Tag: M.W=200-250

Horvath, Daniel Vajk published the artcileRegioexhaustive Functionalization of the Carbocyclic Core of Isoquinoline: Concise Synthesis of Oxoaporphine Core and Ellipticine, Formula: C11H16BNO3, the publication is Synthesis (2018), 50(11), 2181-2190, database is CAplus.

A general and versatile strategy has been developed for the functionalization of the carbocyclic core of the isoquinoline. This regioexhaustive approach employs electrophilic halogenation as a toolbox methodol. and delivers highly decorated intermediates that can be further elaborated toward medicinally relevant building blocks or natural products.

Synthesis 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, Formula: C11H16BNO3.

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

Pernet, Erwan published the artcileLeukotriene B₄-type I interferon axis regulates macrophage-mediated disease tolerance to influenza infection, Quality Control of 321673-30-7, the publication is Nature Microbiology (2019), 4(8), 1389-1400, database is CAplus and MEDLINE.

Host defense against influenza A virus (IAV) infection depends not only on host resistance to eliminate the virus, but also disease tolerance to limit lung tissue damage and maintain pulmonary function. Fatal IAV infections are frequently the result of a maladaptive immune response that compromises disease tolerance rather than host resistance to infection. Here, we show that the leukotriene B₄ (LTB₄)-type I interferon (IFN) axis promotes a distinct mechanism of disease tolerance to pulmonary IAV infection. We demonstrate that mice genetically deficient in LTB₄ signalling (Blt1R^-/-) are more susceptible to IAV infection compared to control mice, despite similar pulmonary viral loads. The increased susceptibility of Blt1R^-/- mice is associated with an accumulation of inflammatory monocyte-derived macrophages (IMMs) causing increased lung immunopathol. We mechanistically define that LTB₄ signalling via the BLT1 receptor enhances the activation of the type I IFN-α/β receptor (IFNAR)/ and signal transducer and activator of transcription 1 (STAT1), which leads to IFN-α production by interstitial macrophages to suppresse in situ IMM proliferation. Importantly, the delivery of a single dose of LTB₄ at the peak viral load reduces IMM proliferation, controls tissue damage and increases survival without affecting host resistance to IAV.

Nature Microbiology 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, Quality Control of 321673-30-7.

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

Shcherbakov, Nikolay V. published the artcileHetero-Tetradehydro-Diels-Alder Cycloaddition of Enynamides and Cyanamides: Gold-Catalyzed Generation of Diversely Substituted 2,6-Diaminopyridines, Synthetic Route of 2451-91-4, the publication is Journal of Organic Chemistry (2021), 86(10), 7218-7228, database is CAplus and MEDLINE.

The reaction proceeds under very mild conditions (DCM, rt) with high functional group tolerance. The obtained 2,6-diaminopyridines I and II represent a useful synthetic platform with an easily modulated substitution pattern for subsequent functionalizations of both the pyridine core and the N-substituents. Gold(I)-catalyzed hetero-tetradehydro-Diels-Alder cycloaddition of enynamides R¹CH=C(R²)CCN(R³)R⁴ [R¹ = C₆H₅, 2-thienyl, 1-naphthyl, etc.; R² = H, Me; R³ = Me, Ph, Bn, Ts; R⁴ = 4-MeC₆H₄S(O)₂, MeS(O)₂, 4-FC₆H₄S(O)₂, CH₂CH=CH₂, 2-(2H-1,3-benzodioxol-5-yl)ethyl; R³R⁴ = -C(O)O(CH₂)₂-] and cyanamides R⁵R⁶NCN (R⁵ = Me, Et, Bn, Ph; R⁶ = Me, Et, Bn, Ph; R⁵R⁶ = -(CH₂)₄-, -(CH₂)₅-, -(CH₂)₂O(CH₂)₂-) and 3,4-dihydro-2(1H)-Isoquinolinecarbonitrile comprises an efficient route to diversely substituted 2,6-diaminopyridines I and II (yields up to 99%).

Journal of Organic Chemistry 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 C18H24N6O6S4, Synthetic Route of 2451-91-4.

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

Sahoo, Daisy published the artcileScavenger receptor class B Type I (SR-BI) assembles into detergent-sensitive dimers and tetramers, Name: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Biochimica et Biophysica Acta, Molecular and Cell Biology of Lipids (2007), 1771(7), 807-817, database is CAplus and MEDLINE.

High d. lipoproteins (HDL) are protective against cardiovascular disease due to their important role in the reverse cholesterol transport (RCT) pathway. The selective transfer of cholesteryl ester (CE) from the HDL core to cells, the last step in RCT, is mediated by scavenger receptor class B type I (SR-BI). SR-BI is a heavily glycosylated cell surface receptor that is highly expressed in the liver, ovaries, testes and adrenal glands, where selective uptake of HDL-CE is most prevalent. Previous studies have shown that SR-BI oligomerizes with itself in steroidogenic tissues as well as in diverse cell lines. In the present study, we provide further evidence for the homo-oligomerization of SR-BI. We show by FPLC and blue native PAGE that SR-BI forms complexes whose sizes suggest the formation of monomers, dimers, and tetramers. Interestingly, homo-oligomerization occurs even with the absence of SR-BI’s C-terminal cytoplasmic domain. Finally, we report that an inhibitor of SR-BI-mediated cholesterol transport, BLT-1, and mutations in the putative leucine zipper region of SR-BI have profound effects on SR-BI function, however, they do not affect receptor self-association These observations indicate that SR-BI homo-oligomerization occurs even when the receptor is non-functional.

Biochimica et Biophysica Acta, Molecular and Cell Biology of Lipids 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, Name: [(2-Hexylcyclopentylidene)amino]thiourea.

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

Kheradmand, Farrah published the artcileLeukotriene A₄ hydrolase: the janus enzyme shows its ugly side in smokers, Synthetic Route of 321673-30-7, the publication is American Journal of Respiratory and Critical Care Medicine (2014), 190(1), 5-7, database is CAplus and MEDLINE.

This paper describes the cigarette smoke chem. acetylates proline-glycine-proline, enhancing its chemotactic activity and protecting it from degradation by LTA4H. And also biochem. and preliminary murine studies suggest that cigarette smoke can selectively abrogate the peptidase activity of LTA4H, with minimal effect on the hydrolase activity.

American Journal of Respiratory and Critical Care 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 C12H23N3S, Synthetic Route of 321673-30-7.

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

Appukkuttan, Prasad published the artcileMicrowave-assisted transition-metal-catalyzed synthesis of N-shifted and ring-expanded buflavine analogues, Formula: C11H16BNO3, the publication is Chemistry – A European Journal (2007), 13(22), 6452-6460, database is CAplus and MEDLINE.

Buflavine analogs I (R = H, MeO) and II (R = H, MeO) are prepared using microwave-assisted Suzuki-Miyaura coupling reactions and ring-closing metathesis reactions as key steps. Suzuki-Miyaura coupling of the bromostyrenes III (R = H, MeO) with an (allyl)(pivaloyl)aminoboronic acid provides a biaryl which undergoes selective ring-closing metathesis in the presence of either the first or the second-generation Grubbs catalysts followed by olefin hydrogenation to yield I (R = H, MeO); attempted reduction of a related vinylnitrostyrene gives inseparable mixtures of the desired biphenylamines along with phenanthridines generated by reductive cyclization. Suzuki-Miyaura coupling of III (R = H, MeO) with 2-formylbenzeneboronic acid, reductive amination with allylamine followed by reductive methylation of the amines, ring-closing metathesis with the second-generation Grubbs catalyst, and olefin hydrogenation provides II (R = H, MeO).

Chemistry – A European Journal 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, Formula: C11H16BNO3.

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

Appukkuttan, Prasad published the artcileMicrowave-Enhanced Synthesis of N-Shifted Buflavine Analogues via a Suzuki-Ring-Closing Metathesis Protocol, Related Products of amides-buliding-blocks, the publication is Organic Letters (2005), 7(13), 2723-2726, database is CAplus and MEDLINE.

A novel, microwave-enhanced six-step synthesis was devised for the synthesis of N-shifted buflavine analogs, I (R = H, OMe). Microwave-enhanced Suzuki-Miyaura cross-coupling and ring-closing metathesis reactions were used as the key steps. Microwave irradiation was found to enhance the ring-closing metathesis reaction to generate the otherwise difficultly obtainable medium-sized ring system of the target mols.

Organic 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, Related Products of amides-buliding-blocks.

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

Pudlo, Marc published the artcileFirst Suzuki-Miyaura type cross-coupling of ortho-azidobromobenzene with arylboronic acids and its application to the synthesis of fused aromatic indole-heterocycles, HPLC of Formula: 146140-95-6, the publication is Tetrahedron (2007), 63(41), 10320-10329, database is CAplus.

A short synthesis of some fused indole-heterocycles, e.g., I (R = H, CN or CHO), has been achieved via Pd-catalyzed cross-coupling reactions between azido-2-bromobenzene and arylboronic acids and subsequent thermally induced nitrene insertion. Addnl., 4-amino-α-carboline, a versatile intermediate toward grossularine analogs has also been prepared by Suzuki-Miyaura cross-coupling of 4-pivaloylaminopyridine-3-boronic acid with 2-bromoaniline, followed by simple functional group transformations.

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

Mancha, Gisela published the artcileEfficient synthesis of racemic and chiral alkenyl sulfoxides by palladium-catalyzed Suzuki coupling, Product Details of C11H16BNO3, the publication is Tetrahedron (2010), 66(34), 6901-6905, database is CAplus.

Alkenyl sulfoxide derivatives are obtained in high yields through a palladium-catalyzed Suzuki/Miyaura cross-coupling reaction of racemic and chiral 1-halo sulfoxides with aryl and alkenyl boronic acids. Chiral substrates react with no loss of optical purity and high optical yields. The reaction takes place with different palladium catalysts, such as Pd(PPh₃)₄ or Pd(OAc)₂/DABCO. Although nitrogen ligands like DABCO lead to an active palladium catalyst, they are less effective than the phosphine ones.

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, Product Details of C11H16BNO3.

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

Morgan, Charles W. published the artcileSelective CRAF Inhibition Elicits Transactivation, Product Details of C11H22N2O4, the publication is Journal of the American Chemical Society (2021), 143(12), 4600-4606, database is CAplus and MEDLINE.

Discovering mols. that regulate closely related protein isoforms is challenging, and in many cases the consequences of isoform-specific pharmacol. regulation remains unknown. RAF isoforms are commonly mutated oncogenes that serve as effector kinases in MAP kinase signaling. BRAF/CRAF heterodimers are believed to be the primary RAF signaling species, and many RAF inhibitors lead to a “paradoxical activation” of RAF kinase activity through transactivation of the CRAF protomer; this leads to resistance mechanisms and secondary tumors. It has been hypothesized that CRAF-selective inhibition might bypass paradoxical activation, but no CRAF-selective inhibitor has been reported and the consequences of pharmacol. inhibiting CRAF have remained unknown. Here, we use bio-orthogonal ligand tethering (BOLT) to selectively target inhibitors to CRAF. Our results suggest that selective CRAF inhibition promotes paradoxical activation and exemplify how BOLT may be used to triage potential targets for drug discovery before any target-selective small mols. are known.

Journal of the American Chemical Society 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 C11H22N2O4, Product Details of C11H22N2O4.

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