Category: amides-buliding-blocks

Rajappa, S. published the artcileA general synthesis of thiazoles. Part 5. Synthesis of 5-acyl-2-dialkylaminothiazoles, Product Details of C5H10N2OS, the publication is Proceedings – Indian Academy of Sciences, Chemical Sciences (1982), 91(5), 445-50, database is CAplus.

The title compounds I [R = morpholino, R¹ = H, R² = Ph, EtO, Me, 4,3-Cl(O₂N)C₆H₄; R = 4-methylpiperazine, R¹ = H, R² = 4-O₂NC₆H₄, 3-O₂NC₆H₄, 4,3-Cl(O₂N)C₆H₄; R = 4-methylpiperazino, R¹ = Me, R² = 3-O₂NC₆H₄] were prepared by cyclization of RCSN:CR¹NMe₂ with R²COCH₂X (X = Cl, Br).

Proceedings – Indian Academy of Sciences, Chemical Sciences published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, Product Details of C5H10N2OS.

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

Monty, Olivier B. C. published the artcileSolution-phase fmoc-based peptide synthesis for DNA-encoded chemical libraries: Reaction conditions, protecting group strategies, and pitfalls, Recommanded Product: H-Lys(Boc)-OH, the publication is ACS Combinatorial Science (2020), 22(12), 833-843, database is CAplus and MEDLINE.

Peptide drug discovery has shown a resurgence since 2000, bringing 28 non-insulin therapeutics to the market compared to 56 since its first peptide drug, insulin, in 1923. While the main method of discovery has been biol. display-phage, mRNA, and ribosome-the synthetic limitations of biol. systems has restricted the depth of exploration of peptide chem. space. In contrast, DNA-encoded chem. offers the synergy of large numbers and ribosome-independent synthetic flexibility for the fast and deeper exploration of the same space. Hence, as a bridge to building DNA-encoded chem. libraries (DECLs) of peptides, we have developed substrate-tolerant amide coupling reaction conditions for amino acid monomers, performed a coupling screen to illustrate such tolerance, developed protecting group strategies for relevant amino acids and reported the limitations thereof, developed a strategy for the coupling of α,α-disubstituted alkenyl amino acids relevant to all-hydrocarbon stapled peptide drug discovery, developed reaction conditions for the coupling of tripeptides likely to be used in DECL builds, and synthesized a fully deprotected DNA-decamer conjugate to illustrate the potency of the developed methodol. for on-DNA peptide synthesis.

ACS Combinatorial Science 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, Recommanded Product: H-Lys(Boc)-OH.

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

Wilking, Melissa J. published the artcileSIRT1 deacetylase is overexpressed in human melanoma and its small molecule inhibition imparts anti-proliferative response via p53 activation, SDS of cas: 380315-80-0, the publication is Archives of Biochemistry and Biophysics (2014), 94-100, database is CAplus and MEDLINE.

Melanoma causes more deaths than any other skin cancer, and its incidence in the US continues to rise. Current medical therapies are insufficient to control this deadly neoplasm, necessitating the development of new target-based approaches. The objective of this study was to determine the role and functional significance of the class III histone deacetylase SIRT1 in melanoma. We have found that SIRT1 is overexpressed in clin. human melanoma tissues and human melanoma cell lines (Sk-Mel-2, WM35, G361, A375, and Hs294T) compared to normal skin and normal melanocytes, resp. In addition, treatment of melanoma cell lines A375, Hs294T, and G361 with Tenovin-1, a small mol. SIRT1 inhibitor, resulted in a significant decrease in cell growth and cell viability. Further, Tenovin-1 treatment also resulted in a marked decrease in the clonogenic survival of melanoma cells. Further experiments showed that the anti-proliferative response of Tenovin-1 was accompanied by an increase in the protein as well as activity of the tumor suppressor p53. This increase in p53 activity was substantiated by an increase in the protein level of its downstream target p21. Overall, these data suggest that small mol. inhibition of SIRT1 causes anti-proliferative effects in melanoma cells. SIRT1 appears to be acting through the activity of the tumor suppressor p53, which is not mutated in the majority of melanomas. However, future detailed studies are needed to further explore the role and mechanism of SIRT1 in melanoma development and progression and its usefulness in melanoma treatment.

Archives of Biochemistry and Biophysics published new progress about 380315-80-0. 380315-80-0 belongs to amides-buliding-blocks, auxiliary class Apoptosis,p53, name is N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, and the molecular formula is C9H10ClNO2, SDS of cas: 380315-80-0.

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

Wilking, Melissa J. published the artcileSirtuin deacetylases: a new target for melanoma management, Formula: C20H23N3O2S, the publication is Cell Cycle (2014), 13(18), 2821-2826, database is CAplus and MEDLINE.

A review. Melanoma continues to cause more deaths than any other skin cancer, necessitating the development of new avenues of treatment. One promising new opportunity comes in the form of mechanism-based therapeutic targets. We recently reported the overexpression and delocalization of the class III histone deacetylase SIRT1 in melanoma, and demonstrated that its small mol. inhibition via Tenovin-1 decreased cell growth and viability of melanoma cells, possibly by a p53 mediated induction of p21. Here, we support our data using addnl. SIRT inhibitors, viz. Sirtinol and Ex-527, which suggests possible benefits of concomitantly inhibiting more than one Sirtuin for an effective cancer management strategy. This “Extra View” paper also includes a discussion of our results in the context of similar recent and concurrent studies. Furthermore, we expand upon our findings in an anal. of new research that may link the cellular localization and growth effects of SIRT1 with the PI3K signaling pathway.

Cell Cycle published new progress about 380315-80-0. 380315-80-0 belongs to amides-buliding-blocks, auxiliary class Apoptosis,p53, name is N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, and the molecular formula is C8H21N3, Formula: C20H23N3O2S.

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

Allam, Bharat Kumar published the artcileHighly efficient one-pot synthesis of primary amides catalyzed by scandium(III) triflate under controlled MW, Product Details of C7H5Cl2NO, the publication is Tetrahedron Letters (2011), 52(44), 5851-5854, database is CAplus.

Primary aryl amides were prepared by amidation of aromatic aldehydes with NH₂OH.HCl by using scandium(III) triflate as a catalyst in water under controlled microwave. This methodol. offers excellent yields in shorter reaction times with enhanced selectivity.

Tetrahedron Letters 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, Product Details of C7H5Cl2NO.

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

Laha, Joydev K. published the artcileSynthesis of unsymmetrical urea from aryl- or pyridyl carboxamides and aminopyridines using PhI(OAc)₂via in situ formation of aryl- or pyridyl isocyanates, Recommanded Product: Isonicotinamide, the publication is New Journal of Chemistry (2021), 45(40), 18815-18823, database is CAplus.

A tandem synthesis of unsym. ureas (N-aryl-N’-pyridylurea and N,N’-bipyridylurea) from aryl- or pyridyl carboxamides and aminopyridines via Hofmann rearrangement has been reported. In particular, benzamides, picolinamide, nicotinamide, and isonicotinamide generate reactive intermediate isocyanates, in situ, in the presence of PhI(OAc)₂, which upon further reaction with aminopyridines form urea derivatives As the formation of pyridylisocyanates from their corresponding carboxamides via Hofmann rearrangement remained unexplored previously, attempts have been made to trap the isocyanates. While the three pyridylisocyanates were trapped as their corresponding carbamates, 3-pyridylisocyanate was isolated and characterized. Unlike closely related previous methods reported for urea synthesis, the current method avoids direct use of isocyanates or eliminates the use of toxic phosgene for the in situ generation of isocyanates.

New Journal of Chemistry 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, Recommanded Product: Isonicotinamide.

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

Singh, Harjit published the artcileSynthesis of heterocyclic compounds via enamines. Part 8. Acid-catalyzed transformations in 4,4,6-trimethyl-1,4-dihydropyrimidine-2(3H)-thione derivatives and related compounds, Formula: C5H10N2OS, the publication is Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999) (1980), 1013-18, database is CAplus.

The N-substituted trimethylpyrimidinethiones I (R = alkyl, alkenyl, Ph) were converted into the corresponding N-substituted 1,3-thiazines II and/or thioureas by heating in 11M HCl at 100-10°. However at 95-100°, Dimroth rearrangement products, e.g. the N-substituted thiazines III (R = alkyl, alkenyl, Ph), were formed. Thus, I (R = Me) (IV) in 11M HCl at 100-10° for 4 h gave 90% methylthiourea. IV in 11M HCl at 95-100° for 2.5 h gave 98% III (R = Me).

Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999) published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C18H34N4O5S, Formula: C5H10N2OS.

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

Singh, Harjit published the artcileSynthesis of heterocyclics via enamines. II. Reactions of cyclohex-1-enyl -aniline, -morpholine, and -piperidine with 1,1-dimethyl-3-oxobutyl isothiocyanate, Synthetic Route of 14294-10-1, the publication is Australian Journal of Chemistry (1975), 28(1), 143-9, database is CAplus.

The condensation of cyclohex-1-enylaniline with 1,1-dimethyl-3-oxobutyl isothiocyanate (I) gave mainly 1,5-benzodiazocine-6(1H)-thione II with some pyrimidine-2-thione III as the minor product. Similar condensations of I with cyclohex-1-enylmorpholine and cyclohex-1-enylpiperidine formed the 1-thiocarbamoyl derivatives through β-elimination of the intermediate IV (X = O, CH2).

Australian Journal of Chemistry published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C10H16Br3N, Synthetic Route of 14294-10-1.

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

Ramesh, Pattipati published the artcileDesign, synthesis and biological evaluation of some novel 3-substituted acrylamide quinoline derivatives, Safety of 2-Cyano-N-ethylacetamide, the publication is International Journal of ChemTech Research (2017), 10(3), 259-270, database is CAplus.

A new series of (2,8-dichloroquinolin-3-yl)acrylamide derivatives I (R¹ = Me, c-Pr, Ph, etc.; R² = H; -R¹R²– = -(CH₂)₄-, -(CH₂)O(CH₂)-) were designed by incorporating simple chem. methods. Here different N-substituted cyanoacetamide derivatives were used as the pharmacophore entities to link with the parent quinoline moiety. Antimicrobial activity of synthesized compounds was screened, which has revealed that the few of the compounds were more potent than the corresponding standard drugs.

International Journal of ChemTech Research 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

Kavina, M. A. published the artcile1-Carbamoylhydantoins. New Aspects of Reactivity, Name: 2-Chloroacetamide, the publication is Russian Journal of Organic Chemistry (2020), 56(12), 2119-2131, database is CAplus.

Some derivatives of 1-carbamoylhydantoins e.g., I undergo cleavage at the N¹-C(O) bond on heating in solution The 1-carbamoylhydantoins e.g., I in aqueous and alc. ammonia rearrange via opening of the imidazole ring, followed by recyclization. Prolonged treatment of 1-carbamoylhydantoins e.g., I with aqueous ammonia can lead to elimination of the C²=O carbonyl group.

Russian Journal of Organic 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, Name: 2-Chloroacetamide.

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