Tag: 200-300

The author of 《An optimised series of substituted N-phenylpyrrolamides as DNA gyrase B inhibitors》 were Tiz, Davide Benedetto; Skok, Ziga; Durcik, Martina; Tomasic, Tihomir; Masic, Lucija Peterlin; Ilas, Janez; Zega, Anamarija; Draskovits, Gabor; Revesz, Tamas; Nyerges, Akos; Pal, Csaba; Cruz, Cristina D.; Tammela, Paivi; Zigon, Dusan; Kikelj, Danijel; Zidar, Nace. And the article was published in European Journal of Medicinal Chemistry in 2019. Application of 109384-19-2 The author mentioned the following in the article:

ATP competitive inhibitors of DNA gyrase and topoisomerase IV have great therapeutic potential, but none of the described synthetic compounds has so far reached the market. To optimize the activities and physicochem. properties of the authors’ previously reported N-phenylpyrrolamide inhibitors, the authors have synthesized an improved, chem. variegated selection of compounds and evaluated them against DNA gyrase and topoisomerase IV enzymes, and against selected Gram-pos. and Gram-neg. bacteria. The most potent compound displayed IC50 values of 6.9 nM against Escherichia coli DNA gyrase and 960 nM against Staphylococcus aureus topoisomerase IV. Several compounds displayed min. inhibitory concentrations (MICs) against Gram-pos. strains in the 1-50 μM range, one of which inhibited the growth of Enterococcus faecalis, Enterococcus faecium, S. aureus and Streptococcus pyogenes with MIC values of 1.56 μM, 1.56 μM, 0.78 μM and 0.72 μM, resp. This compound has been investigated further on methicillin-resistant S. aureus (MRSA) and on ciprofloxacin non-susceptible and extremely drug resistant strain of S. aureus (MRSA VISA). It exhibited the MIC value of 2.5 μM on both strains, and MIC value of 32 μM against MRSA in the presence of inactivated human blood serum. Further studies are needed to confirm its mode of action. The results came from multiple reactions, including the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Application of 109384-19-2)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Application of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Chaturvedula, Prasad V.; Pin, Sokhom; Tholady, George; Conway, Charlie M.; Macor, John E.; Dubowchik, Gene M. published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Design and synthesis of potent antagonists containing rigid spirocyclic privileged structures for the CGRP receptor》.Related Products of 136624-42-5 The author mentioned the following in the article:

We report the synthesis of rigid spirocyclic systems as conformationally constrained variants of the Ala-Phe-NH2 dipeptide amide C-terminus of the calcitonin gene-related peptide (CGRP). CGRP receptor antagonists containing these moieties displayed potent affinity, functional antagonism and excellent oxidative stability. Structure-activity relationship studies demonstrated the relative importance of hydrogen bond donor/acceptor functionalities and the preferred orientation of an aromatic ring. Antagonists showed potent and full reversal of CGRP-induced dilation of ex vivo human intracranial arteries.4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5Related Products of 136624-42-5) was used in this study.

4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Related Products of 136624-42-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Application of 109384-19-2In 2021 ,《Development of autotaxin inhibitors: A series of tetrazole cinnamides》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Thomson, Christopher G.; Le Grand, Darren; Dowling, Mark; Beattie, David; Elphick, Lucy; Faller, Michael; Freeman, Mark; Hardaker, Elizabeth; Head, Victoria; Hemmig, Rene; Hill, Johan; Lister, Andrew; Pascoe, David; Rieffel, Sebastien; Shrestha, Binesh; Steward, Oliver; Zink, Florence. The article contains the following contents:

A series of inhibitors of autotaxin (ATX) have been developed from a high throughput screening hit, 1a (I), which shows an alternative binding mode to known catalytic site inhibitors. Selectivity over the hERG channel and microsomal clearance were dependent on the lipophilicity of the compounds, and this was optimized by reduction of clogD while maintaining high affinity ATX inhibition. Compound 15a (II) shows good oral exposure, and concentration dependent inhibition of formation of LPA in vivo, as shown in pharmacokinetic-pharmacodynamic (PK/PD) experimentstert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Application of 109384-19-2) was used in this study.

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Application of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The author of 《Photoredox-catalyzed synthesis of sulfones through deaminative insertion of sulfur dioxide》 were Wang, Xuefeng; Kuang, Yunyan; Ye, Shengqing; Wu, Jie. And the article was published in Chemical Communications (Cambridge, United Kingdom) in 2019. Reference of tert-Butyl 4-aminopiperidine-1-carboxylate The author mentioned the following in the article:

Katritzky salts were used as the alkyl radical precursors with the insertion of sulfur dioxide under photoredox catalysis. This transformation first enables direct generation of various alkylsulfonyl radicals by photoinduced single electron reduction, leading to diverse dialkyl sulfones in good to excellent yields. A radical pathway was proposed under visible-light induced conditions with the insertion of sulfur dioxide. In the experiment, the researchers used tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Reference of tert-Butyl 4-aminopiperidine-1-carboxylate)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Reference of tert-Butyl 4-aminopiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Related Products of 109384-19-2In 2021 ,《Polyplex-Loaded Hydrogels for Local Gene Delivery to Human Dermal Fibroblasts》 appeared in ACS Biomaterials Science & Engineering. The author of the article were Duran-Mota, Jose Antonio; Yani, Julia Quintanas; Almquist, Benjamin D.; Borros, Salvador; Oliva, Nuria. The article conveys some information:

