Month: November 2022

Hernandez-Folgado, Laura published the artcileNovel derivatives of 3-alkyl-1,5-diaryl-1H-1,2,4-triazoles and their pharmacological evaluation as CB₁ cannabinoid ligands, Name: 2,4-Dichlorobenzamide, the publication is Monatshefte fuer Chemie (2008), 139(9), 1073-1082, database is CAplus.

In a previous study, the authors identified 3-alkyl-1,5-diaryl-1H-1,2,4-triazoles, e.g., I, to be a novel class of cannabinoid type-1 (CB₁) receptor antagonists. However, the synthesis yields for the ligands were low. An alternative synthesis pathway with improved yields is presented here. In addition, they have synthesized new structural derivatives and studied their results in competitive radioligand binding assays for cannabinoid receptors.

Monatshefte fuer Chemie published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, Name: 2,4-Dichlorobenzamide.

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

Rothlingshofer, Manuel published the artcileNucleic Acid-Templated Energy Transfer Leading to a Photorelease Reaction and its Application to a System Displaying a Nonlinear Response, Safety of 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, the publication is Journal of the American Chemical Society (2011), 133(45), 18110-18113, database is CAplus and MEDLINE.

The photocleavage of a nitrobenzyl-type linker (NPPOC) at 405 nm wavelength was enabled by nucleic acid-templated energy transfer from a sensitizer (thioxanthenone) to the linker. This strategy was used to release profluorescent rhodamine, which facilitated monitoring of the reaction via fluorescence measurement in a nonoverlapping window with the sensitizer/photocleavage reaction. The rate acceleration of the templated reaction was greater than 20-fold over the background reaction. The templated reaction was used in conjunction with strand displacement to design four-component systems that responded to an analyte (DNA). Programming a specific hierarchical relationship among the four components enabled the design of a system that responded first pos. and then neg. to increasing levels of an analyte.

Journal of the American Chemical Society published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C40H35N7O8, Safety of 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid.

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

Huang, Kuo-Ting published the artcileCombinatorial Self-Assembly of Glycan Fragments into Microarrays, Recommanded Product: 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, the publication is ChemBioChem (2011), 12(1), 56-60, database is CAplus and MEDLINE.

We have demonstrated that complex glycan arrays can be accessed through the combinatorial self assembly of PNA-encoded carbohydrate fragments. Although the use of DNA microarrays to sort carbohydrate-DNA conjugates had previously been reported, previous efforts were restricted to monosaccharides and did not explore a broad range of glycan structures, nor their combinatorial assembly. The cooperativity of the fragments in their interaction with carbohydrate-binding proteins was demonstrated with two different lectins. The binding profile showed the strongest interaction for discrete combinations of two fragments. Importantly, the PNA-tagged glycans can be readily prepared from native oligosaccharides obtained from natural or com. sources by conversion of the anomeric position into a thiol on a mg scale by a two- to three-step process. The simplicity of the protocols described should make glycan arrays more broadly accessible. Immobilization of glycans by hybridization offers a reliable approach by which to obtain a homogeneous distribution of ligands within a microarray spot and allows the use of microarrays with higher d. than accessible by contact printing, which is currently the standard practice. Last but not least, combinatorial self assembly of fragments on DNA microarrays should be broadly applicable beyond the glycan fragments described here.

ChemBioChem published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C40H35N7O8, Recommanded Product: 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid.

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

Hill, Timothy A. published the artcileInhibition of Dynamin Mediated Endocytosis by the Dynoles-Synthesis and Functional Activity of a Family of Indoles, SDS of cas: 15029-36-4, the publication is Journal of Medicinal Chemistry (2009), 52(12), 3762-3773, database is CAplus and MEDLINE.

Screening identified two bisindolylmaleimides as 100 μM inhibitors of the GTPase activity of dynamin I. Focused library approaches allowed development of indole-based dynamin inhibitors called dynoles. 100-Fold in vitro enhancement of potency was noted with the best inhibitor, 2-cyano-N-octyl-3-[1-(3-dimethylaminopropyl)-1H-indol-3-yl]-acrylamide (dynole 34-2), a 1.3 ± 0.3 μM dynamin I inhibitor. Dynole 34-2 potently inhibited receptor mediated endocytosis (RME) internalization of Texas red-transferrin. The rank order of potency for a variety of dynole analogs on RME in U2OS cells matched their rank order for dynamin inhibition, suggesting that the mechanism of inhibition is via dynamin. Dynoles are the most active dynamin I inhibitors reported for in vitro or RME evaluations. Dynole 34-2 is 15-fold more active than dynasore against dynamin I and 6-fold more active against dynamin mediated RME (IC₅₀ ∼15 μM; RME IC₅₀ ∼80 μM). The dynoles represent a new series of tools to better probe endocytosis and dynamin-mediated trafficking events in a variety of cells.

