Huber, Vincent J.’s team published research in Bioorganic & Medicinal Chemistry in 17 | CAS: 51987-99-6

Bioorganic & Medicinal Chemistry published new progress about 51987-99-6. 51987-99-6 belongs to amides-buliding-blocks, auxiliary class Pyridine,Thiadiazole,Amine,Amide,Inhibitor, name is N-(1,3,4-Thiadiazol-2-yl)nicotinamide, and the molecular formula is C8H6N4OS, Formula: C8H6N4OS.

Huber, Vincent J. published the artcileIdentification of Aquaporin 4 inhibitors using in vitro and in silico methods, Formula: C8H6N4OS, the publication is Bioorganic & Medicinal Chemistry (2009), 17(1), 411-417, database is CAplus and MEDLINE.

The in vitro inhibitory effects and in silico docking energies of 18 compounds with respect to Aquaporin 4 (AQP4) were investigated. More than half of the compounds tested showed inhibitory activity in the in vitro functional assay and included the 5-HT1B/1D agonists sumatriptan, and rizatriptan. Moreover, the observed inhibitory activity of the compounds used in this study at 20 μM showed a strong correlation with their in silico docking energies, r 2 = 0.64, which was consistent with that found in previous studies. The AQP4 inhibitory IC50 values of three compounds, 2-(nicotinamido)-1,3,4-thiadiazole, sumatriptan and rizatriptan, were subsequently found to be 3, 11, and 2 μM, resp.

Bioorganic & Medicinal Chemistry published new progress about 51987-99-6. 51987-99-6 belongs to amides-buliding-blocks, auxiliary class Pyridine,Thiadiazole,Amine,Amide,Inhibitor, name is N-(1,3,4-Thiadiazol-2-yl)nicotinamide, and the molecular formula is C8H6N4OS, Formula: C8H6N4OS.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Anabuki, Tomoaki’s team published research in Bioorganic & Medicinal Chemistry Letters in 28 | CAS: 2418-95-3

Bioorganic & Medicinal Chemistry Letters published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, SDS of cas: 2418-95-3.

Anabuki, Tomoaki published the artcileNovel biotin linker with alkyne and amino groups for chemical labelling of a target protein of a bioactive small molecule, SDS of cas: 2418-95-3, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(4), 783-786, database is CAplus and MEDLINE.

We synthesized a novel linker (I) with biotin, alkyne and amino groups for the identification of target proteins using a small mol. that contains an azide group (azide probe). The alkyne in the linker bound the azide probe via an azide-alkyne Huisgen cycloaddition A protein cross-linker effectively bound the conjugate of the linker and an azide probe with a target protein. The covalently bound complex was detected by western blotting. Linker I was applied to a model system using an abscisic acid receptor, RCAR/PYR/PYL (PYL). Cross-linked complexes of linker I, the azide probes and the target proteins were successfully visualized by western blotting. This method of target protein identification was more effective than a previously developed method that uses a second linker with biotin, alkyne, and benzophenone (linker II) that acts to photo-crosslink target proteins. The system developed in this study is a method for identifying the target proteins of small bioactive mols. and is different from photo-affinity labeling.

Bioorganic & Medicinal Chemistry Letters published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, SDS of cas: 2418-95-3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Khairullina, V. R.’s team published research in Pharmaceutical Chemistry Journal in 48 | CAS: 321673-30-7

Pharmaceutical Chemistry Journal published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Application of [(2-Hexylcyclopentylidene)amino]thiourea.

Khairullina, V. R. published the artcileStructural Analysis of Leukotriene B4 (LBT4) Receptor (BLT1 AND BLT2) Antagonists, Application of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Pharmaceutical Chemistry Journal (2014), 48(5), 317-322, database is CAplus.

The structural characteristics typical of highly and moderately effective antagonists of BLT1 and BLT2 receptors were identified and the extents of their influences on the target property were evaluated. Two models for predicting inhibitory activity were constructed for series of sulfur-, nitrogen- and oxygen-containing heterocyclic compounds with significant prognostic levels of greater than 80% using two methods based on sample recognition theory. These structural patterns can be used for virtual screening of potential drugs for antiallergic activity associated with blockade of leukotriene LTB4-sensitive BLT1 and BLT2 receptors.

