Category: amides-buliding-blocks

Guion-Firmin, Julia published the artcileDiarrhoea with the angiotensin receptor neprilysin inhibitor sacubitril + valsartan: A pharmacovigilance study, COA of Formula: C24H29N5O3, the publication is Fundamental & Clinical Pharmacology (2022), 36(2), 378-389, database is CAplus and MEDLINE.

Diarrhoea is an adverse drug reaction of the angiotensin receptor neprilysin inhibitor (ARNI) sacubitril + valsartan. It was also described with olmesartan and more recently with other angiotensin receptor blockers. The study was performed to compare diarrhoea reports in pharmacovigilance databases with sacubitril + valsartan and valsartan. The study used reports of diarrhoea with the ARNI sacubitril + valsartan registered: first in the French PharmacoVigilance Database (FPVD) and second in Vigibase, the WHO Global Individual Case Safety Report database. After description of the main characteristics, disproportionality analyses were performed. Results are reported as reporting odds ratios (ROR) with 95% confidence interval. We found 29 reports of diarrhoea with sacubitril + valsartan in the FPVD and 686 in Vigibase. With sacubitril + valsartan, diarrhoea occurred more frequently in males around 70 years with a median delay of 3 days. With valsartan, diarrhoea occurred more frequently in females around 68 years with a median delay of 0.5 days. In the FPVD, a significant association was found with sacubitril + valsartan in comparison with valsartan alone before (ROR = 8.78 [5.19-14.85]) and after (ROR = 11.19 [5.89-21.25]) exclusion of concomitant drugs known to be associated with diarrhoea. A significant association was also found in Vigibase after adjustment on age, sex, reporter and its location (ROR = 1.31 [1.14-1.50]). Diarrhoea reported with sacubitril + valsartan has marked differences in gender, delay of occurrence and frequency of reporting in comparison with diarrhoea with valsartan. From a pharmacodynamic point of view, these results suggest a specific role of sacubitril in diarrhoea.

Fundamental & Clinical Pharmacology published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, COA of Formula: C24H29N5O3.

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

Matsuda, Takehisa published the artcileSynthesis of Multifunctional, Nonionic Vinyl Polymers and Their ¹³C Spin-Lattice Relaxation Times in Deuterium Oxide Solutions, Synthetic Route of 2479-62-1, the publication is Macromolecules (1996), 29(16), 5375-5383, database is CAplus.

A study was conducted to design very hydrophilic vinyl polymers. Various nonionic, water-soluble polymers with hydroxyl or primary amide groups in their side chains were prepared by radical polymerization of corresponding monomers or by polymer reactions to modify side chains derivatized in poly(vinyl ethers). The functional groups interconnecting a hydrophobic main chain and a side chain included ether, secondary and tertiary amide, and ester groups. The number of hydroxyl groups incorporated in the side chains per monomer unit ranged from one to nine, and that of primary amide groups ranged from one to three. The spin-lattice relaxation times (T₁) of individual carbon atoms were measured in deuterium oxide (D₂O) by an inversion-recovery Fourier transform method as an indicator of chain or group mobility. As for the effect of interconnecting groups on the mobilities of main and side chains, these increased in the following order: ether > ester and tertiary amide > secondary amide. Considerably reduced T₁ values were found with increasing number of hydroxyl groups in the side chains. The addition of lithium bromide to D₂O solutions substantially increased T₁ values for hydroxyl group-derivatized polymers, indicating that intramol. hydrogen bonds responsible for reduced T₁ values are broken to enhance chain or group mobility. On the other hand, minimal effect of lithium bromide addition was found for ether- or primary amide-derivatized polymers. These results suggest that, when an ether group is incorporated as an interconnecting group into a vinyl polymer and primary amide groups are well distributed at the terminal ends of the side chains, such a polymer could have high chain and group mobility, which may impart high hydrophilicity. The mol. structure-mobility relationship was discussed in terms of T₁ values. It is suggested that a combination of factors, such as the structure of interconnecting group, the structure of hydrophilic group, intra- and interpendant-group interactions, hydrogen bonding, and steric factors, all contribute to T₁ values.

Macromolecules published new progress about 2479-62-1. 2479-62-1 belongs to amides-buliding-blocks, auxiliary class Monomers,Acrylamide Monomers, name is N-(2-Amino-2-oxoethyl)acrylamide, and the molecular formula is C5H8N2O2, Synthetic Route of 2479-62-1.

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

Hirai, Kentaro published the artcileStudies on heterocyclic cation systems. XI. Syntheses of 2-disubstituted-amino-4-arylthiazol-5-ylalkanoic acids, COA of Formula: C5H10N2OS, the publication is Chemical & Pharmaceutical Bulletin (1977), 25(9), 2292-9, database is CAplus.

2-Disubstituted-amino-4-arylthiazol-5-ylalkanoic acids I (R = piperidino, morpholino, MeNH, BzNH, p-ClC₆H₄CONH, R¹ = H, Me; R² = Ph, 2-thienyl, p-ClC₆H₄, p-BrC₆H₄) were prepared Thus, dehydration of S-(α-benzoyl-β-ethoxycarbonyl)ethyl 1-piperidinethiocarbonate in the presence of aqueous HClO₄-Ac₂O yielded 4-ethoxycarbonylmethyl-5-phenyl-2-piperidino-1,3-oxathiolium perchlorate, which underwent nucleophilic reaction with NH₃ and the 5-ethoxycarbonylmethyl-4-phenyl-2-piperidinothiazole hydrolyzed to give I (R = piperidino, R¹ = H, R² = Ph). I were also synthesized by the classical Hantzsch method. I were evaluated as antiinflammatory agents on carrageenin induced abscess in rats.

Chemical & Pharmaceutical Bulletin 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, COA of Formula: C5H10N2OS.

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

Kanemoto, Kazuya published the artcileRhodium-catalyzed odorless synthesis of diaryl sulfides from borylarenes and S-aryl thiosulfonates, Computed Properties of 146140-95-6, the publication is Chemical Communications (Cambridge, United Kingdom) (2017), 53(77), 10640-10643, database is CAplus and MEDLINE.

Diaryl sulfides such as I [R¹ = 4-BrC₆H₄, 4-Me₂NC₆H₄, 3-thienyl, etc.; R² = 4-MeC₆H₄, 2-FC₆H₄, 3-HOC₆H₄] were efficiently prepared by rhodium-catalyzed odorless deborylative arylthiolation of organoborons with S-aryl thiosulfonates. The ready availability of starting materials and further transformation of sulfides was rendered a diverse range of organosulfur compounds easily accessible.

Chemical Communications (Cambridge, United Kingdom) 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, Computed Properties of 146140-95-6.

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

Wu, Chaoneng published the artcile“Pro-resolution” and anti-inflammation, a role of RvE1 in anti-atherosclerosis and plaque stabilization, Quality Control of 321673-30-7, the publication is Medical Hypotheses (2008), 71(2), 252-255, database is CAplus and MEDLINE.

A review. Summary: Inflammation governs atherosclerosis and is firmly regulated. Endogenous mechanisms to keep inflammation self-limiting are unclear. In the present article, we propose that RvE1 (resolution E1), an endogenous lipid mediator, inhibits inflammation through “pro-resolution” and counter-modulating immunity in atherosclerosis. The background comes from studies on the potent programming of resolution and immuno-inflammation of RvE1 and its precursor, eicosapentaenoic acid, in treating chronic inflammatory disease with unknown mechanisms. In light of the interaction between RvE1 and leukotrieneB4 (LTB4) and their potential impaired immunity regulation hematostasis, we hypothesize that RvE1 play an anti-atherosclerosis and plaque stabilization role through “pro-resolution” and anti-inflammation which may be realized by blocking LTB4/BLT1 (receptor of LTB4) pathway. Our hypothesis generates potentially clin. viewpoint to systematically look for pro- and anti-inflammation and “pro-resolution” process in atherosclerosis. Furthermore, we suggest that RvE1 might be particularly indicated for the treatment of atherosclerotic diseases and plaque stabilization which might ensure an effective management for patients with coronary artery disease.

Medical Hypotheses 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 C14H12N2S, Quality Control of 321673-30-7.

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

Wang, Xuan published the artcileRuthenium-Promoted C-H Activation Reactions between DNA-Conjugated Acrylamide and Aromatic Acids, SDS of cas: 2479-62-1, the publication is Organic Letters (2018), 20(16), 4764-4768, database is CAplus and MEDLINE.

The first example of DNA-compatible C-H activation reaction between DNA-conjugated acrylamides and aromatic acids has been developed. This new transformation enables aromatic acid, previously considered as monofunctional building block, to act like a bifunctional building block for the DNA encoded library synthesis. The general scope of aromatic acid was established for this new on-DNA C-H activation, which paved the way for its application in combinatorial library preparation

Organic Letters published new progress about 2479-62-1. 2479-62-1 belongs to amides-buliding-blocks, auxiliary class Monomers,Acrylamide Monomers, name is N-(2-Amino-2-oxoethyl)acrylamide, and the molecular formula is C6H8O4, SDS of cas: 2479-62-1.

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

Gan, Na published the artcileHow hydrophilic group affects drug-protein binding modes: Differences in interaction between sirtuins inhibitors Tenovin-1/Tenovin-6 and human serum albumin, Formula: C25H34N4O2S, the publication is Journal of Pharmaceutical and Biomedical Analysis (2021), 114121, database is CAplus and MEDLINE.

Introduction of hydrophilic groups can improve the solubility of leading drugs but inevitably affect their interaction with proteins. This study selected sirtuin inhibitors Tenovin-1 (T1) and Tenovin-6 (T6) as drug models to determine differences in binding mode to human serum albumin (HSA). T1 and T6 quenched the endogenous fluorescence of HSA via static quenching mechanism. Introduction of hydrophilic groups greatly reduced the binding constant, i.e., from 1.302 x 104 L mol-1 for the HSA-T6 system to 0.128 x 104 L mol-1 for the HSA-T1 system. HSA-T1 system was mainly driven by electrostatic interactions while that of HSA-T6 system was hydrophobic interaction and both systems were spontaneous reactions. Site marker experiments and mol. docking indicated that both systems mainly bound to the hydrophobic site I of HSA. Mol. dynamics (MD) simulation anal. further revealed that Tyr148, Tyr150 and Arg257 residues played a key role in this recognition process for both systems. In particular, T6 maintained addnl. several hydrogen bonds with the surrounding residues. T1 had almost no effect on the esterase-like activity of HSA, but T6 inhibited the hydrolysis of p-NPA. Furthermore, differential scanning calorimetry (VP-DSC), CD (CD) and Fourier transform IR (FTIR) spectroscopy confirmed that HSA in the T6 system undergone a more significant conformational transition than that in the T1 system.

Journal of Pharmaceutical and Biomedical Analysis published new progress about 1011557-82-6. 1011557-82-6 belongs to amides-buliding-blocks, auxiliary class Epigenetics,Sirtuin, name is 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, and the molecular formula is C25H34N4O2S, Formula: C25H34N4O2S.

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

Gan, Na published the artcileHow hydrophilic group affects drug-protein binding modes: Differences in interaction between sirtuins inhibitors Tenovin-1/Tenovin-6 and human serum albumin, Computed Properties of 380315-80-0, the publication is Journal of Pharmaceutical and Biomedical Analysis (2021), 114121, database is CAplus and MEDLINE.