Journal of Medicinal Chemistry published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C5H8N2O, SDS of cas: 15029-36-4.

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

Tomlin, Frederick M. published the artcileSite-specific incorporation of quadricyclane into a protein and photocleavage of the quadricyclane ligation adduct, COA of Formula: C11H22N2O4, the publication is Bioorganic & Medicinal Chemistry (2018), 26(19), 5280-5290, database is CAplus and MEDLINE.

The quadricyclane (QC) ligation is a bioorthogonal reaction between a quadricyclane moiety and a nickel bis(dithiolene) derivative Here we show that a QC amino acid can be incorporated into a protein site-specifically using the pyrrolysine-based genetic code expansion platform, and subsequently used for ligation chem. Addnl., we exploited the photolability of the QC ligation product to render the adduct cleavable with a handheld UV lamp. We further developed a protein purification method that involves QC ligation of biotin to a protein of interest, capture on streptavidin resin, and finally release using only UV light. The QC ligation thus brings novel chem. manipulations to the realm of bioorthogonal chem.

Bioorganic & Medicinal 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 C8H12BNO5S, COA of Formula: C11H22N2O4.

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

Song, Guoyong published the artcileSynthesis of Quinolines via Rh(III)-Catalyzed Oxidative Annulation of Pyridines, Formula: C10H14N2O, the publication is Journal of Organic Chemistry (2011), 76(18), 7583-7589, database is CAplus and MEDLINE.

Selective synthesis of quinolines, e.g., I (R¹ = H, Me, MeO, Cl; R² = H, Me, MeO, Cl), has been achieved via oxidative annulation of functionalized pyridines with two alkyne mols. under Rh(III)-catalyzed cascade C-H activation of pyridines using Cu(OAc)₂ as an oxidant. The selectivity of this reaction is oxidant-dependent, particularly on the anion of the oxidant.

Journal of Organic Chemistry published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C8H7NaO4S, Formula: C10H14N2O.

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

Li, Wanjing published the artcileEfficacy of angiotensin receptor neprilysin inhibitor in Asian patients with refractory hypertension, Product Details of C24H29N5O3, the publication is Journal of Clinical Hypertension (Hoboken, NJ, United States) (2022), 24(4), 449-456, database is CAplus and MEDLINE.

Sacubitril/valsartan, simultaneously inhibits neprilysin and angiotensin II receptor, showed an effect in reducing blood pressure (BP). The authors aimed to study whether it can be used as an antihypertensive agent in patients with refractory hypertension who have already been treated. A total of 66 Chinese patients with refractory hypertension were enrolled. Patients received sacubitril/valsartan 200 instead of angiotensin II receptor blocker or angiotensin converting enzyme inhibitor while other agents continued. If BP was uncontrolled after 4 wk, sacubitril/valsartan was increased to 400 mg. The BP reduction was evaluated by office BP and ambulatory BP monitoring after 8-wk treatment. The baseline office BP and mean arterial pressure (MAP) were 150.0/95.0 mmHg and 113.3 mmHg. BP and MAP reduced to 130.6/83.2 mmHg and 99.0 mmHg at week 8. Office BP and MAP reductions were 19.4/11.8 mmHg and 14.3 mmHg at endpoint (all p < .001). The 24-h, daytime and nighttime ambulatory BP were 146.2/89.1, 148.1/90.3, and 137.5/83.7 mmHg, resp. at baseline, and BP reduced to 129.6/79.8, 130.6/81.1, and 121.7/75.8 mmHg, resp. at week 8. The 24-h, daytime and nighttime ambulatory BP reductions were 16.6/9.3, 17.5/9.2, and 15.8/7.9 mmHg, resp. at endpoint (all p < .001). Sacubitril/valsartan significantly reduced office and ambulatory BP in refractory hypertension patients. Author study provided new evidence for sacubitril/valsartan in refractory hypertension.

Journal of Clinical Hypertension (Hoboken, NJ, United States) published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Product Details of C24H29N5O3.

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

Jagt, Richard B. C. published the artcilePattern-based recognition of heparin contaminants by an array of self-assembling fluorescent receptors, Quality Control of 1869-45-0, the publication is Angewandte Chemie, International Edition (2009), 48(11), 1995-1997, database is CAplus and MEDLINE.

