 of PI3Kδ was written by Miller, Michelle S.;Mountford, Simon J.;Pinson, Jo-Anne;Zheng, Zhaohua;Kunzli, Marco;Patel, Vanit;Hogg, Simon J.;Shortt, Jake;Jennings, Ian G.;Thompson, Philip E.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2016.Recommanded Product: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

A series of PI3Kδ inhibitors derived from the pan-PI3K inhibitor ZSTK474 was prepared that target a non-conserved region of the catalytic site. Dependent upon the substituents present, these analogs show different levels of isoform selectivity and sensitivity to the mutation N836D in PI3Kδ. As a marker of ‘on-target’ activity and permeability, a selection of the most potent PI3Kδ inhibitors were shown to inhibit pAkt production in the Nawalma Burkitt lymphoma cell line. 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.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 derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Recommanded Product: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Mechanism of local anesthetic action. 1. Receptor problem was written by Schultz, Otto E.;Ziegler, A.. And the article was included in Pharmazie in 1970.COA of Formula: C8H11NO4 The following contents are mentioned in the article:

Furfuryl alc. was treated 1 hr at -5° with PBr3 and the product treated with MeNH2 and alc. NaI 72 hr at 100-20° to give I. Treatment of I with HBr-HOAc gave a ring-opened product which was cyclized with KOH to give 63% II. Similarly prepared were 10 other compounds including III, IV, V, VI, and VII. The local anesthetic activity of these compounds vs. procaine-HCl (III) was determined III had 80% of the VIII activity. The mechanism of local anesthetic activity is discussed. This study involved multiple reactions and reactants, such as Ethyl 2,3-dioxopiperidine-4-carboxylate (cas: 30727-21-0COA of Formula: C8H11NO4).

Ethyl 2,3-dioxopiperidine-4-carboxylate (cas: 30727-21-0) 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.COA of Formula: C8H11NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Structure-Activity Relationship Studies of Targeting Ligands against Breast Cancer Cells was written by Yao, Nianhuan;Xiao, Wenwu;Meza, Leah;Tseng, Harry;Chuck, Mathida;Lam, Kit S.. And the article was included in Journal of Medicinal Chemistry in 2009.Product Details of 86069-86-5 The following contents are mentioned in the article:

A series of LXY3 analogs was designed and synthesized. Their binding affinity was demonstrated using MDA-MB-231 breast cancer cells adherence inhibition assay. Further structure-activity relationship was obtained. One analog was discovered to have 3.5-fold increase of the binding affinity. Fluorescent microscopy and in vivo and ex vivo imaging studies demonstrated that it is an efficient in vivo targeting agent against α3 integrin of MDA-MB-231 breast tumor xenograft implant. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Product Details of 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 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.Product Details of 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Structure-Activity Relationship Studies of Targeting Ligands against Breast Cancer Cells was written by Yao, Nianhuan;Xiao, Wenwu;Meza, Leah;Tseng, Harry;Chuck, Mathida;Lam, Kit S.. And the article was included in Journal of Medicinal Chemistry in 2009.Name: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

A series of LXY3 analogs was designed and synthesized. Their binding affinity was demonstrated using MDA-MB-231 breast cancer cells adherence inhibition assay. Further structure-activity relationship was obtained. One analog was discovered to have 3.5-fold increase of the binding affinity. Fluorescent microscopy and in vivo and ex vivo imaging studies demonstrated that it is an efficient in vivo targeting agent against α3 integrin of MDA-MB-231 breast tumor xenograft implant. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Name: (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. 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.Name: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Anti-histamines boost immunotherapy was written by Cully, Megan. And the article was included in Nature Reviews Drug Discovery in 2022.Synthetic Route of C32H39NO4 The following contents are mentioned in the article:

A review. ICB with anti-PD1, anti-PDL1 or anti-CTLA4 antibodies has been particularly useful in melanoma. A similar trend was observed in individuals with lung, breast or colon cancer. Bone marrow- derived macrophages (BMDMs) from mice lacking hrh1 , which encodes H 1 receptor, or wild-type BMDMs treated with the H 1 -directed antihistamine, fexofenadine, had anti-inflammatory features. Ex vivo, these BMDMs stimulated T cells, and those T cells had increased tumor cell killing. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Synthetic Route of C32H39NO4).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Synthetic Route of C32H39NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

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