Month: November 2022

Yasuda, Daisuke published the artcileRole of leukotrienes in various diseases: analyses of the receptor-deficient mice, Formula: C12H23N3S, the publication is Jikken Igaku (2010), 28(20), 3378-3385, database is CAplus.

Leukotriene (LT) is conventionally known as bioactive lipids and play an important role in the innate immune response or allergic reaction to the bacteria, and cysteinyl LT and LTB₄ (LTC₄, LTD₄, LTE₄) will be generally classified based on the difference in production pathway. By the identification of two kinds each of G protein-coupled receptors towards each leukotriene in latter half of 1990, (BLT1, CysLT1 and BLT2, CysLT2) triggered energetic research were promoted and as a result, the role of leukotriene in the body has gradually become clear with a wide range of possibilities. In this paper, the anal. result of mice engineered receptor that has reported in the course of the research and also introduce here the latest findings on the metabolic disease of bone, multiple sclerosis, and reperfusion myocardial ischemia, recent involvement of the LT model in various diseases.

Jikken Igaku 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 C7H5Br2F, Formula: C12H23N3S.

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

Hashimoto, Toru published the artcileIridium-Catalyzed [2+2+2] Cycloaddition of α,ω-Diynes with Cyanamides, Application In Synthesis of 2451-91-4, the publication is Advanced Synthesis & Catalysis (2015), 357(18), 3901-3916, database is CAplus.

The complex [Ir(cod)Cl]₂/DPPF or rac-BINAP is an efficient catalyst for the [2+2+2] cycloaddition of α,ω-diynes with cyanamides. A wide range of cyanamides derived from secondary amines are good coupling partners for α,ω-diynes. The reaction of unsym. α,ω-diynes possessing two different internal alkyne moieties with cyanamides is regioselective. A competitive experiment showed that cyanamide is more reactive than nitrile. This higher reactivity of cyanamide than nitrile was analyzed based on d. functional theory (DFT) calculations at the B3LYP level.

Advanced Synthesis & Catalysis 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 In Synthesis of 2451-91-4.

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

Yokota, Yosuke published the artcileAbsence of LTB4/BLT1 axis facilitates generation of mouse GM-CSF-induced long-lasting antitumor immunologic memory by enhancing innate and adaptive immune systems, Synthetic Route of 321673-30-7, the publication is Blood (2012), 120(17), 3444-3454, database is CAplus and MEDLINE.

BLT1 is a high-affinity receptor for leukotriene B4 (LTB4) that is a potent lipid chemoattractant for myeloid leukocytes. The role of LTB4/BLT1 axis in tumor immunol., including cytokine-based tumor vaccine, however, remains unknown. We here demonstrated that BLT1-deficient mice rejected s.c. tumor challenge of GM-CSF gene-transduced WEHI3B (WGM) leukemia cells (KO/WGM) and elicited robust antitumor responses against second tumor challenge with WEHI3B cells. During GM-CSF-induced tumor regression, the defective LTB4/BLT1 signaling significantly reduced tumor-infiltrating myeloid-derived suppressor cells, increased the maturation status of dendritic cells in tumor tissues, enhanced their CD4⁺ T-cell stimulation capacity and migration rate of dendritic cells that had phagocytosed tumor-associated antigens into tumor-draining lymph nodes, suggesting a pos. impact on GM-CSF-sensitized innate immunity. Furthermore, KO/WGM mice displayed activated adaptive immunity by attenuating regulatory CD4⁺ T subsets and increasing numbers of Th17 and memory CD44^hiCD4⁺ T subsets, both of which elicited superior antitumor effects as evidenced by adoptive cell transfer. In vivo depletion assays also revealed that CD4⁺ T cells were the main effectors of the persistent antitumor immunity. Our data collectively underscore a neg. role of LTB4/BLT1 signaling in effective generation and maintenance of GM-CSF-induced antitumor memory CD4⁺ T cells.

Blood 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 C28H18O4, Synthetic Route of 321673-30-7.

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

Sugiyama, Toru published the artcileβ-PNA: Peptide nucleic acid (PNA) with a chiral center at the β-position of the PNA backbone, Category: amides-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(24), 7317-7320, database is CAplus and MEDLINE.

Peptide nucleic acid (PNA) monomers with a Me group at the β-position have been synthesized. The modified monomers were incorporated into PNA oligomers using Fmoc chem. for solid-phase synthesis. Thermal denaturation and CD studies have shown that PNA containing the S-form monomers was well suited to form a hybrid duplex with DNA, whose stability was comparable to that of unmodified PNA-DNA duplex, whereas PNA containing the R-form monomers was not.

Bioorganic & Medicinal Chemistry Letters 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 C27H29N5O5, Category: amides-buliding-blocks.

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

Luo, Zhongli published the artcileOne-Pot Synthesis of Tertiary Amides from Organic Trichlorides through Oxygen Atom Incorporation from Air by Convergent Paired Electrolysis, Computed Properties of 360-92-9, the publication is Journal of Organic Chemistry (2021), 86(8), 5983-5990, database is CAplus and MEDLINE.

A convergent paired electrolysis catalyzed by a B12 complex for the one-pot synthesis of a tertiary amide from organic trichlorides has been developed. Various readily available organic trichlorides, such as benzotrichloride and its derivatives, chloroform, dichlorodiphenyltrichloroethane (DDT), trichloro-2,2,2-trifluoroethane (CFC-113a), and trichloroacetonitrile (CNCCl₃), were converted to amides in the presence of tertiary amines through oxygen incorporation from air at room temperature The amide formation mechanism in the paired electrolysis, which was mediated by a cobalt complex, was proposed.

Journal of Organic Chemistry 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 C6H10F3NO, Computed Properties of 360-92-9.

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

Takatori, Kichitaro published the artcileSyntheses of amides derived from heterocyclic acids and heterocyclic amines and their antitumor activities, Application In Synthesis of 51987-99-6, the publication is Yakugaku Zasshi (1976), 96(4), 471-4, database is CAplus and MEDLINE.

Pyridineacetamides I, II (R = 3-, 4-pyridyl) and 12 thiadiazoles (III, R = 3-,4-pyridyl, 2-thienyl, 2-furyl; R1 = H, CHMe2, CH2CHMe2) were prepared from the phenyl esters of heterocyclic acids and heterocyclic amines preparation procedure not given in the original. III (R = 4-pyridyl, R1 = H, CHMe2, CH2CHMe2; R = 3-pyridyl, R1 = CHMe2, R = 2-thienyl, R1 = CHMe2CH2CHMe2; R = 2-furyl, R1 = CHMe2, CH2CHMe2) had slight antitumor activity against Ehrlich ascites carcinoma and crocker sarcoma-180 in mice.

Yakugaku Zasshi 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 C42H63O3P, Application In Synthesis of 51987-99-6.

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

Ghidu, Victor P. published the artcileA new and efficient synthetic route for the anxiolytic agent CL285032, Synthetic Route of 325715-13-7, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(1), 259-261, database is CAplus and MEDLINE.

CL285032, i.e. 6-[3-(acetylmethylamino)phenyl]-3-methyl[1,2,4]triazolo[4,3-b]pyridazine, is an anxiolytic compound currently under investigation as a possible treatment for canine noise phobia associated anxiety. A robust scale-up and manufacturing process is essential for the development and marketability of the drug. The current synthetic route, although reliable, requires 7 steps and has a low overall yield (18%), leaving opportunity for improvement. The authors present an efficient alternative approach toward the synthesis of CL285032 from 3-AcMeNC₆H₄Ac over 3 steps with 65% overall yield.

Bioorganic & Medicinal Chemistry Letters published new progress about 325715-13-7. 325715-13-7 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Ketone,Amide, name is N-(3-Acetylphenyl)-N-methylacetamide, and the molecular formula is C11H13NO2, Synthetic Route of 325715-13-7.

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

Kumar, Arvind published the artcileKetene dithioacetals. Part 12. Synthesis and reactions of α-oxoketene dithioacetals derived from heterocyclic ketones, Safety of 2-Cyano-N-ethylacetamide, the publication is Journal of Chemical Research, Synopses (1979), 268-9, database is CAplus.