Tracking down potential killers: Strong host-guest interactions enable the facile combination of polycationic cyclodextrin binding motifs (blue) with fluorescent reporters (orange) tethered to a hydrophobic guest mol. (dark green). An array of supramol. fluorescent receptors prepared by this modular approach was used for the pattern-based recognition of neg. charged contaminants in the anticoagulant drug heparin.

Angewandte Chemie, International Edition published new progress about 1869-45-0. 1869-45-0 belongs to amides-buliding-blocks, auxiliary class Trifluoromethylated Building Blocks, name is 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, and the molecular formula is C4H6F3NOS, Quality Control of 1869-45-0.

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

Dojer, Brina published the artcileIron(II) pyridinecarboxamide complexes: Synthesis, crystal structures and magnetic properties, Application In Synthesis of 1453-82-3, the publication is Journal of Molecular Structure (2022), 133393, database is CAplus.

Two new mononuclear complexes of iron(II) pyridinecarboxamides (picolinamide – pia, isonicotinamide – isn), [Fe(pia)₃]·(SO₄)·3H₂O (1) and (isnH)₂[Fe(isn)₂(SO₄)₂(H₂O)₂]·H₂O (2) were synthesized by the reaction of iron(II) sulfate heptahydrate and pyridinecarboxamides in different solvents by standard method under reflux. Both compounds were characterized by single-crystal x-ray diffraction structure anal., magnetic measurements and by FTIR spectroscopy. In the complex cation of 1 Fe²⁺ ion is six coordinated by three nitrogen and three oxygen atoms from three bidentate picolinamide ligands in mer mode. In complex anion of 2 central Fe²⁺ ion is six coordinated by two isonicotinamide ligands, two sulfate ligands and two water mols. in trans mode. In both structures complex ions are connected with counterions and crystal water mols. with intermol. hydrogen bonds. Magnetic properties of the compounds were measured between 2 K and 300 K giving the results: μ_eff = 4.5 μB for compound 1 and μ_eff = 4.7 μB for 2. Exptl. values of the IR spectra are comparable with literature data and are in good agreement with results of the structural anal.

Journal of Molecular Structure published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Application In Synthesis of 1453-82-3.

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

Galet, Colette published the artcileEffect of a Low-Fat Fish Oil Diet on Proinflammatory Eicosanoids and Cell-Cycle Progression Score in Men Undergoing Radical Prostatectomy, Category: amides-buliding-blocks, the publication is Cancer Prevention Research (2014), 7(1), 97-104, database is CAplus and MEDLINE.

We previously reported that a 4- to 6-wk low-fat fish oil (LFFO) diet did not affect serum insulin-like growth factor (IGF)-1 levels (primary outcome) but resulted in lower omega-6 to omega-3 fatty acid ratios in prostate tissue and lower prostate cancer proliferation (Ki67) as compared with a Western diet. In this post hoc anal., the effect of the LFFO intervention on serum pro-inflammatory eicosanoids, leukotriene B4 (LTB4) and 15-S-hydroxyeicosatetraenoic acid [15(S)-HETE], and the cell-cycle progression (CCP) score were investigated. Serum fatty acids and eicosanoids were measured by gas chromatog. and ELISA. CCP score was determined by quant. real-time reverse transcriptase PCR (RT-PCR). Associations between serum eicosanoids, Ki67, and CCP score were evaluated using partial correlation analyses. BLT1 (LTB4 receptor) expression was determined in prostate cancer cell lines and prostatectomy specimens. Serum omega-6 fatty acids and 15(S)-HETE levels were significantly reduced, and serum omega-3 levels were increased in the LFFO group relative to the Western diet group, whereas there was no change in LTB4 levels. The CCP score was significantly lower in the LFFO compared with the Western diet group. The 15(S)-HETE change correlated with tissue Ki67 (R = 0.48; P < 0.01) but not with CCP score. The LTB4 change correlated with the CCP score (r = 0.4; P = 0.02) but not with Ki67. The LTB4 receptor BLT1 was detected in prostate cancer cell lines and human prostate cancer specimens. In conclusion, an LFFO diet resulted in decreased 15(S)-HETE levels and lower CCP score relative to a Western diet. Further studies are warranted to determine whether the LFFO diet antiproliferative effects are mediated through the LTB4/BLT1 and 15(S)-HETE pathways. Cancer Prev Res; 7(1); 97-104. ©2013 AACR.

Cancer Prevention Research 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, Category: amides-buliding-blocks.

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