Category: amides-buliding-blocks

Ma, Pengcheng published the artcileBiodegradable peptide polymers as alternatives to antibiotics used in aquaculture, Computed Properties of 2418-95-3, the publication is Biomaterials Science (2022), 10(15), 4193-4207, database is CAplus and MEDLINE.

The pressure of antimicrobial resistance has forced many countries to reduce or even prohibit the use of antibiotics in feed. Therefore, it is an urgent need to develop alternatives to antibiotics to control infectious diseases in feed and aquaculture. To address this long-lasting challenge, we prepared peptide polymers that display potent and broad-spectrum activity against common pathogenic bacteria in aquaculture, low hemolysis and low cytotoxicity, and do not induce bacteria to develop resistance or cross-resistance to antibiotics. The optimal peptide polymer demonstrates strong in vivo therapeutic potential in an adult zebrafish infection model. Moreover, the optimal peptide polymer is biodegradable by enzymes into single amino acids and dipeptides to totally lose its antibacterial activity and, therefore, will not cause antimicrobial selective pressure. Our study suggests that peptide polymers are promising alternatives to antibiotics in aquaculture and open new avenues to address the global challenge of antimicrobial resistance.

Biomaterials 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, Computed Properties of 2418-95-3.

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

Wang, Chunxiang published the artcileIron-Catalyzed Cycloaddition Reaction of Diynes and Cyanamides at Room Temperature, Formula: C15H14N2, the publication is Journal of Organic Chemistry (2013), 78(7), 3065-3072, database is CAplus and MEDLINE.

An iron-catalyzed [2+2+2] cycloaddition reaction of diynes and cyanamides at room temperature is reported. Highly substituted 2-aminopyridines were obtained in good to excellent yields with high regioselectivity. E.g., in presence of FeI₂, dppp, and Zn dust, [2+2+2] cycloaddition reaction of MeCCCH₂NTsCH₂CCMe and (Me₂CH)₂NCN gave 91% 2-aminopyridine derivative (I). Insights toward the reaction process were investigated through in situ IR spectra and control experiments In this iron-catalyzed cycloaddition reaction, the active iron species was generated only in the presence of both alkynes and nitriles. The lower reaction temperature, broad substrates scope, and inversed regioselectivity make it a complementary method to the previously developed iron catalytic system.

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 C8H5F3N4, Formula: C15H14N2.

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

Li, Yongwang published the artcileA study on the rules of ligands in highly efficient Ru-amide/AC catalysts for acetylene hydrochlorination, Recommanded Product: 2-Chloroacetamide, the publication is Catalysis Science & Technology (2021), 11(22), 7347-7358, database is CAplus.

To explore the role of substituents on ligands in the modification of metal catalysts, a series of Ru-amide/AC catalysts are synthesized with various amide ligands derived from formamide and assessed for acetylene hydrochlorination. Activity evaluation reveals a rule that replacing a hydrogen on formamide with an electron donor substituent can enhance the catalytic performance, while electron withdrawing substituents have the opposite effect. However, formanilide, which violates this law, shows the best modification effect, which is proved to be the effect of steric hindrance by characterization and DFT calculation Therefore, another rule is concluded that the electron donor ability and steric hindrance of substituents on amide ligands jointly affect the modification effect. Finally, benzanilide, with a superior modification effect, which searched based on the above results, gives strong evidence for the correction of these rules. This work provides a theor. basis for the search for efficient ligands for acetylene hydrochlorination.

Catalysis Science & Technology 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, Recommanded Product: 2-Chloroacetamide.

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

Ge, Yongmei published the artcileA ZIF-8-based multifunctional intelligent drug release system for chronic osteomyelitis, Formula: C17H14F3N3O2S, the publication is Colloids and Surfaces, B: Biointerfaces (2022), 112354, database is CAplus and MEDLINE.

Chronic osteomyelitis (COM) is an inflammatory bone disease caused by bacterial infection. Conventional treatment with antibiotics is prone to resistance and other side effects, and it is ineffective against inflammation caused by infection and bone loss. To treat COM comprehensively, based on the acidic microenvironment of osteomyelitis, we used ZIF-8 and celecoxib to construct a multifunctional intelligent drug release system with pH response effect, named CEL@ZIF-8. Material characterization revealed that celecoxib is successfully loaded into ZIF-8. Ion release and drug release experiments indicated that CEL@ZIF-8 can respond well to the pH and intelligently control the release of ions and drugs. Antibacterial assays manifested that CEL@ZIF-8 is able to inhibit the growth of bacteria significantly. In vitro cell experiments demonstrated that CEL@ZIF-8 can significantly up-regulate the expression of osteogenesis-related cytokines and down-regulate the levels of inflammatory factors. Studies verify that the novel drug release system possesses multiple functions: antibacterial, osteogenesis, anti-inflammatory and intelligent release, suggesting a tremendous clin. promise for the treatment of COM.

