Tag: M.W=200-250

Rocca, Patrick published the artcileA short synthesis of the antimicrobial marine sponge pigment fascaplysine, Application of (2-Pivalamidophenyl)boronic acid, the publication is Tetrahedron Letters (1993), 34(49), 7917-18, database is CAplus.

A short and convergent synthesis of fascaplysine (I) was achieved from 3-fluoro-4-iodopyridine and 2-Me₃CCONHC₆H₄B(OH)₂ in 4 steps and 76% overall yield. The approach is based on recently developed methodol. including metalation, hetero cross-coupling and cyclization.

Tetrahedron Letters 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, Application of (2-Pivalamidophenyl)boronic acid.

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

Hostyn, Steven published the artcileSynthesis of the benzo-β-carboline isoneocryptolepine: the missing indoloquinoline isomer in the alkaloid series cryptolepine, neocryptolepine and isocryptolepine, HPLC of Formula: 146140-95-6, the publication is Tetrahedron (2005), 61(6), 1571-1577, database is CAplus.

7H-Indolo[2,3-c]quinoline has been synthesized in two steps via a new approach starting from com. available 3-bromoquinoline and 2-bromoaniline. The new methodol. consists of two consecutive palladium-catalyzed reactions: a selective Buchwald/Hartwig amination followed by an intramol. Heck-type reaction. Alternatively, the same skeleton has also been prepared via the combination of a Suzuki arylation with an intramol. nitrene insertion starting from 4-chloroquinoline and {2-[(2,2-dimethylpropanoyl)amino]phenyl}boronic acid. Selective methylation of 7H-indolo[2,3-c]quinoline yielded 5-methyl-5H-indolo[2,3-c]quinoline (isoneocryptolepine, I) which is an interesting new lead compound in the search for new antiplasmodial drugs.

Tetrahedron 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, HPLC of Formula: 146140-95-6.

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

Tapolcsanyi, Pal published the artcileSynthesis of the dibenzo[f,h]phthalazine and dibenzo[f,h]cinnoline skeleton via a Suzuki-Pd-catalyzed intramolecular arylation’ and a Suzuki-Pschorr’ approach, Computed Properties of 146140-95-6, the publication is Tetrahedron (2003), 59(31), 5919-5926, database is CAplus.

Palladium-catalyzed intramol. arylation of 2-benzyl-5-(2-bromophenyl)-4-phenylpyridazin-3(2H)-one yielded hitherto unknown 2-benzyldibenzo[f,h]phthalazin-1(2H)-one. The synthesis of this new tetracyclic pyridazinone from 2-benzyl-5-(2-aminophenyl)-4-phenylpyridazin-3(2H)-one via a Pschorr type reaction was also investigated. Similarly, the construction of 2-methyldibenzo[f,h]cinnolin-3(2H)-one from 2-methyl-5-(2-bromophenyl)-6-phenylpyridazin-3(2H)-one and 2-methyl-5-(2-aminophenyl)-6-phenylpyridazin-3(2H)-one is also reported. Removal of the N-benzyl protective group of 2-benzyl-dibenzo[f,h]phthalazin-1(2H)-one with AlCl₃ yielded unsubstituted dibenzo[f,h]phthalazin-1(2H)-one.

Tetrahedron 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 C15H10O2, Computed Properties of 146140-95-6.

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

Kaithwas, Gaurav published the artcileEffect of L. usitatissimum (flaxseed/linseed) fixed oil against distinct phases of inflammation, Product Details of C12H23N3S, the publication is ISRN Inflammation (2013), 735158/1-735158/5, 5 pp., database is CAplus and MEDLINE.

The present investigation summarizes the effect of Linum usitatissimum fixed oil against different phases of acute inflammatory reaction, namely, protein exudation, peritoneal capillary permeability and leukocyte migration. The fixed oil exhibited dose-dependent inhibition of protein exudation vascular permeability, comparable to standard aspirin. The oil also inhibited the leukocyte migration in pleural exudates in a dose-dependent manner. Production of less vasodilatory (PGE3) and chemotactic (LTB5) eicosanoids through EPA (derived from linolenic acid) metabolism could account for the above observations.

ISRN Inflammation 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, Product Details of C12H23N3S.

