Month: November 2022

Smith, David P. published the artcileTrifluoromethyldiazirine: an effective photo-induced cross-linking probe for exploring amyloid formation, Quality Control of 360-92-9, the publication is Chemical Communications (Cambridge, United Kingdom) (2008), 5728-5730, database is CAplus and MEDLINE.

The separative and anal. power of ion mobility spectrometry-mass spectrometry combined with photo-induced crosslinking of site-specifically incorporated trifluoromethyldiazirine provides a powerful approach towards structural characterization of amyloid fibrils.

Chemical Communications (Cambridge, United Kingdom) published new progress about 360-92-9. 360-92-9 belongs to amides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Amine,Aliphatic hydrocarbon chain,Amide, name is N,N-Diethyl-2,2,2-trifluoroacetamide, and the molecular formula is C24H29N5O3, Quality Control of 360-92-9.

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

Jahn, Ullrich published the artcile3,3-dichloroprop-2-eniminium salts (vinylogous Viehe salts). A study of their reactivity towards nucleophiles, Quality Control of 14294-10-1, the publication is Synthesis (1997), 573-588, database is CAplus.

The title compounds, [Cl₂C:CC:N⁺R₂]Cl^– [I; R₂ = Me₂, (CH₂)₄, (CH₂)₂O(CH₂)₂, (CH₂)₅] react regioselectively at either the 1- or 3-position depending on the reaction pattern. Chloro substitution affording new propene iminium salts is preferred e.g. in the reaction with mercaptans, amines, and some activated arenes and hetarenes. Nucleophilic attack at the 1-position providing in allyl or allylidene structure is observed e.g. in the reaction with H₂O, EtOH, trialkyl phosphite, Me₃SiCN, Grignard reagents, and acceptor activated methylene compounds Reaction at both positions with heterocyclization to 1,3-thiazine-6-thiones occurs with thioamide functions. The regiochem. depends on a complex interplay of several factors in contrast to the FMO predicted orientation. The utility of I and some consecutive products as versatile C₃-building blocks for further syntheses is foreseeable.

Synthesis published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, Quality Control of 14294-10-1.

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

Brice, Reoyo-Prats published the artcileContinuous degradation of micropollutants in real world treated wastewaters by photooxidation in dynamic conditions, HPLC of Formula: 137862-53-4, the publication is Water Research (2022), 118777, database is CAplus and MEDLINE.

Wastewater is a major issue for the ecosystem because of its considerable quantities, the treatment methods adopted in the large majority of WWTPs, and its level of contamination by various types of pollutants, especially emerging ones. One of the solutions considered to reduce this pressure on water is the reuse of wastewater after treatment for watering green areas, road cleaning, industry, groundwater recharge but also for crop irrigation. This paper proposes to study the capabilities of a photoreactor for the removal of micropollutants contained in wastewater from wastewater treatment plants. The experiments are carried out under dynamic artificial irradiation conditions which can be controlled in order to apply irradiation representative of the sunshine conditions. The experiments aim at treating a real effluent from urban wastewater. On the basis of these data, the photo-oxidation mass capacities expressed per unit of irradiated surface and per day were evaluated. Our results show that the oxidation process acts in a selective and differentiated manner according to the categories of substances and within each category. Some mols. are not or only partially oxidized. Note that the photo-reactor fed continuously with wastewater from wastewater treatment plants containing about 80 substances, is subjected to a typical irradiation setpoint of a sunny day in Apr. This allows to define the instantaneous and daily capacities of the system with respect to the target mols.

Water Research 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, HPLC of Formula: 137862-53-4.

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

Hijioka, Masanori published the artcileInhibition of leukotriene B₄ action mitigates intracerebral hemorrhage-associated pathological events in mice, Application of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Journal of Pharmacology and Experimental Therapeutics (2017), 360(3), 399-408, database is CAplus and MEDLINE.

Infiltration of neutrophils has been suggested to play an important role in the pathogenesis of intracerebral hemorrhage (ICH) for which effective therapeutic interventions remain unavailable. In the present study we focused on leukotriene B₄ (LTB₄) as a potent chemotactic factor for neutrophils in order to address its contribution to the pathol. events associated with ICH. ICH with hematoma expansion into the internal capsule that resulted in severe sensorimotor dysfunction was induced by injection of collagenase in mouse striatum. We found that LTB₄ as well as mRNAs of 5-lipoxygenase (5-LOX) and 5-LOXactivating protein were increased in the brain after ICH. Daily treatment with a 5-LOX inhibitor zileuton (3 or 10 mg/kg, i.v.) prevented ICH-induced increase in LTB₄, attenuated neutrophil infiltration into the hematoma, and ameliorated sensorimotor dysfunction. In addition, mice deficient in LTB₄ receptor BLT1 exhibited a lower number of infiltrating neutrophils in the hematoma and lower levels of sensorimotor dysfunction after ICH than did wild-type mice. Similarly, daily treatment of mice with BLT antagonist ONO-4057 (30 or 100 mg/kg, by mouth) from 3 h after induction of ICH inhibited neutrophil infiltration and ameliorated sensorimotor dysfunction. ONO-4057 also attenuated inflammatory responses of microglia/macrophages in the perihematoma region and axon injury in the internal capsule. These results identify LTB₄ as a critical factor that plays a major role in the pathogenic events in ICH, and BLT1 is proposed as a promising target for ICH therapy.

Journal of Pharmacology and Experimental Therapeutics 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

Erdem, Rahsan published the artcileA Phase 2a randomized, single-center, double-blind, placebo-controlled study to evaluate the safety and preliminary efficacy of oral iOWH032 against cholera diarrhea in a controlled human infection model., Formula: C22H15Br2N3O4, the publication is PLoS neglected tropical diseases (2021), 15(11), e0009969, database is MEDLINE.

Cholera remains a major cause of infectious diarrhea globally. Despite the increased availability of cholera vaccines, there is still an urgent need for other effective interventions to reduce morbidity and mortality. Furthermore, increased prevalence of antibiotic-resistant Vibrio cholerae threatens the use of many drugs commonly used to treat cholera. We developed iOWH032, a synthetic small molecule inhibitor of the cystic fibrosis transmembrane conductance regulator chloride channel, as an antisecretory, host-directed therapeutic for cholera. In the study reported here, we tested iOWH032 in a Phase 2a cholera controlled human infection model. Forty-seven subjects were experimentally infected with V. cholerae El Tor Inaba strain N16961 in an inpatient setting and randomized to receive 500 mg iOWH032 or placebo by mouth every 8 hours for 3 days to determine the safety and efficacy of the compound as a potential treatment for cholera. We found that iOWH032 was generally safe and achieved a mean (± standard deviation) plasma level of 4,270 ng/mL (±2,170) after 3 days of oral dosing. However, the median (95% confidence interval) diarrheal stool output rate for the iOWH032 group was 25.4 mL/hour (8.9, 58.3), compared to 32.6 mL/hour (15.8, 48.2) for the placebo group, a reduction of 23%, which was not statistically significant. There was also no significant decrease in diarrhea severity and number or frequency of stools associated with iOWH032 treatment. We conclude that iOWH032 does not merit future development for treatment of cholera and offer lessons learned for others developing antisecretory therapeutic candidates that seek to demonstrate proof of principle in a cholera controlled human infection model study. Trial registration: This study is registered with ClinicalTrials.gov as NCT04150250.

PLoS neglected tropical diseases published new progress about 1191252-49-9. 1191252-49-9 belongs to amides-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,CFTR, name is 3-(3,5-Dibromo-4-hydroxyphenyl)-N-(4-phenoxybenzyl)-1,2,4-oxadiazole-5-carboxamide, and the molecular formula is C22H15Br2N3O4, Formula: C22H15Br2N3O4.

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

Wellaway, Christopher R. published the artcileDiscovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening, Related Products of amides-buliding-blocks, the publication is Journal of Medicinal Chemistry (2020), 63(2), 714-746, database is CAplus and MEDLINE.