Ten title dithioacetals I [R²R³ = C(SMe)₂](R = H, Me; R¹ = H, Me, OMe; X = O, S, NSO₂C₆H₄Me-4; n = 1, 2) were prepared (51-75%) from the corresponding benzopyranones I (R² = R³ = H) by treatment with CS₂ in the presence of NaOCMe₃ followed by methylation. I [R = R¹ = H, R²R³ = C(SMe)₂, X = S, n = 1] (II) reacted with NH₂NH₂ in EtOH in the presence and absence of morpholine to give 48% benzothiopyranopyrazole III (R = NHNH₂) and 87% III (R = SMe), resp. II reacted with H₂NC(:NH)NH₂ to give 30% benzothiopyranopyrimidine IV (R = OMe) and 9% IV (R = H) and with NCCH₂CONHR (R = H, Me, Et) in the presence of NaOCHMe₂ to give 76% benzothiopyranopyridone V and 69-74% benzothiopyranonaphthyridinedione VI (R = Me, Et), resp.

Journal of Chemical Research, Synopses 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, Safety of 2-Cyano-N-ethylacetamide.

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

Marae, Islam S. published the artcileSynthesis, characterization and crystal structure of some novel partially hydrogenated isoquinolines and their fused heterocyclic systems, Application of 2-Chloroacetamide, the publication is Journal of Heterocyclic Chemistry (2022), 59(7), 1230-1240, database is CAplus.

Ketonic hydrolysis of 7-acetyl-4-cyano-1,6-dimethyl-6-hydroxy-8-phenyl-5,6,7,8-tetrahydro-isoquinoline-3(2H)-thione via heating with aqueous solution of potassium hydroxide resulted in both deacetylation and dehydration affording new 7,8-dihydroisoquinoline scaffold (7,8-DHISQ) I. Two simple mechanistic approaches are postulated for this synthesis. One of them was supported by converting II into I via heating with aqueous solution of potassium hydroxide. I was used as a key intermediate for synthesizing other 7,8-DHISQ’s III and IV, as well as 7,8-dihydrothienoisoquinoline. Reaction of compound II with 2-chloroacetamide by refluxing in ethanol containing sodium acetate gave 7-acetyl-1-amino-5,8-dimethyl-6-phenyl-6,7-dihydrothieno[2,3-c] isoquinoline-2-carboxamide which was converted into full aromatized pyrimidothienoisoquinoline on treatment with tri-Et orthoformate. Reaction of II with both hydrazine hydrate and hydroxylamine hydrochloride afforded tetrahydropyrazolo-isoquinoline and tetrahydroisoxazoloisoquinoline, resp. Reaction of tetrahydroisoxazoloisoquinoline with N-(4-chlorophenyl)-2-chloroacetamide produced (N-phenylcarbamoylmethylthio)tetra-hydroisoxazoloisoquinoline which was converted into tetrahydroisoxazolothieno-isoquinoline upon heating with sodium ethoxide. Also, crystal structures of compounds III and another tetrahydropyrazoloisoquinoline were determined via X-rays diffraction anal.

Journal of Heterocyclic 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, Application of 2-Chloroacetamide.

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

Adrian, Rafael A. published the artcileBis(isonicotinamide-κN)silver(I) trifluoromethanesulfonate acetonitrile disolvate, Application In Synthesis of 1453-82-3, the publication is IUCrData (2021), 6(10), x211073, database is CAplus.

The central AgI atom of the title salt, [Ag(INAM)₂](CF₃SO₃)·2CH₃CN, where INAM is isonicotinamide (C₆H₆N₂O), is twofold coordinated by the pyridine N atoms of two isonicotinamide ligands creating a slightly distorted linear mol. geometry. The formation of polymeric chains {[Ag(INAM)₂]⁺}_n, held together by discrete hydrogen bonds through the amide group of the INAM ligand leaves voids for non-coordinating acetonitrile mols. that interact the silver metal center via regium bonds.

IUCrData 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