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

Subramanian, Bhagawat C. published the artcileThe role of the LTB₄-BLT1 axis in chemotactic gradient sensing and directed leukocyte migration, Synthetic Route of 321673-30-7, the publication is Seminars in Immunology (2017), 16-29, database is CAplus and MEDLINE.

Directed leukocyte migration is a hallmark of inflammatory immune responses. Leukotrienes are derived from arachidonic acid and represent a class of potent lipid mediators of leukocyte migration. In this review, we summarize the essential steps leading to the production of LTB₄ in leukocytes. We discuss the recent findings on the exosomal packaging and transport of LTB₄ in the context of chemotactic gradients formation and regulation of leukocyte recruitment. We also discuss the dynamic roles of the LTB₄ receptors, BLT1 and BLT2, in mediating chemotactic signaling in leukocytes and contrast them to other structurally related leukotrienes that bind to distinct GPCRs. Finally, we highlight the specific roles of the LTB₄-BLT1 axis in mediating signal-relay between chemotaxing neutrophils and its potential contribution to a wide variety of inflammatory conditions including tumor progression and metastasis, where LTB₄ is emerging as a key signaling component.

Seminars in Immunology 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 C15H14O, Synthetic Route of 321673-30-7.

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

Trecourt, Francois published the artcileSynthesis of 11H-pyrido[2,3-a]carbazoles and 6H-pyrido[3,2-b]carbazoles from bromo-8-methoxyquinolines, HPLC of Formula: 146140-95-6, the publication is Tetrahedron (1995), 51(43), 11743-50, database is CAplus.

Cross-coupling reaction via substituted 7-bromoquinolines and (2-aminophenyl)boric acids afforded substituted 7-(2-aminophenyl)quinolines. These compounds are intermediates for 11H-pyrido[2,3-a]carbazoles and 6H-pyrido[3,2-b]carbazoles.

Tetrahedron 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 C12H10F2Si, HPLC of Formula: 146140-95-6.

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

Wu, Ye published the artcileStapled Wasp Venom-Derived Oncolytic Peptides with Side Chains Induce Rapid Membrane Lysis and Prolonged Immune Responses in Melanoma, Recommanded Product: H-Lys(Boc)-OH, the publication is Journal of Medicinal Chemistry (2021), 64(9), 5802-5815, database is CAplus and MEDLINE.

Peptide stapling chem. represents an attractive strategy to promote the clin. translation of protein epitope mimetics, but its use has not been applied to natural cytotoxic peptides (NCPs) to produce new oncolytic peptides. Based on a wasp venom peptide, a series of stapled anoplin peptides (StAnos) were prepared The optimized stapled Ano-3/3s were shown to be protease-resistant and exerted superior tumor cell-selective cytotoxicity by rapid membrane disruption. In addition, Ano-3/3s induced tumor ablation in mice through the direct oncolytic effect and subsequent stimulation of immunogenic cell death. This synergistic oncolytic-immunotherapy effect is more remarkable on melanoma than on triple-neg. breast cancer in vivo. The efficacies exerted by Ano-3/3s on melanoma were further characterized by CD8+ T cell infiltration, and the addition of anti-CD8 antibodies diminished the long-term antitumor effects. In summary, these results support stapled peptide chem. as an advantageous method to enhance the NCP potency for oncolytic therapy.

Journal of 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 C15H21BO3, Recommanded Product: H-Lys(Boc)-OH.

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

Wang, Min published the artcileApolipoprotein M induces inhibition of inflammatory responses via the S1PR1 and DHCR24 pathways, Related Products of amides-buliding-blocks, the publication is Molecular Medicine Reports (2019), 19(2), 1272-1283, database is CAplus and MEDLINE.