Impaired cutaneous healing leading to chronic wounds affects between 2 and 6% of the total population in most developed countries and it places a substantial burden on healthcare budgets. Current treatments involving antibiotic dressings and mech. debridement are often not effective, causing severe pain, emotional distress, and social isolation in patients for years or even decades, ultimately resulting in limb amputation. Alternatively, gene therapy (such as mRNA therapies) has emerged as a viable option to promote wound healing through modulation of gene expression. However, protecting the genetic cargo from degradation and efficient transfection into primary cells remain significant challenges in the push to clin. translation. Another limiting aspect of current therapies is the lack of sustained release of drugs to match the therapeutic window. Herein, we have developed an injectable, biodegradable and cytocompatible hydrogel-based wound dressing that delivers poly(β-amino ester)s (pBAEs) nanoparticles in a sustained manner over a range of therapeutic windows. We also demonstrate that pBAE nanoparticles, successfully used in previous in vivo studies, protect the mRNA load and efficiently transfect human dermal fibroblasts upon sustained release from the hydrogel wound dressing. This prototype wound dressing technol. can enable the development of novel gene therapies for the treatment of chronic wounds. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Related Products of 109384-19-2)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Related Products of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Amides of pyrrole- and thiophene-fused anthraquinone derivatives: a role of the heterocyclic core in antitumor properties》 was written by Tikhomirov, Alexander S.; Litvinova, Valeria A.; Andreeva, Daria V.; Tsvetkov, Vladimir B.; Dezhenkova, Lyubov G.; Volodina, Yulia L.; Kaluzhny, Dmitry N.; Treshalin, Ivan D.; Schols, Dominique; Ramonova, Alla A.; Moisenovich, Mikhail M.; Shtil, Alexander A.; Shchekotikhin, Andrey E.. Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:

A new series of naphtho[2,3-f]indole-3-carboxamides I [R1 = Me; R2 = (3S)-3-aminopyrrolidin-1-yl, ((3S)-pyrrolidin-3-yl)amino, 4-amino-1-piperidyl, etc.; X = NH, NMe, NBn, etc.;] and anthra[2,3-b]thiophene-3-carboxamides I [R1 = H, X = S] was synthesized via coupling the resp. acids with cyclic diamines and dissected the role of the heterocyclic core in antitumor properties. New compounds demonstrated a submicromolar antiproliferative potency close to doxorubicin (Dox) against five tumor cell lines of various tissue origin. In contrast to Dox, the new compounds were similarly cytotoxic for HCT116 colon carcinoma cells (wild type p53) and their isogenic p53 knockout counterparts. Compound I [R1 = Me; R2 = (3S)-3-aminopyrrolidin-1-yl; X = NH] formed more affine complexes with DNA duplex than furan and thiophene analogs, a property that could be translated into a stronger inhibition of topoisomerase 1 mediated DNA unwinding. At tolerable doses the water soluble derivative I [R1 = Me; R2 = (3S)-3-aminopyrrolidin-1-yl; X = NH] significantly inhibited tumor growth (up to 79%) and increased the lifespan (153%) of mice bearing P388 lymphoma transplants. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. In organic chemistry, amines are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (NH3), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines).Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Turk, Benjamin E.; Jiang, Hongsi; Liu, Jun O. published an article in Proceedings of the National Academy of Sciences of the United States of America. The title of the article was 《Binding of thalidomide to α1-acid glycoprotein may be involved in its inhibition of tumor necrosis factor α production》.Recommanded Product: Benzyl (2,6-dioxopiperidin-3-yl)carbamate The author mentioned the following in the article:

In addition to its well known sedative and teratogenic effects, thalidomide also possesses potent immunomodulatory and antiinflammatory activities, being most effective against leprosy and chronic graft-vs.-host disease. The immunomodulatory activity of thalidomide has been ascribed to the selective inhibition of tumor necrosis factor α from monocytes. The mol. mechanism for the immunomodulatory effect of thalidomide remains unknown. To elucidate this mechanism, we synthesized an active photoaffinity label of thalidomide as a probe to identify the mol. target of the drug. Using the probe, we specifically labeled a pair of proteins of 43-45 kDa with high acidity from bovine thymus extract Purification of these proteins and partial peptide sequence determination revealed them to be α1-acid glycoprotein (AGP). We show that the binding of thalidomide photoaffinity label to authentic human AGP is competed with both thalidomide and the nonradioactive photoaffinity label at concentrations comparable to those required for inhibition of production of tumor necrosis factor α from human monocytes, suggesting that AGP may be involved in the immunomodulatory activity of thalidomide. The experimental process involved the reaction of Benzyl (2,6-dioxopiperidin-3-yl)carbamate(cas: 24666-55-5Recommanded Product: Benzyl (2,6-dioxopiperidin-3-yl)carbamate)

Benzyl (2,6-dioxopiperidin-3-yl)carbamate(cas: 24666-55-5) belongs to anime. Left-handed and right-handed forms (mirror-image configurations, known as optical isomers or enantiomers) are possible when all the substituents on the central nitrogen atom are different (i.e., the nitrogen is chiral). With amines, there is extremely rapid inversion in which the two configurations are interconverted.Recommanded Product: Benzyl (2,6-dioxopiperidin-3-yl)carbamate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem