Tag: M.W=200-250

Andreichikov, Yu. S. published the artcileChemistry of oxalyl derivatives of methyl ketones. XXXVIII. [4_π + 2_π]-Cycloaddition of aroylketenes at the CN bond of N-cyanoamines and phenyl cyanate, Application of N,N-Dibenzylcyanamide, the publication is Zhurnal Organicheskoi Khimii (1984), 20(8), 1755-9, database is CAplus.

Heating furandiones I, R = H, Me, Cl, EtO, Br, MeO) gave intermediate Ketenes p-RC₆H₄COCH:CO which cyclize with R¹CN to give oxazinones II (R² = R³ = Et, allyl, Bu, PhCH₂; R² = Me, R³ = Ph), III and IV. Reaction of I (R = H) with o-ClC₆H₄NHCN gave oxazolidinone V.

Zhurnal Organicheskoi Khimii 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 of N,N-Dibenzylcyanamide.

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

Riedl, Zsuzsanna published the artcileSynthesis of novel 1-methyl-1H-pyridazino[3,4-b]indoles, Quality Control of 146140-95-6, the publication is Tetrahedron (2006), 62(1), 121-129, database is CAplus.

New synthetic pathways have been elaborated to 1-methyl-1H-pyridazino[3,4-b]indoles starting from halopyridazin-3(2H)-ones. Suzuki cross-coupling reaction of chloro, iodo, dichloro, and dibromo substituted pyridazin-3(2H)-ones with 2-pivaloylaminophenylboronic acid followed by hydrolysis of the amide and subsequent ring closure via condensation gave fused indoles. Some of these compounds showed biol. activity as antitrypanosomal agents.

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, Quality Control of 146140-95-6.

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

Nakahara, Shinsuke published the artcileSynthesis of neoamphimedine, Recommanded Product: (2-Pivalamidophenyl)boronic acid, the publication is Heterocycles (2012), 85(4), 933-940, database is CAplus.

The synthesis of neoamphimedine {(I), from Xestospongia sp.}, which is a potent antitumor agent both in vitro and in vivo, also can induce topoisomerase II-mediated catenation of plasmid DNA in vitro. The synthesis was achieved in twelve steps from 2,5-dimethoxyphenethylamine in 6% overall yield.

Heterocycles 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, Recommanded Product: (2-Pivalamidophenyl)boronic acid.

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

Chignen Possi, Kelvine published the artcileInfluences of histidine-1 and azaphenylalanine-4 on the affinity, anti-inflammatory, and antiangiogenic activities of azapeptide cluster of differentiation 36 receptor modulators, Application of H-Lys(Boc)-OH, the publication is Journal of Medicinal Chemistry (2017), 60(22), 9263-9274, database is CAplus and MEDLINE.

Azapeptide analogs of growth hormone releasing peptide-6 (GHRP-6) exhibit promising affinity, selectivity, and modulator activity on the cluster of differentiation 36 receptor (CD36). For example, [A¹, azaF⁴] and [azaY⁴]-GHRP-6 were previously shown to bind selectively to CD36 and exhibited resp. significant antiangiogenic and slight angiogenic activities in a microvascular sprouting assay using choroid explants. The influences of the 1- and 4-position residues on the affinity, anti-inflammatory, and antiangiogenic activity of these azapeptides have now been studied in detail by the synthesis and anal. of a set of 25 analogs featuring Ala¹ or His¹ and a variety of aromatic side chains at the aza-amino acid residue in the 4-position. Although their binding affinities differed only by a factor of 17, the analogs exhibited significant differences in ability to modulate production of nitric oxide (NO) in macrophages and choroidal neovascularization.

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 C11H22N2O4, Application of H-Lys(Boc)-OH.

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

Suzuki, Tateki published the artcileCrystal structures reveal an elusive functional domain of pyrrolysyl-tRNA synthetase, HPLC of Formula: 2418-95-3, the publication is Nature Chemical Biology (2017), 13(12), 1261-1266, database is CAplus and MEDLINE.

Pyrrolysyl-tRNA synthetase (PylRS) is a major tool in genetic code expansion using noncanonical amino acids, yet its structure and function are not completely understood. Here, we describe the crystal structure of the previously uncharacterized essential N-terminal domain of this unique enzyme from Methanosarcina mazei in complex with tRNA^Pyl. This structure explains why PylRS remains orthogonal in a broad range of organisms, from bacteria to humans. The structure also illustrates why tRNA^Pyl recognition by PylRS is anticodon-independent; the anticodon does not contact the enzyme. Then, using standard microbiol. culture equipment, we established a new method for laboratory evolution, PANCE, a noncontinuous counterpart of previously developed phage-assisted continuous evolution (PACE). With this method, we evolved novel PylRS variants with enhanced activity and amino acid specificity. Finally, we employed an evolved PylRS variant to determine its N-terminal domain structure and showed how its mutations improved PylRS activity in the genetic encoding of N^ε-(tert-butoxycarbonyl)-L-lysine (BocK), a noncanonical amino acid.

Nature Chemical Biology 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 C5H10N2OS, HPLC of Formula: 2418-95-3.

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

Nodling, Alexander R. published the artcileCyanine dye mediated mitochondrial targeting enhances the anti-cancer activity of small-molecule cargoes, Related Products of amides-buliding-blocks, the publication is Chemical Communications (Cambridge, United Kingdom) (2020), 56(34), 4672-4675, database is CAplus and MEDLINE.

Organelle-specific delivery systems are of significant clin. interest. The authors demonstrate the use of common cyanine dyes Cy3 and Cy5 as vectors for targeting and delivering cargoes to mitochondria in cancer cells. Specifically, conjugation to the dyes can increase cytotoxicity by up to 1000-fold.

Chemical Communications (Cambridge, United Kingdom) 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, Related Products of amides-buliding-blocks.

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

Aizpurua, Jesus M. published the artcileDiscovery of a novel family of FKBP12 “reshapers” and their use as calcium modulators in skeletal muscle under nitro-oxidative stress, Product Details of C11H22N2O4, the publication is European Journal of Medicinal Chemistry (2021), 113160, database is CAplus and MEDLINE.

The hypothesis of rescuing FKBP12/RyR1 interaction and intracellular calcium homeostasis through mol. “reshaping” of FKBP12 was investigated. To this end, novel 4-arylthioalkyl-1-carboxyalkyl-1,2,3-triazoles were designed and synthesized, and their efficacy was tested in human myotubes. A library of 17 compounds (10a-n) designed to dock the FKBP12/RyR1 hot-spot interface contact residues, was readily prepared from free α-amino acids and arylthioalkynes using CuAAC “click” protocols amenable to one-pot transformations in high overall yields and total configurational integrity. To model nitro-oxidative stress, human myotubes were treated with the peroxynitrite donor SIN1, and evidence was found that some triazoles 10 were able to normalize calcium levels, as well as FKBP12/RyR1 interaction. For example, compound 10 b at 150 nM rescued 46% of FKBP12/RyR1 interaction and up to 70% of resting cytosolic calcium levels in human myotubes under nitro-oxidative stress. All compounds 10 analyzed showed target engagement to FKBP12 and low levels of cytotoxicity in vitro. Compounds 10b, 10c, 10h, and 10iR were identified as potential therapeutic candidates to protect myotubes in muscle disorders with underlying nitro-oxidative stress, FKBP12/RyR1 dysfunction and calcium dysregulation.

European 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 C11H22N2O4, Product Details of C11H22N2O4.

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

Miyabe, Yoshishige published the artcileLTB₄ and BLT1 in inflammatory arthritis, Application of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Seminars in Immunology (2017), 52-57, database is CAplus and MEDLINE.

Inflammatory arthritis, including rheumatoid arthritis (RA), is characterized by infiltration of inflammatory cells into the joints. Biol. agents targeting TNF-α and IL-6 dramatically improve RA. However, some RA patients do not respond to current treatments and these broadly active upstream biol. agents increase the risk of severe infection. Therefore, there remains a need for other effective and safe treatments for RA. Many studies have implicated that blockade of leukotriene B4 (LTB₄) and its high affinity receptor BLT1 dramatically suppress arthritis in animal models. In addition, levels of LTB₄ in serum, synovial fluid and synovial tissue are increased in RA patients compared to healthy donors or osteoarthritis patients. These data suggest that LTB₄ and BLT1 likely contribute to the pathogenesis of human RA. However, several clin. trials inhibiting BLT1 in RA were not successful. Our recent data revealed that LTB₄ is a key mediator in a complement, lipid, cytokine and chemokine cascade that first initiates and then sustains neutrophilic inflammation in inflammatory arthritis. These new mechanistic studies suggest novel ways to target the LTB₄-BLT1 pathway for the treatment of RA and other inflammatory diseases.

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 C12H23N3S, Application of [(2-Hexylcyclopentylidene)amino]thiourea.

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

Rebstock, Anne-Sophie published the artcileSynthesis and deprotonation of 2-(pyridyl)phenols and 2-(pyridyl)anilines, SDS of cas: 146140-95-6, the publication is Organic & Biomolecular Chemistry (2003), 1(17), 3064-3068, database is CAplus and MEDLINE.

2-(2- And 3-Pyridyl)anilines, 2,2-dimethyl-N-[2-(2- and 3-pyridyl)phenyl]propanamides, and 2-, 3- and 4-(2-methoxyphenyl)pyridines are readily synthesized using cross-coupling reactions. Whereas 2-(3-pyridinyl)benzenamine and 2-(2-pyridinyl)benzenamine undergo side reactions, the corresponding 2,2-dimethyl-N-[2-(2-pyridinyl)phenyl]propanamide and 2,2-dimethyl-N-[2-(3-pyridinyl)phenyl]propanamide (amides) are deprotonated with lithium 2,2,6,6-tetramethylpiperidide. When 2-(2-methoxyphenyl)pyridine (ether) is subjected to the same reagent, lithiation occurs at C6′.

Organic & Biomolecular Chemistry 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, SDS of cas: 146140-95-6.

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

Trecourt, Francois published the artcileSynthesis of 7H-pyrido[2,3-c]carbazoles from 5-bromo-8-methoxyquinolines via coupling and azide cyclization reactions, Quality Control of 146140-95-6, the publication is Journal of Heterocyclic Chemistry (1995), 32(4), 1261-7, database is CAplus.

A new strategy for the synthesis of substituted 7H-pyrido[2,3-c]carbazoles has been developed from substituted 5-bromoquinolines by using cross-coupling reaction with (2-aminophenyl)boric acids, followed by a regioselective azide cyclization.

Journal of Heterocyclic Chemistry 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 C8H15ClN2, Quality Control of 146140-95-6.

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