Tag: M.W=200-250

Schroth, W. published the artcileThe dehydration of ureas by two-phase dichlorocarbene reaction, a synthetic access to substituted cyanamides, Category: amides-buliding-blocks, the publication is Journal fuer Praktische Chemie (Leipzig) (1983), 325(5), 787-802, database is CAplus.

A wide variety of N,N-disubstituted ureas were dehydrated in the CHCl₃/NaOH catalytic 2-phase system under mild conditions. The sequence of urea transamidation and dehydration offers a profitable approach to aprotic cyanamides. Among various phase-transfer catalysts tertiary amines prove to be the most efficient. Tertiary amines may also be used in the transformation of carboxamides and thioamides to the corresponding nitriles. The application of the same technique is less suitable in the case of N-monosubstituted ureas, N,N‘-disubstituted ureas, and N-(dialkylaminomethylene)ureas, since subsequent reactions of the cyanamides predominate. The dehydration mechanism is elucidated in terms of HOMO-perturbation theory.

Journal fuer Praktische Chemie (Leipzig) 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

Schroth, Werner published the artcileDehydration of ureas with dichlorocarbene in the phase transfer method, Computed Properties of 2451-91-4, the publication is Zeitschrift fuer Chemie (1981), 21(1), 25-7, database is CAplus.

Mono- and disubstituted ureas RR¹NCONH₂ [R = alkyl, R¹ = H, alkyl, or Ph; R = R¹ = PhCH₂; or RR¹ = (CH₂)₄, (CH₂)₅, oxydiethylene, or (phenylimino) diethylene] were dehydrated by treatment with :CCl₂ in the presence of a phase-transfer catalyst, (PhCH₂)Et₃NCl, to give 20-85% RR¹NCN. (CH₂)₄NCSNH₂ was obtained in 45% yield by the addition of H₂S to (CH₂)₄NCN in the presence of an equimolar amount of dry Et₃N.

Zeitschrift fuer Chemie 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, Computed Properties of 2451-91-4.

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

Paulsen, Marianne H. published the artcileAn amphipathic cyclic tetrapeptide scaffold containing halogenated β^2,2-amino acids with activity against multiresistant bacteria, Product Details of C11H22N2O4, the publication is Journal of Peptide Science (2018), 24(10), n/a, database is CAplus and MEDLINE.

The present study describes the synthesis and biol. studies of a small series of head-to-tail cyclic tetrapeptides of the general structure c(Lys-β^2,2-Xaa-Lys) containing one lipophilic β^2,2-amino acid and Lys, Gly, Ala, or Phe as the Xaa residue in the sequence. The peptides were investigated for antimicrobial activity against gram-pos. and gram-neg. reference strains and 30 multiresistant clin. isolates including strains with extended spectrum β-lactamase-carbapenemase (ESBL-CARBA) production Toxicity was determined against human red blood cells. The most potent peptides showed high activity against the gram-pos. clin. isolates with min. inhibitory concentrations of 4-8 μg/mL and low hemolytic activity. The combination of high antimicrobial activity and low toxicity shows that these cyclic tetrapeptides containing lipophilic β^2,2-amino acids form a valuable scaffold for designing novel antimicrobial agents.

Journal of Peptide Science 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, Product Details of C11H22N2O4.

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

Krajsovszky, Gabor published the artcileSuzuki-aza-Wittig, Suzuki-condensation and aza-Wittig-electrocyclic ring-closure tandem reactions for synthesis of fused nitrogen-containing ring systems, Recommanded Product: (2-Pivalamidophenyl)boronic acid, the publication is ARKIVOC (Gainesville, FL, United States) (2011), 229-253, database is CAplus.

Tandem combinations of Suzuki-aza-Wittig, Suzuki-condensation, and aza-Wittig-electrocyclic ring closure reactions for the synthesis of new pyridazino[4,5-c]isoquinolinone, pyridazino[4,5-c]quinolinone, and pyrimido[5,4-c]quinoline derivatives were described.

ARKIVOC (Gainesville, FL, United States) 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, Recommanded Product: (2-Pivalamidophenyl)boronic acid.

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

Beletskiy, Evgeny V. published the artcileSelective binding and extraction of aqueous dihydrogen phosphate solutions via three-armed thiourea receptors, Related Products of amides-buliding-blocks, the publication is Organic & Biomolecular Chemistry (2015), 13(38), 9844-9849, database is CAplus and MEDLINE.

A series of neutral anion receptors with one to three thiourea arms were synthesized and their binding to tetrabutylammonium chloride, acetate, and dihydrogen phosphate salts in aqueous DMSO mixtures was examined The three-armed thiourea host was found to strongly and selectively bind H₂PO₄^– even in DMSO solutions containing up to 30% water. This enabled the dihydrogen phosphate salt to be extracted from water into chloroform in its dibasic form despite the high heat of the hydration of HPO₄^2-.

Organic & Biomolecular Chemistry 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, Related Products of amides-buliding-blocks.

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

Verhoog, Stefan published the artcile¹⁸F-Trifluoromethylation of unmodified peptides with 5-¹⁸F-(trifluoromethyl)dibenzothiophenium trifluoromethanesulfonate, COA of Formula: C11H22N2O4, the publication is Journal of the American Chemical Society (2018), 140(5), 1572-1575, database is CAplus and MEDLINE.

The ¹⁸F-labeling of 5-(trifluoromethyl)-dibenzothiophenium trifluoromethanesulfonate, commonly referred to as the Umemoto reagent, has been accomplished applying a halogen exchange ¹⁸F-fluorination with ¹⁸F-fluoride, followed by oxidative cyclization with oxone and trifluoromethanesulfonic anhydride. This new ¹⁸F-reagent allows for the direct chemoselective ¹⁸F-labeling of unmodified peptides at the thiol cysteine residue.

Journal of the American Chemical Society 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 C17H18N3NaO3S, COA of Formula: C11H22N2O4.

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

Ren, Kun published the artcileQuercetin induces the selective uptake of HDL-cholesterol via promoting SR-BI expression and the activation of the PPARγ/LXRα pathway, SDS of cas: 321673-30-7, the publication is Food & Function (2018), 9(1), 624-635, database is CAplus and MEDLINE.

Reverse cholesterol transport (RCT) is the process to deliver cholesterol to the liver for further excretion and involves scavenger receptor class B type I (SR-BI)-mediated selective lipid uptake (SLU) from high-d. lipoprotein cholesterol (HDL-C). The up-regulation of hepatic SR-BI expression accelerates HDL-C clearance in circulation and impedes the development of atherosclerosis (AS). In the present study, we explored the modulation of hepatic SR-BI expression and SR-BI-mediated SLU by quercetin, a natural flavonoid compound in the diet with a favorable role in cardiovascular disorders. We found that quercetin significantly increased the expression level of SR-BI in HepG2 cells in a concentration- and time-dependent manner. Besides, quercetin had stimulatory effects on the binding of 1,1′-dioctadecyl-3,3,3′,3′-tetramethylindocarbocyanine perchlorate (Dil)-labeled HDL to hepatocytes and ¹²⁵I/³H-CE-HDL association Treatment with small interfering RNA (siRNA) or SR-BI specific inhibitor, BLT-1, inhibited quercetin-induced Dil-HDL binding and selective HDL-C uptake. Treatment with quercetin increased both proliferator-activated receptor γ (PPARγ) and liver X receptor α (LXRα) levels. Addnl., the quercetin-induced expression of SR-BI, Dil-HDL binding and the selective uptake of HDL-C were significantly attenuated by treatment with PPARγ siRNA, LXRα siRNA, and their antagonists, resp. In C57BL/6 mice, quercetin administration potently increased SR-BI, PPARγ and LXRα levels and lipid accumulation in the liver. Altogether, our results suggest that quercetin-induced up-regulation of SR-BI and subsequent lipid uptake in hepatocytes might contribute to its beneficial effects on cholesterol homeostasis and atherogenesis.

Food & Function 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, SDS of cas: 321673-30-7.

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

Burnett, Marianne E. published the artcileStructural characterization of the aquaporin inhibitor 2-nicotinamido-1,3,4-thiadiazole, Synthetic Route of 51987-99-6, the publication is Acta Crystallographica, Section C: Structural Chemistry (2015), 71(12), 1074-1079, database is CAplus and MEDLINE.

Nicotinamides are a class of compounds with a wide variety of applications, from use as antimicrobial agents to inhibitors of biol. processes. These compounds are also cofactors, which are necessary components of metabolic processes. Structural modification gives rise to the activities observed Similarly, 1,3,4-thiadiazoles have been shown to possess antioxidant, antimicrobial, or anti-inflammatory biol. activity. To take advantage of each of the inherent characteristics of the two aforementioned functional groups, 2-nicotinamido-1,3,4-thiadiazole, C₈H₆N₄OS, was synthesized. Since defining chem. connectivity is paramount in understanding biol. activity, in this report, the structural characterization of 2-nicotinamido-1,3,4-thiadiazole has been carried out using X-ray crystallog. methods. The NMR-derived assignments were made possible by utilizing one- (1D) and two-dimensional (2D) NMR techniques. In addition, UV-Visible and IR spectroscopies, and elemental anal. were used to fully characterize the product synthesized by the one-step reaction between nicotinoyl chloride hydrochloride and 2-amino-1,3,4-thiadiazole. Computational parameters related to blood-brain barrier permeability are also presented.

Acta Crystallographica, Section C: Structural 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, Synthetic Route of 51987-99-6.

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

Kaloudi, Aikaterini published the artcile[^99mTc]Tc-DGA1, a Promising CCK₂R-Antagonist-Based Tracer for Tumor Diagnosis with Single-Photon Emission Computed Tomography, Product Details of C11H22N2O4, the publication is Molecular Pharmaceutics (2020), 17(8), 3116-3128, database is CAplus and MEDLINE.

Radiolabeled gastrin analogs have been proposed for theranostics of cholecystokinin subtype 2 receptor (CCK₂R)-pos. cancer. Peptide radioligands based on other receptor antagonists have displayed superior pharmacokinetics and higher biosafety than agonists. Here, we present DGA1, a derivative of the nonpeptidic CCK₂R antagonist Z-360 carrying an acyclic tetraamine, for [^99mTc]Tc labeling. Preclin. comparison of [^99mTc]Tc-DGA1 with [^99mTc]Tc-DG2 (CCK₂R-agonist reference) was conducted in HEK293-CCK₂R/CCK_2i4svR cells and mice models, qualifying [^99mTc]Tc-DGA1 for further study in patients with CCK₂R-pos. tumors and single-photon emission computed tomog./CT.

Molecular Pharmaceutics 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, Product Details of C11H22N2O4.

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

Okuno, Toshiaki published the artcileBiochemical characterization of three BLT receptors in zebrafish, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is PLoS One (2015), 10(3), e0117888/1-e0117888/19, database is CAplus and MEDLINE.

The leukotriene B4 (LTB4) receptor 1 (BLT1) is a high affinity receptor for LTB4, a chemotactic and inflammatory eicosanoid. The LTB4 receptor 2 (BLT2) was originally identified as a low affinity receptor for LTB4, and, more recently, as a high affinity receptor for 12-hydroxyheptadecatrienoic acid (12-HHT). The zebrafish BLT receptors have not been previously identified and the in vivo functions of these receptors have been unknown. In this paper, we describe one zebrafish BLT1-like receptor, Blt1, and two zebrafish BLT2-like receptors, Blt2a and Blt2b. Cells expressing Blt1 exhibited LTB4-induced intracellular [Ca2+] increases, inhibition of cAMP production, ligand-dependent [35S]GTPγS binding, and transforming growth factor-α (TGFα) shedding activity in a dose-dependent manner, similar to human BLT1. Cells expressing Blt2a and Blt2b exhibited 12-HHT- and LTB4-induced intracellular [Ca2+] increases, inhibition of cAMP production, [35S]GTPγS binding, and TGFα shedding activity, with a dose-dependency similar to human BLT2. Reverse transcription (RT)-PCR anal. and whole-mount in situ hybridization revealed that blt1, blt2a, blt2b, zebrafish LTA4 hydrolase (lta4h), and zebrafish 5-lipoxiganase (5lo) are expressed in zebrafish embryos. Knockdown of blt1 by morpholino antisense oligonucleotides resulted in delayed epiboly at gastrulation. Consistently, knockdown of lta4h, an enzyme mediating LTB4 production, induced a phenotype similar to knockdown of blt1. These results suggest that the LTB4-BLT1 axis is involved in epiboly in zebrafish development.

PLoS One 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, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea.

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