Month: November 2022

Ghosh, Santanu published the artcileAminofluorene-Mediated Biomimetic Domino Amination-Oxygenation of Aldehydes to Amides, Application of 2,4-Dichlorobenzamide, the publication is Organic Letters (2016), 18(22), 5788-5791, database is CAplus and MEDLINE.

A conceptually novel biomimetic strategy based on a domino amination-oxygenation reaction was developed for direct amidation of aldehydes under metal-free conditions employing mol. oxygen as the oxidant. 9-Aminofluorene derivatives acted as pyridoxamine-5′-phosphate equivalent for efficient, chemoselective, and operationally simple amine-transfer oxygenation reaction. Unprecedented RNH transfer involving secondary amines to produce secondary amides was achieved. In the presence of ¹⁸O₂, ¹⁸O-amide was formed with excellent (95%) isotopic purity.

Organic Letters 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

Ghosh, Santanu published the artcileMetal-Free Thermal Activation of Molecular Oxygen Enabled Direct α-CH₂-Oxygenation of Free Amines, COA of Formula: C7H5Cl2NO, the publication is Journal of Organic Chemistry (2018), 83(1), 260-266, database is CAplus and MEDLINE.

Direct oxidation of α-CH₂ group of free amines is hard to achieve due to the higher reactivity of amine moiety. Therefore, oxidation of amines involves the use of sophisticated metallic reagents/catalyst in the presence or absence of hazardous oxidants under sensitive reaction conditions. A novel method for direct C-H oxygenation of aliphatic amines through a metal-free activation of mol. oxygen has been developed. Both activated and unactivated free amines were oxygenated efficiently to provide a wide variety of amides (primary, secondary) and lactams under operationally simple conditions without the aid of metallic reagents and toxic oxidants. The method has been applied to the synthesis of highly functionalized amide-containing medicinal drugs, such as O-Me-alibendol and -buclosamide.

Journal of Organic Chemistry 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, COA of Formula: C7H5Cl2NO.

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

Rahabi, Mouna published the artcileDivergent Roles for Macrophage C-type Lectin Receptors, Dectin-1 and Mannose Receptors, in the Intestinal Inflammatory Response, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Cell Reports (2020), 30(13), 4386-4398.e5, database is CAplus and MEDLINE.

Colonic macrophages are considered to be major effectors of inflammatory bowel diseases (IBDs) and the control of gut inflammation through C-type lectin receptors is an emerging concept. We show that during colitis, the loss of dectin-1 on myeloid cells prevents intestinal inflammation, while the lack of mannose receptor (MR) exacerbates it. A marked increase in dectin-1 expression in dextran sulfate sodium (DSS)-exposed MR-deficient mice supports the critical contribution of dectin-1 to colitis outcome. Dectin-1 is crucial for Ly6C^highCCR2^high monocyte population enrichment in the blood and their recruitment to inflamed colon as precursors of inflammatory macrophages. Dectin-1 also promotes inflammasome-dependent interleukin-1β (IL-1β) secretion through leukotriene B4 production Interestingly, colonic inflammation is associated with a concomitant overexpression of dectin-1/CCL2/LTA4H and downregulation of MR on macrophages from IBD patients. Thus, MR and dectin-1 on macrophages are important mucosal inflammatory regulators that contribute to the intestinal inflammation.

Cell Reports 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

Sanders, Brandi D. published the artcileIdentification and characterization of novel sirtuin inhibitor scaffolds, HPLC of Formula: 1011557-82-6, the publication is Bioorganic & Medicinal Chemistry (2009), 17(19), 7031-7041, database is CAplus and MEDLINE.

The sirtuin proteins are broadly conserved NAD⁺-dependent deacetylases that are implicated in diverse biol. processes including DNA recombination and repair, transcriptional silencing, longevity, apoptosis, axonal protection, insulin signaling, and fat mobilization. Because of these associations, the identification of small mol. sirtuin modulators has been of significant interest. Here we report on high throughput screening against the yeast sirtuin, Hst2, leading to the identification of four unique inhibitor scaffolds that also inhibit the human sirtuins, SIRT1-3, and are able to inhibit telomeric silencing of yeast Sir2 in vivo. The identified inhibitor scaffolds range in potency from IC₅₀ values of 6.5-130 μM against Hst2. Each of the inhibitor scaffolds binds reversibly to the enzyme, and kinetic anal. reveals that each of the inhibitors is non-competitive with respect to both acetyl-lysine and NAD⁺ binding. Limited SAR anal. of the scaffolds also identifies which functional groups may be important for inhibition. These sirtuin inhibitors are low mol. weight and well-suited for lead mol. optimization, making them useful chem. probes to study the mechanism and biol. roles of sirtuins and potential starting points for optimization into therapeutics.

Bioorganic & Medicinal Chemistry published new progress about 1011557-82-6. 1011557-82-6 belongs to amides-buliding-blocks, auxiliary class Epigenetics,Sirtuin, name is 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, and the molecular formula is C25H34N4O2S, HPLC of Formula: 1011557-82-6.

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

Klimochkin, Yu. N. published the artcileSynthesis and Chemical Transformations of N-Adamantylated Amides, Formula: C2H4ClNO, the publication is Russian Journal of Organic Chemistry (2022), 58(5), 669-678, database is CAplus.

N-Adamantylated amides, e.g., I were synthesized from 1-adamantyl nitrate. The reactions were carried out in the sulfuric acid media. The proposed method was usefulness for the preparation of antiviral drug tromantadine. A number of new cage aminoamides were synthesized by reactions of N-(1-adamantyl)-2-chloroacetamide with nitrogen-containing nucleophiles with potential biol. activity.

Russian Journal of Organic Chemistry published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Formula: C2H4ClNO.

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

Yakovleva, N. L. published the artcileReaction of carboxy-, carbethoxy-, and hydroxymethylpyridines with phosphorous amides, Safety of N,N-Diethylisonicotinamide, the publication is Khimiko-Farmatsevticheskii Zhurnal (1980), 14(1), 67-9, database is CAplus.

Heating nicotinic acid, isonicotinic acid or their Et esters with P(NEt₂)₃ gave 34.8-88% resp. diethylamides; yields were higher (88%, 79.5%) using the acids. Amines I and II were prepared in 21.5 and 14.8% yield resp. from the corresponding hydroxymethyl derivatives

Khimiko-Farmatsevticheskii Zhurnal 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 C10H9NO, Safety of N,N-Diethylisonicotinamide.

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

Grabic, Roman published the artcileDesorption of pharmaceuticals and illicit drugs from different stabilized sludge types across pH, Application In Synthesis of 137862-53-4, the publication is Water Research (2022), 118651, database is CAplus and MEDLINE.

Pharmaceutical and illicit drug residues in sewage sludge may present important risks following direct application to agricultural soils, potentially resulting in uptake by plants. Leaching/desorption tests were performed on different types of stabilized sewage sludge originating from multiple treatment technologies in the Slovak Republic. Acid rain and base-rich condition of soil with different pH conditions were simulated to model the effect of widely varying pH (pH 2, 4, 7, 9, and 12) on the leaching/desorption of pharmaceuticals and illicit drugs. Twenty-nine of 93 target analytes were found above the limit of quantification in sludge or associated leachates. Total desorbed amounts of pharmaceuticals and illicit drugs ranged from 810 to 4000μg/kg, and 110 to 3600μg/kg of the dry mass of anaerobic and aerobic sludge, resp. Desorbed fractions were calculated as these values are normalized to initial sludge concentration and, therefore, were more suitable for qual. description of the behavior of individual compounds Using principal component anal., qual. anal. of the desorbed fraction confirmed the differences among sludge types, pharmaceuticals, and desorption pH. Desorbed fractions could not be related to the octanol/water distribution coefficient Desorbed fractions also did not reflect the expected ionization of studied mols. unless converted into their relative values. Generally, the lowest mobility was observed within the environmentally relevant pH range of 4-9, and high pH generally resulted in high desorption, especially in anaerobically stabilized sludges.