Introduction of hydrophilic groups can improve the solubility of leading drugs but inevitably affect their interaction with proteins. This study selected sirtuin inhibitors Tenovin-1 (T1) and Tenovin-6 (T6) as drug models to determine differences in binding mode to human serum albumin (HSA). T1 and T6 quenched the endogenous fluorescence of HSA via static quenching mechanism. Introduction of hydrophilic groups greatly reduced the binding constant, i.e., from 1.302 x 104 L mol-1 for the HSA-T6 system to 0.128 x 104 L mol-1 for the HSA-T1 system. HSA-T1 system was mainly driven by electrostatic interactions while that of HSA-T6 system was hydrophobic interaction and both systems were spontaneous reactions. Site marker experiments and mol. docking indicated that both systems mainly bound to the hydrophobic site I of HSA. Mol. dynamics (MD) simulation anal. further revealed that Tyr148, Tyr150 and Arg257 residues played a key role in this recognition process for both systems. In particular, T6 maintained addnl. several hydrogen bonds with the surrounding residues. T1 had almost no effect on the esterase-like activity of HSA, but T6 inhibited the hydrolysis of p-NPA. Furthermore, differential scanning calorimetry (VP-DSC), CD (CD) and Fourier transform IR (FTIR) spectroscopy confirmed that HSA in the T6 system undergone a more significant conformational transition than that in the T1 system.

Journal of Pharmaceutical and Biomedical Analysis 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 C20H23N3O2S, Computed Properties of 380315-80-0.

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

Li, Hao published the artcileEfficient Synthesis of 1,9-Substituted Benzo[h][1,6]naphthyridin-2(1H)-ones and Evaluation of their Plasmodium falciparum Gametocytocidal Activities, Application In Synthesis of 947533-21-3, the publication is ACS Combinatorial Science (2017), 19(12), 748-754, database is CAplus and MEDLINE.

A novel three-component, two-step, 1-pot nucleophilic aromatic substitution (S_NAr)-intramol. cyclization-Suzuki coupling reaction was developed for the synthesis of benzo[h][1,6]naphthyridin-2(1H)-ones (Torins). On the basis of the new efficiently convergent synthetic route, a library of Torin 2 analogs was synthesized. The antimalarial activities of these compounds were evaluated against asexual parasites using a growth inhibition assay and gametocytes using a viability assay.

ACS Combinatorial Science published new progress about 947533-21-3. 947533-21-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Boronic acid and ester,Amine,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (6-Acetamidopyridin-3-yl)boronic acid, and the molecular formula is C7H9BN2O3, Application In Synthesis of 947533-21-3.

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

Patel, Paresma R. published the artcileIn vitro evaluation of imidazo[4,5-c]quinolin-2-ones as gametocytocidal antimalarial agents, Name: (6-Acetamidopyridin-3-yl)boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(12), 2907-2911, database is CAplus and MEDLINE.

Novel imidazo[4,5-c]quinolin-2-ones, such as I, were synthesized and evaluated in asexual blood stage and late stage gametocyte assays of Plasmodium falciparum, a major causative agent of malaria. The design of these compounds is based on a recently identified lead compound from a high throughput screen. A concise synthesis was developed that allowed for generation of analogs with substitution around both the quinoline and imidazolidinone rings. Through structure-activity relationship studies, a number of potent compounds were identified that possessed excellent antimalarial activity against both the asexual and sexual stages with minimal cytotoxicity in mammalian cells. This is the first Letter describing SAR and gametocytocidal activity of imidazo[4,5-c]quinolin-2-ones, a new lead series for malaria treatment and prevention.

Bioorganic & Medicinal Chemistry Letters published new progress about 947533-21-3. 947533-21-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Boronic acid and ester,Amine,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (6-Acetamidopyridin-3-yl)boronic acid, and the molecular formula is C7H9BN2O3, Name: (6-Acetamidopyridin-3-yl)boronic acid.

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