The bromodomain and extraterminal (BET) family of bromodomain-containing proteins are important regulators of the epigenome through their ability to recognize N-acetyl lysine (KAc) post-translational modifications on histone tails. These interactions have been implicated in various disease states and, consequently, disruption of BET-KAc binding has emerged as an attractive therapeutic strategy with a number of small mol. inhibitors now under investigation in the clinic. However, until the utility of these advanced candidates is fully assessed by these trials, there remains scope for the discovery of inhibitors from new chemotypes with alternative physicochem., pharmacokinetic, and pharmacodynamic profiles. Herein, we describe the discovery of a candidate-quality dimethylpyridone benzimidazole compound which originated from the hybridization of a dimethylphenol benzimidazole series, identified using encoded library technol., with an N-Me pyridone series identified through fragment screening. Optimization via structure- and property-based design led to I-BET469, which possesses favorable oral pharmacokinetic properties, displays activity in vivo, and is projected to have a low human efficacious dose.

Journal of Medicinal Chemistry published new progress about 475216-25-2. 475216-25-2 belongs to amides-buliding-blocks, auxiliary class Fluoride,Nitro Compound,Amine,Benzene,Amide,Benzene Compounds, name is 4-Fluoro-N-methyl-3-nitrobenzamide, and the molecular formula is C3H9ClOS, Related Products of amides-buliding-blocks.

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

Kamata, Mariko published the artcileRole of the high-affinity leukotriene B4 receptor signaling in fibrosis after unilateral ureteral obstruction in mice, Application of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is PLoS One (2019), 14(2), e0202842, database is CAplus and MEDLINE.

Leukotriene B4 (LTB4) is a lipid mediator that acts as a potent chemoattractant for inflammatory leukocytes. Kidney fibrosis is caused by migrating inflammatory cells and kidney-resident cells. Here, we examined the role of the high-affinity LTB4 receptor BLT1 during development of kidney fibrosis induced by unilateral ureteral obstruction (UUO) in wild-type (WT) mice and BLT1 knockout (BLT1-/-) mice. We found elevated expression of 5-lipoxygenase (5-LOX), which generates LTB4, in the renal tubules of UUO kidneys from WT mice and BLT1-/- mice. Accumulation of immunoreactive type I collagen in WT UUO kidneys increased over time; however, the increase was less prominent in BLT1-/- UUO kidneys. Accumulation of S100A4-pos. fibroblasts increased temporally in WT UUO kidneys, but was again less pronounced in-BLT1-/- UUO kidneys. The same was true of mRNA encoding transforming growth factor-β (TGF)-β and fibroblast growth factor (FGF)-2. Finally, accumulation of F4/80-pos. macrophages, which secrete TGF-β, increased temporally in WT UUO and BLT1-/- UUO kidneys, but to a lesser extent in the latter. Following LTB4 stimulation in vitro, macrophages showed increased expression of mRNA encoding TGF-β/FGF-2 and Col1a1, whereas L929 fibroblasts showed increased expression of mRNA encoding α smooth muscle actin (SMA). Bone marrow (BM) transplantation studies revealed that the area pos. for type I collagen was significantly smaller in BLT1-/-BM→WT than in WT-BM→WT. Thus, LTB4-BLT1 signaling plays a critical role in fibrosis in UUO kidneys by increasing accumulation of macrophages and fibroblasts. Therefore, blocking BLT1 may prevent renal fibrosis.

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, Application of [(2-Hexylcyclopentylidene)amino]thiourea.

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

Rezaei, Manuchehr published the artcileOne-pot green catalytic synthesis of primary amides in aqueous medium by Cu^II-immobilized silica-based magnetic retrievable nanocatalyst, Application of 2,4-Dichlorobenzamide, the publication is Catalysis Communications (2017), 38-42, database is CAplus.

In order to develop a new nanocatalyst, a copper-birhodanine derivative complex crafted onto Fe₃O₄@SiO₂ nanoparticle [abbreviated as Fe₃O₄@SiO₂-Ligand-Cu(II)] was synthesized and the structure was characterized by different physicochem. techniques. This new magnetic nanoparticle revealed high catalytic performance for one-pot green synthesis of primary amides from aldehydes and NH₂OH·HCl in water as a green solvent. The effects of catalyst amounts, reaction temperature, various bases and type of solvent on catalytic activity were also investigated. The catalyst was retrieved eight times without significant loss of its catalytic activity.