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, Application In Synthesis of 137862-53-4.

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

Ito, Sohei published the artcileLeukotriene B₄/leukotriene B₄ receptor pathway is involved in hepatic microcirculatory dysfunction elicited by endotoxin, SDS of cas: 321673-30-7, the publication is Shock (2008), 30(1), 87-91, database is CAplus and MEDLINE.

Leukotrienes (LTs), metabolites of arachidonic acid through 5-lipoxygenase (5-LOX), have been known to play a role in leukocyte recruitment. However, the contribution of LTB₄ to liver microcirculatory dysfunction during endotoxemia remains unknown. LTB₄ receptor (BLT1) has been identified as a high-affinity receptor specific for LTB₄. The present study was conducted to examine the roles of LTB₄ and BLT1 in hepatic microcirculatory dysfunction elicited by LPS in mice. The number of leukocytes adhering to the endothelial cells of the hepatic microvessels and perfused sinusoids was determined 4 h after the administration of LPS (0.3 mg/kg, i.v.) to male C57Bl6 mice by in vivo microscopy. A 5-LOX synthase inhibitor, AA-861 (10 or 100 mg/kg, s.c), was administered 30 min before LPS injection. BLT1 knockout mice were used to investigate whether LPS-induced hepatic microcirculatory dysfunction is mediated by BLT1 signaling. The expression of 5-LOX, intercellular adhesion mol. (ICAM) 1, and TNF-α in the liver was measured by real-time reverse-transcriptase-polymerase chain reaction. The administration of LPS caused significant accumulation of leukocyte adhesion to the hepatic microvessels and reduced sinusoidal perfusion when compared with saline-treated mice. The hepatic microcirculatory dysfunction elicited by LPS was minimized in mice pretreated with AA-861 or in BLT1 knockout mice. This was associated with the suppression of hepatic expression of 5-LOX, ICAM-1, and TNF-α. These findings suggest that the LTB₄/BLT1 pathway mediates hepatic microcirculatory dysfunction by enhanced expression of ICAM-1 and TNF-α in a murine model of endotoxemia.

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, SDS of cas: 321673-30-7.

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

Novotorzhina, Nelya N. published the artcileSynthesis of new derivatives of N,N-diethyldithiocarbamine acid and study of their anti-seize properties, Name: 2-Chloroacetamide, the publication is Neft Kimyasi va Neft E’mali Proseslari (2021), 22(1), 41-49, database is CAplus.

By the reaction of sodium N,N-diethyldithiocarbamate and chloroacetamide, S-carbamoylmethyldiethyldithiocarbamate was obtained. The conditions of two different methods for producing S(N-2,2-dimethyl-4-methyloxymethyl-1,3 dioxolane) carbamoylmethyldiethyldithiocarbamate were proposed. One of which was based on the homocondensation of hydroxylmethylcarbamoyldiethyldithiocarbamate and 2,2-dimethyl-4-hydroxymethyl-1,3-dioxolane, the other on the interaction of 2,2-dimethyl-4- chloromethylcarbamoylmethyloxymethyl-1,3-dioxolane and sodium N,N-diethyldithiocarbamate. At the first stage of the study, 4 starting reagents were synthesized, 2 of which were not previously described in the literature: 2,2-dimethyl-4-chloromethylcarbamoylmethoxymethyi-1,3-dioxolane and S-hydroxymethylcarbamoylethyldithiocarbamate. The structure of the synthesized compounds was proved by determining their elemental compositions, calculating mol. refractions based on refractive indexes and specific gravities, as well as recording IR absorption spectra on a spectrophotometer. The presence of comparatively high extreme pressure properties of the synthesized compounds in the mineral oil SN-1200 and synthetic oil consisting of penta erythritol of fatty acids was revealed and it was shown that they are superior to the known additives in the literature of tricresyl phosphate and N-allyl-5-hexyloxycarbocarbonylmethyl-1,3-thiazolidin-4-one-2-thione.

Neft Kimyasi va Neft E’mali Proseslari published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Name: 2-Chloroacetamide.

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