Apolipoprotein M (ApoM) is a type of apolipoprotein. It is well known that high-d. lipoprotein (HDL) decreases inflammatory responses via the apoM-sphingosine-1-phosphate (S1P) pathway. The present study further investigated the importance of ApoM in the inhibitory effects of HDL on inflammation. Furthermore, cell culture experiments were performed using a permanent human hybrid endothelial cell line (EA.hy926). In cell culture experiments, when cells were pre-cultured with rec-apoM or were engineered to overexpress apoM (apoMTg), they exhibited decreased expression levels of IL-1beta and MCP-1 following TNF-a treatment compared with in normal apoM-expressing cells (apoMTgN) Furthermore, the mRNA expression levels of IL-1beta and MCP-1 were significantly elevated following addition of the S1PR1 inhibitor W146, but not by the scavenger receptor class B type I inhibitor, block lipid transport-1 (BLT-1), in apoMTg cells prior to TNF-a treatment. Conversely, there were no differences in these inflammatory biomarkers under the same conditions in apoMTgN cells. The mRNA expression levels of DHCR24 were significantly reduced by the addition of BLT-1 prior to TNF-a treatment in apoMTg cells; however, there was no difference in the expression of this inflammatory biomarker in apoMTgN cells. In conclusion, ApoM displayed inhibitory effects against the inflammatory response in vivo and in vitro; these effects may be induced via the S1PR1 and DHCR24 pathways.

Molecular Medicine 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 C8H8O3, Related Products of amides-buliding-blocks.

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

Yu, Renchao published the artcileBaicalin promotes cholesterol efflux by regulating the expression of SR-BI in macrophages, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Experimental and Therapeutic Medicine (2016), 12(6), 4113-4120, database is CAplus and MEDLINE.

Intake of a high dosage of baicalin has previously been shown to attenuate hyperlipidemia induced by a high-fat diet. Baicalin functions as an activator of peroxisome proliferator-activated receptor-γ (PPAR-γ), which is the key regulator of reverse cholesterol transport (RCT). The present study aimed to test the hypothesis that baicalin could promote cholesterol efflux in macrophages through activating PPAR-γ. Phorbol 12-myristate 13-acetate-stimulated THP-1 cells were treated with oxidized low-d. lipoprotein and (3H)-cholesterol for 24 h, and the effects of baicalin on cholesterol efflux were evaluated in the presence of apolipoprotein A-1 (ApoA-1), or high-d. lipoprotein subfraction 2 (HDL2) or subfraction 3 (HDL3). The expression levels of scavenger receptor class B type I (SR-BI), PPAR-γ and liver X receptor-α (LXRα) were detected and specific inhibitors or activators of SR-BI, PPAR-γ and LXRα were applied to investigate the mechanism. Treatment of THP-1 macrophages with baicalin significantly accelerated HDL-mediated, but not ApoA-1-mediated cholesterol efflux. However, baicalin treatment increased the expression of SR-BI at the mRNA and protein levels in a dose- and time-dependent manner, and pre-treatment with the SR-BI inhibitor BLT-1 and SR-BI small interfering RNA significantly inhibited baicalin-induced cholesterol efflux. Furthermore, baicalin increased the expression of PPAR-γ and LXRα, and the application of specific agonists and inhibitors of PPAR-γ and LXRα changed the expression of SR-BI, as well as cholesterol efflux. It may be concluded that baicalin induced cholesterol efflux from THP-1 macrophages via the PPAR-γ/LXRα/SR-BI pathway.

Experimental and Therapeutic Medicine 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 C20H21ClN4O4, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea.

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

Watanabe, Masaki published the artcileA turn on and a turn off: BLT1 and BLT2 mechanisms in the lung, Related Products of amides-buliding-blocks, the publication is Expert Review of Respiratory Medicine (2014), 8(4), 381-383, database is CAplus and MEDLINE.

A review. Leukotriene B₄ (LTB₄), a potent lipid mediator of inflammation derived from arachidonic acid through the action of 5-lipoxygenase, has been implicated in the pathophysiol. of several inflammatory diseases, including asthma and chronic obstructive pulmonary disease. A high-affinity LTB₄ receptor BLT1 has been shown to exert proinflammatory roles. A cyclooxygenase metabolite, 12(S)-hydroxyheptadeca-5Z, 8E, 10E-trienoic acid (12-HHT), is an endogenous ligand for BLT2, a low-affinity LTB₄ receptor. The recent study indicated that BLT2 has a protective role in allergic airway inflammation, suggesting different functions between BLT1 and BLT2 in the pathogenesis of asthma. Selective BLT1 antagonists may have a potential therapeutic application in patients with asthma, and BLT2 may represent a novel therapeutic target for lung diseases.

Expert Review of Respiratory Medicine 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 C8H5F3N4, Related Products of amides-buliding-blocks.

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