Catalysis Communications 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, Application of 2,4-Dichlorobenzamide.

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

Paula-Neto, Heitor A. published the artcileInhibition of Guanylyl Cyclase Restores Neutrophil Migration and Maintains Bactericidal Activity Increasing Survival in Sepsis, Application In Synthesis of 321673-30-7, the publication is Shock (2011), 35(1), 17-27, database is CAplus and MEDLINE.

Sepsis results from an overwhelming response to infection and is a major contributor to death in intensive care units worldwide. In recent years, we and others have shown that neutrophil functionality is impaired in sepsis. This correlates with sepsis severity and contributes to aggravation of sepsis by precluding bacterial clearance. Nitric oxide (NO) is a major contributor to the impairment of neutrophil function in sepsis. However, attempts to inhibit NO synthesis in sepsis resulted in increased death despite restoring neutrophil migration. This could be in part attributed to a reduction of the NO-dependent microbicidal activity of neutrophils. In sepsis, the beneficial effects resulting from the inhibition of soluble guanylyl cyclase (sGC), a downstream target of NO, have long been appreciated but poorly understood. However, the effects of sGC inhibition on neutrophil function in sepsis have never been addressed. In the present study, we show that TLR activation in human neutrophils leads to decreased chemotaxis, which correlated with chemotactic receptor internalization and increased G protein-coupled receptor kinase 2 expression, in a process involving the NO-sGC-protein kinase G axis. We also demonstrate that inhibition of sGC activity increased survival in a murine model of sepsis, which was paralleled by restored neutrophil migratory function and increased bacterial clearance. Finally, the beneficial effect of sGC inhibition could also be demonstrated in mice treated after the onset of sepsis. Our results suggest that the beneficial effects of sGC inhibition in sepsis could be at least in part attributed to a recovery of neutrophil functionality.

Shock 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 In Synthesis of 321673-30-7.

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

Gonzalez-Fernandez, Rebeca published the artcileCatalytic hydration of cyanamides with phosphinous acid-based ruthenium(II) and osmium(II) complexes: scope and mechanistic insights, SDS of cas: 2451-91-4, the publication is Catalysis Science & Technology (2020), 10(12), 4084-4098, database is CAplus.

The synthesis of a large variety of ureas (26 examples) was successfully accomplished by hydration of the corresponding cyanamides using the phosphinous acid-based complexes I [M = Ru, Os] as catalysts. The reactions proceeded cleanly under mild conditions (40-70°), in the absence of any additive, employing low metal loadings (1 mol%) and water as the sole solvent. In almost all the cases, the osmium complex I [M = Os] featured a superior reactivity in comparison to that of its ruthenium counterpart I [M = Ru]. In addition, for both catalysts, the reaction rates observed for the hydration of the cyanamide substrates were remarkably faster than those involving classical aliphatic and aromatic nitriles. Computational studies allowed us to rationalize all these trends. Thus, the calculations indicated that the presence of a nitrogen atom directly linked to the C≡N bond depopulates electronically the nitrile carbon by inductive effect when coordinated to the metal center, thus favoring the intramol. nucleophilic attack of the OH group of the phosphinous acid ligand to this carbon. On the other hand, the higher reactivity of Os vs Ru seems to be related with the lower ring strain on the incipient metallacycle that starts to form in the transition state associated with this key step in the catalytic cycle. Indirect exptl. evidence of the generation of the metallacyclic intermediates was obtained by studying the reactivity of I [M = Ru] towards dimethylcyanamide in methanol and ethanol. The reactions afforded compounds II·SbF₆ [R = Me, Et], resulting from the alcoholysis of the metallacycle, which could be characterized by single-crystal X-ray diffraction.

Catalysis Science & Technology 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, SDS of cas: 2451-91-4.

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