Tag: M.W=200-250

Wu, Yong-qian published the artcile1-Cyanoimidazole as a Mild and Efficient Electrophilic Cyanating Agent, Formula: C15H14N2, the publication is Organic Letters (2000), 2(6), 795-797, database is CAplus and MEDLINE.

A mild and high-yielding cyanating reaction of amine, sulfur, and carbanion nucleophiles, e.g., PhNH₂, (PhCH₂)₂NH, PhCCH, PhCH₂SH, is reported which uses 1-cyanoimidazole as an electrophilic cyanating agent to give the corresponding cyanated products, e.g., PhNHCN, (PhCH₂)₂NCN, PhCCCN, PhCH₂SCN.

Organic Letters 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 C5H5BO5, Formula: C15H14N2.

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

Ayres, James N. published the artcileN-Cyanation of Secondary Amines Using Trichloroacetonitrile, Category: amides-buliding-blocks, the publication is Organic Letters (2016), 18(21), 5528-5531, database is CAplus and MEDLINE.

A one-pot N-cyanation of secondary amines has been developed using trichloroacetonitrile as an inexpensive cyano source. A diverse range of cyclic and acyclic secondary amines can be readily transformed into the corresponding cyanamides in good isolated yields, with the method successfully utilized in the final synthetic step of a biol. active rolipram-derived cyanamide. This approach exhibits distinct selectivity when compared to the use of highly toxic cyanogen bromide.

Organic Letters 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, Category: amides-buliding-blocks.

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

Peterson, Randall T. published the artcileSmall molecule developmental screens reveal the logic and timing of vertebrate development, HPLC of Formula: 321673-30-7, the publication is Proceedings of the National Academy of Sciences of the United States of America (2000), 97(24), 12965-12969, database is CAplus and MEDLINE.

Much has been learned about vertebrate development by random mutagenesis followed by phenotypic screening and by targeted gene disruption followed by phenotypic anal. in model organisms. Because the timing of many developmental events is critical, it would be useful to have temporal control over modulation of gene function, a luxury frequently not possible with genetic mutants. Here, the authors used synthetic small mols. from the DiverSet E obtained from Chembridge Corp., to demonstrate that small mols. capable of conditional gene product modulation can be identified through developmental screens in zebrafish. The authors have identified several small mols. that specifically modulate various aspects of vertebrate ontogeny, including development of the central nervous system, the cardiovascular system, the neural crest, and the ear. Several of the small mols. identified allowed the authors to dissect the logic of melanocyte and otolith development and to identify critical periods for these events. Small mols. identified in this way offer potential to dissect further these and other developmental processes and to identify novel genes involved in vertebrate development.

Proceedings of the National Academy of Sciences of the United States of America 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, HPLC of Formula: 321673-30-7.

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

Serezani, Carlos H. published the artcileLeukotriene B₄ amplifies NF-κB activation in mouse macrophages by reducing SOCS1 inhibition of MyD88 expression, COA of Formula: C12H23N3S, the publication is Journal of Clinical Investigation (2011), 121(2), 671-682, database is CAplus and MEDLINE.

Activation of NF-κB and 5-lipoxygenase-mediated (5-LO-mediated) biosynthesis of the lipid mediator leukotriene B₄ (LTB₄) are pivotal components of host defense and inflammatory responses. However, the role of LTB₄ in mediating innate immune responses elicited by specific TLR ligands and cytokines is unknown. Here we have shown that responses dependent on MyD88 (an adaptor protein that mediates signaling through all of the known TLRs, except TLR3, as well as IL-1β and IL-18) are reduced in mice lacking either 5-LO or the LTB₄ receptor BTL1, and that macrophages from these mice are impaired in MyD88-dependent activation of NF-κB. This macrophage defect was associated with lower basal and inducible expression of MyD88 and reflected impaired activation of STAT1 and overexpression of the STAT1 inhibitor SOCS1. Expression of MyD88 and responsiveness to the TLR4 ligand LPS were decreased by Stat1 siRNA silencing in WT macrophages and restored by Socs1 siRNA in 5-LO-deficient macrophages. These results uncover a pivotal role in macrophages for the GPCR BLT1 in regulating activation of NF-κB through Stat1-dependent expression of MyD88.

Journal of Clinical Investigation 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 C26H31N3O3, COA of Formula: C12H23N3S.

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

Han, Boyang published the artcileConstruction of cyclophane-braced peptide macrocycles via palladium-catalyzed picolinamide-directed intramolecular C(sp²)-H arylation, Category: amides-buliding-blocks, the publication is Organic Letters (2020), 22(17), 6879-6883, database is CAplus and MEDLINE.

A versatile method for the construction of C(sp²)-linked cyclophane peptide macrocycles via Pd-catalyzed picolinamide-directed intramol. arylation of aryl and alkenyl C-H bonds of amino acid side chains with aryl iodides is developed. This method provides simple and efficient access to a variety of cyclophane-braced structures from readily accessible linear peptide precursors.

Organic 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, Category: amides-buliding-blocks.

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

Yuan, Zhefan published the artcileZwitterionic Peptide Cloak Mimics Protein Surfaces for Protein Protection, Application of H-Lys(Boc)-OH, the publication is Angewandte Chemie, International Edition (2020), 59(50), 22378-22381, database is CAplus and MEDLINE.

Inspired by the amino acid composition of natural protein surfaces, we developed a zwitterionic cloak containing multi-layers of short alternating glutamic acid and lysine (EK) peptides as a facile, highly effective and low-immunogenicity approach for the protection and delivery of biotherapeutics. Each EK layer grafted to proteins provides multiple times of new lysine reaction sites for the growth of subsequent EK layers. This unique design allows EK peptides to achieve high coating d. on proteins, overcoming the limitation of traditional conjugation strategies that rely on the number of innate lysine groups. A triple-layer EK cloak manifests to successfully eliminate the specific and non-specific interactions of protected asparaginase with biol. media while prolong the drug circulation time and significantly mitigate its immunogenicity in vivo, suggesting an EK peptide cloak as a promising approach to improve the safety and efficacy of biotherapeutics.

Angewandte Chemie, International Edition 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 Al2H32O28S3, Application of H-Lys(Boc)-OH.

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

Shi, Xiaoyu published the artcileLabel-retention expansion microscopy, Recommanded Product: H-Lys(Boc)-OH, the publication is Journal of Cell Biology (2021), 220(9), e202105067, database is CAplus and MEDLINE.

Expansion microscopy (ExM) increases the effective resolving power of any microscope by expanding the sample with swellable hydrogel. Since its invention, ExM has been successfully applied to a wide range of cell, tissue, and animal samples. Still, fluorescence signal loss during polymerization and digestion limits mol.-scale imaging using ExM. Here, we report the development of label-retention ExM (LR-ExM) with a set of trifunctional anchors that not only prevent signal loss but also enable high-efficiency labeling using SNAP and CLIP tags. We have demonstrated multicolor LR-ExM for a variety of subcellular structures. Combining LR-ExM with superresoln. stochastic optical reconstruction microscopy (STORM), we have achieved mol. resolution in the visualization of polyhedral lattice of clathrin-coated pits in situ.

Journal of Cell Biology 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 C37H30ClIrOP2, Recommanded Product: H-Lys(Boc)-OH.

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

Wang, Xiaoran published the artcileAquaporin 4 differentially modulates osmotic effects on vasopressin neurons in rat supraoptic nucleus, Name: N-(1,3,4-Thiadiazol-2-yl)nicotinamide, the publication is Acta Physiologica (2021), 232(3), e13672, database is CAplus and MEDLINE.

Aim : Glial fibrillary acidic protein (GFAP) molecularly associates with aquaporin 4 (AQP4) in astrocytic plasticity. Here, we further examined how AQP4 modulates osmotic effects on vasopressin (VP) neurons in rat supraoptic nucleus (SON) through interactions with GFAP in astrocytes. Methods : Brain slices from adult male rats were kept under osmotic stimulation. Western blot, co-immunoprecipitation, immunohistochem. and patch-clamp recordings were used for anal. of expressions and interactions between GFAP and AQP4, astrocyte-specific proteins in the SON, as well as their influence on VP neuronal activity. Data were analyzed using SPSS software. Results : Hyposmotic challenge (HOC) of acute SON slices caused an early (within 5 min) and transient increase in the colocalization of AQP4 with GFAP filaments. This effect was prominent at astrocytic processes surrounding VP neuron somata and was accompanied by inhibition of VP neuronal activity. Similar HOC effect was seen in the SON isolated from rats subjected to in vivo HOC, wherein a transiently increased mol. association between GFAP and AQP4 was detected using co-immunoprecipitation The late stage rebound excitation (10 min) of VP neurons in brain slices subjected to HOC and the associated astrocytic GFAP’s ‘return to normal’ were both hampered by 2-(nicotinamide)-1,3,4-thiadiazole, a specific AQP4 channel blocker that itself did not influence VP neuronal activity. Moreover, this agent prevented hyperosmotic stress-evoked excitation of VP neurons and associated reduction in GFAP filaments. Conclusion : These findings indicate that osmotically driven increase in VP neuronal activity requires the activation of AQP4, which determines a retraction of GFAP filaments.

Acta Physiologica 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 C5H7F3O3, Name: N-(1,3,4-Thiadiazol-2-yl)nicotinamide.

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

Schindler, Norbert published the artcileReactions with dialkylcyanamides. Reaction of dialkylcyanamides with sulfur or phosphorus halides. Synthesis of substituted chloroformamidines, Application of N,N-Dibenzylcyanamide, the publication is Chemische Berichte (1973), 106(1), 56-61, database is CAplus.

Reaction of R2NCN (R = Et, PhCH2, cyclohexyl; R2N = piperidino) with SCl2 (or SOCl2), SO2Cl2, and P(X)Cl3 (X = O or S) yielded ≤90% (R2NCCl:N)2S+Cl Cl-, ≤100% R2NCCl:NSO2Cl, and ≤87% R2NCCl:NP(X)Cl2, resp. The compounds obtained were characterized by the ir spectra.

Chemische Berichte 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, Application of N,N-Dibenzylcyanamide.

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

Soni, Navneet Omprakash published the artcileTargeting LTB4 -BLT1 – in diabetic nephropathy?, Category: amides-buliding-blocks, the publication is World Journal of Pharmacy and Pharmaceutical Sciences (2017), 6(9), 312-315, database is CAplus.

A review. Lipid mediators play important role in renal injury many of lipid mediators are expressed and up regulated in response to toxins, drugs and in metabolic disorder. Lipid mediators also play role in vascular complication. So new intervention target can be thought by targeting the mediators Diabetic complication can be reduced unfortunately very few study are available to test the hypothesis and come to conclusion. But from all available study reports one can say targeting lipid mediators have future scope as well as limitation.

World Journal of Pharmacy and 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 C14H14, Category: amides-buliding-blocks.

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