Colloids and Surfaces, B: Biointerfaces published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, Formula: C17H14F3N3O2S.

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

Li, Ling published the artcileActivation of p53 by SIRT1 Inhibition Enhances Elimination of CML Leukemia Stem Cells in Combination with Imatinib, Related Products of amides-buliding-blocks, the publication is Cancer Cell (2012), 21(2), 266-281, database is CAplus and MEDLINE.

BCR-ABL tyrosine kinase inhibitors (TKI) fail to eliminate quiescent leukemia stem cells (LSC) in chronic myelogenous leukemia (CML). Thus, strategies targeting LSC are required to achieve cure. We show that the NAD⁺-dependent deacetylase SIRT1 is overexpressed in human CML LSC. Pharmacol. inhibition of SIRT1 or SIRT1 knockdown increased apoptosis in LSC of chronic phase and blast crisis CML and reduced their growth in vitro and in vivo. SIRT1 effects were enhanced in combination with the BCR-ABL TKI imatinib. SIRT1 inhibition increased p53 acetylation and transcriptional activity in CML progenitors, and the inhibitory effects of SIRT1 targeting on CML cells depended on p53 expression and acetylation. Activation of p53 via SIRT1 inhibition represents a potential approach to target CML LSC.

Cancer Cell 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, Related Products of amides-buliding-blocks.

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

Zheng, Chunxiong published the artcileIn Situ Modification of the Tumor Cell Surface with Immunomodulating Nanoparticles for Effective Suppression of Tumor Growth in Mice, COA of Formula: C10H12BNO5, the publication is Advanced Materials (Weinheim, Germany) (2019), 31(32), n/a, database is CAplus and MEDLINE.

Current cancer immunotherapies including chimeric antigen receptor (CAR)-based therapies and checkpoint immune inhibitors have demonstrated significant clin. success, but always suffer from immunotoxicity and autoimmune disease. Recently, nanomaterial-based immunotherapies are developed to precisely control in vivo immune activation in tumor tissues for reducing immune-related adverse events. However, little consideration has been put on the spatial modulation of interactions between immune cells and cancer cells to optimize the efficacy of cancer immunotherapies. Herein, a rational design of immunomodulating nanoparticles is demonstrated that can in situ modify the tumor cell surface with natural killer cell (NK cell)-activating signals to achieve in situ activation of tumor-infiltrating NK cells, as well as direction of their antitumor immunity toward tumor cells. Using these immunomodulating nanoparticles, the remarkable inhibition of tumor growth is observed in mice without noticeable side effects. This study provides an accurate immunomodulation strategy that achieves safe and effective antitumor immunity through in situ NK cell activation in tumors. Further development by constructing interactions with various immune cells can potentially make this nanotechnol. become a general platform for the design of advanced immunotherapies for cancer treatments.

Advanced Materials (Weinheim, Germany) published new progress about 2024542-05-8. 2024542-05-8 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Boronic Acids, name is 3-(4-Boronobenzamido)propanoic acid, and the molecular formula is C7H3Cl2F3O2S, COA of Formula: C10H12BNO5.

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

Zhang, Lijun published the artcileCannizzaro-Type Disproportionation of Aromatic Aldehydes to Amides and Alcohols by Using Either a Stoichiometric Amount or a Catalytic Amount of Lanthanide Compounds, Recommanded Product: 2,4-Dichlorobenzamide, the publication is Journal of Organic Chemistry (2006), 71(8), 3149-3153, database is CAplus and MEDLINE.

Aromatic aldehydes can be directly converted to the corresponding amides and alcs. in good to excellent yields by treatment with LiN(SiMe₃)₂ in the presence of catalytic lanthanide chlorides LnCl₃ or with a stoichiometric amount of lanthanide amides [(Me₃Si)₂N]₃Ln(μ-Cl)Li(THF)₃ at ambient temperature. The effects of solvents, substituents on the Ph ring, and lanthanide metals on the reaction have been examined The mechanism of the disproportionation reaction was proposed based on the exptl. results.

Journal of Organic 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 C5H10O2S, Recommanded Product: 2,4-Dichlorobenzamide.

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

Wei, Jing published the artcile3D-Pharmacophore Models for Selective A_2A and A_2B Adenosine Receptor Antagonists, Product Details of C27H29N5O5, the publication is Journal of Chemical Information and Modeling (2007), 47(2), 613-625, database is CAplus and MEDLINE.

Three-dimensional pharmacophore models were generated for A_2A and A_2B adenosine receptors (ARs) based on highly selective A_2A and A_2B antagonists using the Catalyst program. The best pharmacophore model for selective A_2A antagonists (Hypo-A_2A) was obtained through a careful validation process. Four features contained in Hypo-A_2A (one ring aromatic feature (R), one pos. ionizable feature (P), one hydrogen bond acceptor lipid feature (L), and one hydrophobic feature (H)) seem to be essential for antagonists in terms of binding activity and A_2A AR selectivity. The best pharmacophore model for selective A_2B antagonists (Hypo-A_2B) was elaborated by modifying the Catalyst common features (HipHop) hypotheses generated from the selective A_2B antagonists training set. Hypo-A_2B also consists of four features: one ring aromatic feature (R), one hydrophobic aliphatic feature (Z), and two hydrogen bond acceptor lipid features (L). All features play an important role in A_2B AR binding affinity and are essential for A_2B selectivity. Both A_2A and A_2B pharmacophore models have been validated toward a wide set of test mols. containing structurally diverse selective antagonists of all AR subtypes. They are capable of identifying correspondingly high potent antagonists and differentiating antagonists between subtypes. The results of our study will act as a valuable tool for retrieving structurally diverse compounds with desired biol. activities and designing novel selective adenosine receptor ligands.

Journal of Chemical Information and Modeling published new progress about 264622-53-9. 264622-53-9 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Adenosine Receptor, name is N-(4-Acetylphenyl)-2-(4-(2,6-dioxo-1,3-dipropyl-2,3,6,9-tetrahydro-1H-purin-8-yl)phenoxy)acetamide, and the molecular formula is C12H9N3O4, Product Details of C27H29N5O5.

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

Ma, Liang published the artcileSynthesis, Activity, and Docking Study of Novel Phenylthiazole-Carboxamido Acid Derivatives as FFA2 Agonists, Quality Control of 2447-79-2, the publication is Chemical Biology & Drug Design (2016), 88(1), 26-37, database is CAplus and MEDLINE.

Free fatty acid receptor 2 (FFA2), also known as GPR43, is activated by short-chain fatty acids (SCFAs) that are mainly produced by the gut microbiota through the fermentation of undigested carbohydrates and dietary fibers. FFA2 currently appears to be a potential target in the management of obesity, diabetes, inflammatory diseases, and cancer. In the study, a series of novel phenylthiazole-carboxamido acid derivatives has been synthesized and evaluated as potential orthosteric FFA2 ligands for the study of structure-activity relationships. Compound 6e was found to exhibit the twofold potent agonistic activity in the stable hFFA2-transfected CHO-K1 cells (EC₅₀ = 23.1 μm) as that of pos. control propionate (EC₅₀ = 43.3 μm). We also reported the results of mutagenesis studies based on the crystal structure of hFFA1 bound to TAK-875 at 2.3 Å resolution to identify important residues for orthosteric agonist 6e inducing FFA2 activation.

Chemical Biology & Drug Design 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, Quality Control of 2447-79-2.

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

Zhang, Yue published the artcileAnderson-type polyoxometalate-based complexes constructed from a new ′V′-like bis-pyridine-bis-amide ligand for selective adsorption of organic dyes and detection of Cr(VI) and Fe(III) ions, Related Products of amides-buliding-blocks, the publication is Inorganic Chemistry Frontiers (2021), 8(20), 4458-4466, database is CAplus.

By introducing a new ′V′-like bis-pyridine-bis-amide ligand 4,4′-bis(4-pyridinecarboxamide)phenylmethane (L) into the reaction system based on Anderson-type polyoxometalates [XMo₆(OH)₆O₁₈]^3- (X = Al or Cr), four metal-organic complexes (MOCs) 1-4, [Zn(HL)(H₂O)₂(XMo₆(OH)₆O₁₈)].5H₂O (1: X = Al; 2: X = Cr), [Co(HL)(H₂O)₂(XMo₆(OH)₆O₁₈)]·5H₂O (3: X = Al; 4: X = Cr), have been prepared under solvothermal conditions, which have been characterized by single crystal X-ray diffraction, IR spectra, and PXRD. All structures of 1-4 involved a 2D layer that originated from XMo₆ polyoxoanions and metal ions, on both sides of which the L ligands were hanged. Complexes 1-4 showed not only outstanding selective adsorption capacities for organic dyes crystal violet, methylene blue and neutral red, but also electrochem. sensing behaviors toward Cr(VI) ions and Fe(III) ions with well-pleasing limits of detection of 0.606 nM (6.24 × 10-5 ppm) and 0.0192 μM (1.08 × 10-3 ppm), suggesting their potential application as multifunctional materials.

Inorganic Chemistry Frontiers 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 C8H11BO2, Related Products of amides-buliding-blocks.

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