Pharmaceutical Chemistry Journal published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Application of [(2-Hexylcyclopentylidene)amino]thiourea.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Nakanishi, Yoshimitsu’s team published research in Science Signaling in 11 | CAS: 321673-30-7

Science Signaling published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Formula: C12H23N3S.

Nakanishi, Yoshimitsu published the artcileStepwise phosphorylation of leukotriene B4 receptor 1 defines cellular responses to leukotriene B4, Formula: C12H23N3S, the publication is Science Signaling (2018), 11(544), eaao5390/1-eaao5390/15, database is CAplus and MEDLINE.

Leukotriene B4 (LTB4) receptor type 1 (BLT1) is abundant in phagocytic and immune cells and plays crucial roles in various inflammatory diseases. BLT1 is phosphorylated at several serine and threonine residues upon stimulation with the inflammatory lipid LTB4. Using Phos-tag gel electrophoresis to sep. differentially phosphorylated forms of BLT1, we identified two distinct types of phosphorylation, basal and ligand-induced, in the carboxyl terminus of human BLT1. In the absence of LTB4, the basal phosphorylation sites were modified to various degrees, giving rise to many different phosphorylated forms of BLT1. Different concentrations of LTB4 induced distinct phosphorylation events, and these ligand-induced modifications facilitated addnl. phosphorylation events at the basal phosphorylation sites. Because neutrophils migrate toward inflammatory sites along a gradient of LTB4, the degree of BLT1 phosphorylation likely increases in parallel with the increase in LTB4 concentration as the cells migrate. At high concentrations of LTB4, deficiencies in these two types of phosphorylation events impaired chemotaxis and β-hexosaminidase release, a proxy for degranulation, in Chinese hamster ovary (CHO-K1) and rat basophilic leukemia (RBL-2H3) cells, resp. These results suggest that an LTB4 gradient around inflammatory sites enhances BLT1 phosphorylation in a stepwise manner to facilitate the precise migration of phagocytic and immune cells and the initiation of local responses, including degranulation.

Science Signaling published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Formula: C12H23N3S.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Soley, Jacob’s team published research in Journal of Organic Chemistry in 85 | CAS: 2418-95-3

Journal of Organic Chemistry published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C38H74Cl2N2O4, Formula: C11H22N2O4.

Soley, Jacob published the artcileMild, Rapid, and Chemoselective Procedure for the Introduction of the 9-Phenyl-9-fluorenyl Protecting Group into Amines, Acids, Alcohols, Sulfonamides, Amides, and Thiols, Formula: C11H22N2O4, the publication is Journal of Organic Chemistry (2020), 85(4), 2068-2081, database is CAplus and MEDLINE.

The 9-phenyl-9-fluorenyl (PhF) group has been used as an Nα protecting group of amino acids and their derivatives mainly as a result of its ability to prevent racemization. However, installing this group using the standard protocol, which employs 9-bromo-9-phenylfluorene/K3PO4/Pb(NO3)2, often takes days and yields can be variable. Here, we demonstrate that the PhF group can be introduced into the amino group of Weinreb’s amides and Me esters of amino acids, as well as into alcs. and carboxylic acids, rapidly and in excellent yields, using 9-chloro-9-phenylfluorene (PhFCl)/N-methylmorpholine (NMM)/AgNO3. Nα-PhF-protected amino acids can be prepared from unprotected α-amino acids, rapidly and often in near quant. yields, by treatment with N,O-bis(trimethylsilyl)acetamide (BSA) and then PhFCl/NMM/AgNO3. Primary alcs. can be protected with the PhF group in the presence of secondary alcs. in moderate yield. Using PhFCl/AgNO3, a primary alc. can be protected in good yield in the presence of a primary ammonium salt or a carboxylic acid. Primary sulfonamides and amides can be protected in moderate to good yields using phenylfluorenyl alc. (PhFOH)/BF3·OEt2/K3PO4, while thiols can be protected in good to excellent yield using PhFOH/BF3·OEt2 even in the presence of a carboxylic acid or primary ammonium group.

Journal of Organic Chemistry published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C38H74Cl2N2O4, Formula: C11H22N2O4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Kanemoto, Kazuya’s team published research in Chemical Communications (Cambridge, United Kingdom) in 53 | CAS: 146140-95-6

Chemical Communications (Cambridge, United Kingdom) published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, Computed Properties of 146140-95-6.

Kanemoto, Kazuya published the artcileRhodium-catalyzed odorless synthesis of diaryl sulfides from borylarenes and S-aryl thiosulfonates, Computed Properties of 146140-95-6, the publication is Chemical Communications (Cambridge, United Kingdom) (2017), 53(77), 10640-10643, database is CAplus and MEDLINE.

Diaryl sulfides such as I [R1 = 4-BrC6H4, 4-Me2NC6H4, 3-thienyl, etc.; R2 = 4-MeC6H4, 2-FC6H4, 3-HOC6H4] were efficiently prepared by rhodium-catalyzed odorless deborylative arylthiolation of organoborons with S-aryl thiosulfonates. The ready availability of starting materials and further transformation of sulfides was rendered a diverse range of organosulfur compounds easily accessible.

Chemical Communications (Cambridge, United Kingdom) published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, Computed Properties of 146140-95-6.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Wu, Chaoneng’s team published research in Medical Hypotheses in 71 | CAS: 321673-30-7

Medical Hypotheses published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C14H12N2S, Quality Control of 321673-30-7.

Wu, Chaoneng published the artcile“Pro-resolution” and anti-inflammation, a role of RvE1 in anti-atherosclerosis and plaque stabilization, Quality Control of 321673-30-7, the publication is Medical Hypotheses (2008), 71(2), 252-255, database is CAplus and MEDLINE.

A review. Summary: Inflammation governs atherosclerosis and is firmly regulated. Endogenous mechanisms to keep inflammation self-limiting are unclear. In the present article, we propose that RvE1 (resolution E1), an endogenous lipid mediator, inhibits inflammation through “pro-resolution” and counter-modulating immunity in atherosclerosis. The background comes from studies on the potent programming of resolution and immuno-inflammation of RvE1 and its precursor, eicosapentaenoic acid, in treating chronic inflammatory disease with unknown mechanisms. In light of the interaction between RvE1 and leukotrieneB4 (LTB4) and their potential impaired immunity regulation hematostasis, we hypothesize that RvE1 play an anti-atherosclerosis and plaque stabilization role through “pro-resolution” and anti-inflammation which may be realized by blocking LTB4/BLT1 (receptor of LTB4) pathway. Our hypothesis generates potentially clin. viewpoint to systematically look for pro- and anti-inflammation and “pro-resolution” process in atherosclerosis. Furthermore, we suggest that RvE1 might be particularly indicated for the treatment of atherosclerotic diseases and plaque stabilization which might ensure an effective management for patients with coronary artery disease.

Medical Hypotheses published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C14H12N2S, Quality Control of 321673-30-7.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Sato, Yuki’s team published research in Journal of Pharmacy & Pharmaceutical Sciences in 15 | CAS: 321673-30-7

Journal of Pharmacy & Pharmaceutical Sciences published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Quality Control of 321673-30-7.

Sato, Yuki published the artcileInvolvement of cholesterol membrane transporter Niemann-Pick C1-like 1 in the intestinal absorption of lutein, Quality Control of 321673-30-7, the publication is Journal of Pharmacy & Pharmaceutical Sciences (2012), 15(2), 256-264, database is CAplus and MEDLINE.

Purpose: Lutein is a carotenoid mainly found in green leafy vegetables and is located in the macula lutea in the human eye. Since humans cannot synthesize lutein de novo, it must be digested as food. The physiol. importance of an orally administered compound depends on its interaction with target tissues. It is therefore important to clarify the absorption mechanism in the intestine. Cholesterol membrane transporters Niemann-Pick C1 Like 1 (NPC1L1) and scavenger receptor class B type 1 (SR-B1) are involved in the intestinal absorption of highly lipophilic compounds including cholesterol. Ezetimibe, a selective inhibitor of intestinal NPC1L1, is the widespread lipid-lowering agent. It is important to investigate the possibility of food-drug interactions in order to prevent undesirable and harmful clin. consequences. The aim of this work was to determine whether NPC1L1, SR-B1 and other transporters are involved in absorption of lutein. Methods: Caco-2 cells were used for accumulation and permeability study of lutein. Lutein concentration was determined by an HPLC system. The cDNA of transporters was isolated from total RNA of Caco-2 cells and the expression of these transporters was confirmed by RT-PCR (reverse transcription – polymerase chain reaction). Results: Ezetimibe inhibited up to 40% of lutein accumulation by Caco-2 cell monolayers. Block lipid transport 1 (BLT-1), a selective chem. inhibitor of SR-B1, also inhibited lutein accumulation by Caco-2 cells. On the other hand, ATP-depletion reagents (sodium fluoride and sodium azide or carbonyl cyanide m-chlorophenylhydrazone) did not influence the accumulation or permeation of lutein significantly. Conclusions: The results show that lutein absorption is, at least in part, mediated by influx transporters NPC1L1 and SR-B1 rather than mediated by efflux transporters such as ABC (ATP-binding cassette) transporters.

Journal of Pharmacy & Pharmaceutical Sciences published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Quality Control of 321673-30-7.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Rydfjord, Jonas’s team published research in Chemistry – A European Journal in 19 | CAS: 2451-91-4

Chemistry – A European Journal published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C15H14N2, Recommanded Product: N,N-Dibenzylcyanamide.

Rydfjord, Jonas published the artcileDecarboxylative Palladium(II)-Catalyzed Synthesis of Aryl Amidines from Aryl Carboxylic Acids: Development and Mechanistic Investigation, Recommanded Product: N,N-Dibenzylcyanamide, the publication is Chemistry – A European Journal (2013), 19(41), 13803-13810, database is CAplus and MEDLINE.

A fast and convenient synthesis of aryl amidines starting from carboxylic acids and cyanamides is reported. The reaction was achieved by palladium(II) catalysis in a one-step microwave protocol using [Pd(O2CCF3)2], 6-methyl-2,2′-bipyridyl, and trifluoroacetic acid (TFA) in N-methylpyrrolidinone (NMP), providing the corresponding aryl amidines in moderate to excellent yields. E.g., in this system, reaction of 2,4,6-trimethoxybenzoic acid and N-cyanopiperidine gave 96% amidine I. The protocol is very robust with regards to the cyanamide coupling partner but requires electron-rich ortho-substituted aryl carboxylic acids. Mechanistic insight was provided by a DFT investigation and direct ESI-MS studies of the reaction. The results of the DFT study correlated well with the exptl. findings and, together with the ESI-MS study, support the suggested mechanism. Furthermore, a scale-out (scale-up) was performed with a non-resonant microwave continuous-flow system, achieving a maximum throughput of 11 mmol h-1 by using a glass reactor with an inner diameter of 3 mm at a flow rate of 1 mL min-1.

Chemistry – A European Journal published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C15H14N2, Recommanded Product: N,N-Dibenzylcyanamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Timari, Geza’s team published research in Synlett in | CAS: 146140-95-6

Synlett published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C7H8BBrO2, HPLC of Formula: 146140-95-6.

Timari, Geza published the artcileA convenient synthesis of two new indoloquinoline alkaloids, HPLC of Formula: 146140-95-6, the publication is Synlett (1997), 1067-1068, database is CAplus.

A concise synthesis of cryptosanguinolentine and cryptotackieine (neocryptolepine), isolated from Cryptolepis sanguinolenta is reported. The Pd-catalyzed cross-coupling reaction of 3-bromoquinoline or 3-bromo-N-methyl-2-quinolinone with 2-(pivaloylamino)phenylboronate gave the corresponding biaryls from which the indoloquinolines could be synthesized.

Synlett published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C7H8BBrO2, HPLC of Formula: 146140-95-6.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics