Category: amides-buliding-blocks

Csanyi, D. published the artcileAn alternative synthesis of quindoline and one of its closely related derivatives, Quality Control of 146140-95-6, the publication is Synthetic Communications (1999), 29(22), 3959-3969, database is CAplus.

The alkaloid quindoline and its tetracyclic isomer indazolo[2,3-a]quinoline have been synthesized utilizing the Pd(0)-catalyzed cross-coupling reaction of pivaloylaminophenylboronic acid with substituted quinolines.

Synthetic Communications 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

Walczynski, K. published the artcileHistamine H₁ receptor ligands. Part I. Novel thiazol-4-ylethanamine derivatives: synthesis and in vitro pharmacology, Recommanded Product: 3-Methoxybenzothioamide, the publication is Farmaco (1999), 54(8), 533-541, database is CAplus and MEDLINE.

A series of 2-substituted thiazol-4-ylethanamines have been synthesized and tested for their histaminergic H₁-receptor activities. The compounds with 2-Ph substitution, regardless of the different physicochem. properties of the meta-substituents at the Ph ring, showed weak H₁-agonistic activity with pD₂ values ranging from 4.35 to 5.36. When the Ph group was replaced by a benzyl group, the resulting compounds all exhibited weak H₁-antagonistic activity (pA₂: 4.14-4.82).

Farmaco published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C10H9NO4S, Recommanded Product: 3-Methoxybenzothioamide.

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

Orr, David published the artcileSingle-Step Microwave-Mediated Syntheses of Oxazoles and Thiazoles from 3-Oxetanone: A Synthetic and Computational Study, Recommanded Product: 3-Methoxybenzothioamide, the publication is Chemistry – A European Journal (2013), 19(29), 9655-9662, database is CAplus and MEDLINE.

The direct microwave-mediated condensation between 3-oxetanone and primary amides and thioamides has delivered moderate to good yields of (hydroxymethyl)oxazoles and (hydroxymethyl)thiazoles. The reactions use a sustainable solvent and only require short reaction times. These are highly competitive methods for the construction of two classes of valuable heteroarenes, which bear a useful locus for further elaboration. Electronic structure calculations have shown that the order of events involves chalcogen atom attack at sp³ carbon and alkyl-oxygen cleavage. The critical role of acid catalysis was shown clearly, and the importance of acid strength was demonstrated. The calculated barriers were also fully consistent with the observed order of thioamide and amide reactivity. Spontaneous ring opening involves a modest degree of C-O cleavage, moderating the extent of strain relief. On the acid-catalyzed pathway, C-O cleavage is less extensive still, but proton transfer to the nucleofuge is well advanced with the carboxylic acid catalysts, and essentially complete with methanesulfonic acid.

Chemistry – A European Journal published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C8H9NOS, Recommanded Product: 3-Methoxybenzothioamide.

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

Bianchini, Gianluca published the artcileDiscovery of Novel TRPM8 Blockers Suitable for the Treatment of Somatic and Ocular Painful Conditions: A Journey through pK_a and LogD Modulation, Name: 3-Methoxybenzothioamide, the publication is Journal of Medicinal Chemistry (2021), 64(22), 16820-16837, database is CAplus and MEDLINE.

Transient receptor potential melastatin 8 (TRPM8) is crucially involved in pain modulation and perception, and TRPM8 antagonists have been proposed as potential therapeutic approaches for pain treatment. Previously, we developed two TRPM8 antagonists and proposed them as drug candidates for topical and systemic pain treatment. Here, we describe the design and synthesis of these two TRPM8 antagonists (27 (I) and 45 (II)) and the rational approach of modulation/replacement of bioisosteric chem. groups, which allowed us to identify a combination of narrow ranges of pK_a and LogD values that were crucial to ultimately optimize their potency and metabolic stability. Following the same approach, we then pursued the development of new TRPM8 antagonists suitable for the topical treatment of ocular painful conditions and identified two new compounds (51 (III) and 59 (IV)), N-alkoxy amide derivatives, that can permeate across ocular tissue and reduce the behavioral responses induced by the topical ocular menthol challenge in vivo.

Journal of Medicinal Chemistry published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C8H9NOS, Name: 3-Methoxybenzothioamide.

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

Wang, Duo-Zhi published the artcileBis[μ-N-(1,3,4-thiadiazol-2-yl)pyridine-3-carboxamide-κ²N¹,N³]disilver(I) bis(perchlorate), Quality Control of 51987-99-6, the publication is Acta Crystallographica, Section E: Structure Reports Online (2007), 63(5), m1294-m1296, database is CAplus.

In the title compound, [Ag₂(C₈H₆N₄OS)₂](ClO₄)₂, each Ag^I center in the centrosym. dinuclear complex cation is coordinated by one pyridine N and a thiadiazole N atom of two inversion-related N-(1,3,4-thiadiazol-2-yl)pyridine-3-carboxamide ligands in an almost linear geometry [Ag-N = 2.187(3) and 2.172(3) Å, and N-Ag-N = 171.8(1)°]. Weak Ag···Ag and Ag-perchlorate interactions, together with π-π stacking interactions, link the complex cations along the a axis to form a ribbon. Crystallog. data are given.

Acta Crystallographica, Section E: Structure Reports Online 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 C10H14N2O, Quality Control of 51987-99-6.

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

Hang, Zhaojun published the artcileA practical method for N-cyanation of secondary amines and sulfonamides, Application In Synthesis of 2451-91-4, the publication is Tetrahedron Letters (2022), 153564, database is CAplus.

Cyanamides are an important class of mols. This work describes a facile synthesis of disubstituted cyanamides. Here, readily accessible 1-cyano-1,2-benziodoxol-3-(1H)-one (CBX) was applied as a stable electrophilic cyanation reagent. Diverse secondary amines were effectively cyanated. Moreover, secondary sulfonamides proved to be suitable substrates and were readily converted to N-alkyl(aryl)-N-arylsulfonyl-cyanamides, as the significant building blocks of the organic transformation.

Tetrahedron Letters 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

Horley, D. published the artcileThe infrared spectra of some titanium(IV) complexes with primary diamines, Recommanded Product: 2,4-Dichlorobenzamide, the publication is Canadian Journal of Chemistry (1965), 43(12), 3201-5, database is CAplus.

A series of Ti(IV) halide-diamine complexes was prepared and their ir spectra measured in the solid state, 300-4000 cm.^-1 The configuration of the ligand and extent of aminolysis of the Ti-halide bond are discussed in relation to the spectra. Some assignments are proposed in the 300-600-cm.^-1 region for the ethylenediamine complexes.

Canadian Journal of 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, Recommanded Product: 2,4-Dichlorobenzamide.

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

Fischer, Helmut published the artcileCoupling of cyanamides with a carbyne ligand – formation of η²-(C,N)-imidazolium complexes and ansa-carbene complexes, Application In Synthesis of 2451-91-4, the publication is Chemische Berichte (1993), 126(11), 2373-8, database is CAplus.

Dicarbonyl(cyclopentadienyl)(phenylcarbyne)manganese complexes [Cp(CO)₂MnCPh]⁺X^– (1–X) (X = BF₄, BCl₄) react with dimethyl-(2a), diethyl-(2b), and diisopropylcyanamide (2c) in five-fold excess by a head-to-tail cyclization of two cyanamides with the carbyne ligand to give η²-(C,N)-imidazolium complexes I. As byproducts ansa-amino(alkylideneamino)carbene complexes II are formed in which a N:C(Ph) group bridges the carbene carbon and the Cp ring. With increasing excess of the cyanamide the product ratio I:II increases. Among the products of the reaction of 1–X with the cyanamides NCNR₂ [NR₂ = N(isobutyl)₂, N(Bzl)₂, N(Me)Ph] no imidazolium complexes I are detected, only ansa-carbene complexes II are isolated. PMe₃/H₂O or pyridine/H₂O displaces the heterocyclic ligand from I (R = Me, X = BF₄). The structure of I (R = Me, X = BF₄) is established by an x-ray anal.

Chemische Berichte 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

Huber, Vincent J. published the artcileIdentification of Aquaporin 4 inhibitors using in vitro and in silico methods, Formula: C8H6N4OS, the publication is Bioorganic & Medicinal Chemistry (2009), 17(1), 411-417, database is CAplus and MEDLINE.

The in vitro inhibitory effects and in silico docking energies of 18 compounds with respect to Aquaporin 4 (AQP4) were investigated. More than half of the compounds tested showed inhibitory activity in the in vitro functional assay and included the 5-HT_1B/1D agonists sumatriptan, and rizatriptan. Moreover, the observed inhibitory activity of the compounds used in this study at 20 μM showed a strong correlation with their in silico docking energies, r ² = 0.64, which was consistent with that found in previous studies. The AQP4 inhibitory IC₅₀ values of three compounds, 2-(nicotinamido)-1,3,4-thiadiazole, sumatriptan and rizatriptan, were subsequently found to be 3, 11, and 2 μM, resp.

Bioorganic & Medicinal Chemistry 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 C8H6N4OS, Formula: C8H6N4OS.

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

Anabuki, Tomoaki published the artcileNovel biotin linker with alkyne and amino groups for chemical labelling of a target protein of a bioactive small molecule, SDS of cas: 2418-95-3, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(4), 783-786, database is CAplus and MEDLINE.

We synthesized a novel linker (I) with biotin, alkyne and amino groups for the identification of target proteins using a small mol. that contains an azide group (azide probe). The alkyne in the linker bound the azide probe via an azide-alkyne Huisgen cycloaddition A protein cross-linker effectively bound the conjugate of the linker and an azide probe with a target protein. The covalently bound complex was detected by western blotting. Linker I was applied to a model system using an abscisic acid receptor, RCAR/PYR/PYL (PYL). Cross-linked complexes of linker I, the azide probes and the target proteins were successfully visualized by western blotting. This method of target protein identification was more effective than a previously developed method that uses a second linker with biotin, alkyne, and benzophenone (linker II) that acts to photo-crosslink target proteins. The system developed in this study is a method for identifying the target proteins of small bioactive mols. and is different from photo-affinity labeling.

Bioorganic & Medicinal Chemistry Letters 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, SDS of cas: 2418-95-3.

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