Category: amides-buliding-blocks

Unni, Aparna Beena published the artcileVapor-Deposited Thin Films: Studying Crystallization and α-relaxation Dynamics of the Molecular Drug Celecoxib, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Journal of Physical Chemistry B (2022), 126(20), 3789-3798, database is CAplus and MEDLINE.

Crystallization is one of the major challenges in using glassy solids for technol. applications. Considering pharmaceutical drugs, maintaining a stable amorphous form is highly desirable for improved solubility Glasses prepared by the phys. vapor deposition technique got attention because they possess very high stability, taking thousands of years for an ordinary glass to achieve. In this work, we have investigated the effect of reducing film thickness on the α-relaxation dynamics and crystallization tendency of vapor-deposited films of celecoxib (CXB), a pharmaceutical substance. We have scrutinized its crystallization behavior above and below the glass-transition temperature (T_g). Even though vapor deposition of CXB cannot inhibit crystallization completely, we found a significant decrease in the crystallization rate with decreasing film thickness. Finally, we have observed striking differences in relaxation dynamics of vapor-deposited thin films above the T_g compared to spin-coated counterparts of the same thickness.

Journal of Physical Chemistry B 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 C3H9ClOS, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide.

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

Sigurdardottir, A. G. published the artcileExploring the chemical space of the lysine-binding pocket of the first kringle domain of hepatocyte growth factor/scatter factor (HGF/SF) yields a new class of inhibitors of HGF/SF-MET binding, Safety of Morpholine-4-carbothioamide, the publication is Chemical Science (2015), 6(11), 6147-6157, database is CAplus and MEDLINE.

The growth/motility factor hepatocyte growth factor/scatter factor (HGF/SF) and its receptor, the tyrosine kinase MET, constitute a signalling system essential for embryogenesis and for tissue/organ regeneration in post-natal life. HGF/SF-MET signalling, however, also plays a key role in the onset of metastasis of a large number of human tumors. Both HGF/SF and MET are high mol. weight proteins that bury an extensive interface upon complex formation and thus constitute a challenging target for the development of low mol. weight inhibitors. Here we have used surface plasmon resonance (SPR), NMR (NMR) and X-ray crystallog. to screen a diverse fragment library of 1338 members as well as a range of piperazine-like compounds Several small mols. were found to bind in the lysine-binding pocket of the kringle 1 domain of HGF/SF and its truncated splice variant NK1. We have defined the binding mode of these compounds, explored their biol. activity and we show that selected fragments inhibit MET downstream signalling. Thus we demonstrate that targeting the lysine-binding pocket of NK1 is an effective strategy to generate MET receptor antagonists and we offer proof of concept that the HGF/SF-MET interface may be successfully targeted with small mols. These studies have broad implications for the development of HGF/SF-MET therapeutics and cancer treatment.

Chemical Science 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, Safety of Morpholine-4-carbothioamide.

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

Lerchen, Hans-Georg published the artcileAntibody-Drug Conjugates with Pyrrole-Based KSP Inhibitors as the Payload Class, Name: (S)-2-((S)-2-(6-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamido)-3-methylbutanamido)-5-ureidopentanoic acid, the publication is Angewandte Chemie, International Edition (2018), 57(46), 15243-15247, database is CAplus and MEDLINE.

The number of cytotoxic payload classes successfully employed in antibody-drug conjugates (ADCs) is still rather limited. The identification of ADC payloads with a novel mode of action will increase therapeutic options and potentially increase the therapeutic window. Herein, the authors describe the utilization of kinesin spindle protein inhibitors (KSPi) as a novel payload class providing highly potent ADCs against different targets, for instance HER-2 or TWEAKR/Fn14. Aspects of tech. optimization include the development of different linker attachment sites, the stabilization of ADC linkage to avoid payload deconjugation and finally, the tailor-made design of active metabolites with a long lasting intracellular exposure in the tumor matching the mode of action of KSP inhibition. These KSPi-ADCs are highly potent and selective in vitro and demonstrate in vivo efficacy in a broad panel of tumor models including complete regressions in a patient-derived urothelial cancer model.

Angewandte Chemie, International Edition published new progress about 916746-27-5. 916746-27-5 belongs to amides-buliding-blocks, auxiliary class ADC Linker,Enzymatic Cleavage Linker, name is (S)-2-((S)-2-(6-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamido)-3-methylbutanamido)-5-ureidopentanoic acid, and the molecular formula is C21H33N5O7, Name: (S)-2-((S)-2-(6-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamido)-3-methylbutanamido)-5-ureidopentanoic acid.

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

Maciag, Monika published the artcilePharmacological assessment of zebrafish-based cardiotoxicity models, Category: amides-buliding-blocks, the publication is Biomedicine & Pharmacotherapy (2022), 112695, database is CAplus and MEDLINE.

Cardiotoxicity remains the most common reason for failure during drug development. Recently, the zebrafish (Danio rerio) model has emerged for the evaluation of drug-dependent cardiotoxicity and for the identification of cardioprotective mols. However, it remains unknown how closely the zebrafish-based results may be translated to humans. To tackle this issue, we established embryonic zebrafish models of doxorubicin-, adrenaline- and terfenadine-induced cardiotoxicity with unified dosing regimen which eventually enabled head-to-head comparison of the drugs. Subsequently, we determined whether human cardioprotective medications – dexrazoxane, metoprolol, carvedilol and valsartan – are able to manage heart dysfunction in zebrafish. Our results indicated that doxorubicin, adrenaline and terfenadine elicited overt signs of cardiotoxicity in fish, and we further showed that the blockade of the renin-angiotensin system and, to a lesser extent, β-adrenergic system, ameliorated the heart disease in zebrafish. From the drug development standpoint, our work opens the possibility to determine the cardiovascular properties of tested compounds using the rapid and affordable zebrafish model.

Biomedicine & Pharmacotherapy 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, Category: amides-buliding-blocks.

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

Yam, Vivian Wing-Wah published the artcileSynthesis, photophysics, ion-binding studies, and structural characterization of organometallic rhenium(I) crown complexes, Recommanded Product: N,N-Diethylisonicotinamide, the publication is Organometallics (1995), 14(9), 4034-6, database is CAplus.

Re(I) complexes [Re(L)(CO)₃Cl] (1, L = I; 2, L = N-(2-pyridinylmethylene)phenylamine) and [Re(phen)(CO)₃(L’)]PF₆ (3, L’ = II; 4, L’ = 4-(N,N-diethylformamido)pyridine) were synthesized and their photophys. and cation binding properties studied. The x-ray crystal structure of 3 also was determined All the complexes exhibited long-lived intense yellow-green to orange-red emission upon visible light excitation both in the solid state and in fluid solutions at 298 K.

Organometallics published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C9H21NO3, Recommanded Product: N,N-Diethylisonicotinamide.

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

Schneggenburger, Philipp E. published the artcileAzide reduction during peptide cleavage from solid support-the choice of thioscavenger?, Application In Synthesis of 186046-83-3, the publication is Journal of Peptide Science (2010), 16(1), 10-14, database is CAplus and MEDLINE.

Peptide azides acquired growing impact because of application in bioconjugation via click chem.’ or Staudinger ligation. Furthermore, there are many methods established in organic synthesis addressing the reduction of azides to amines, but no observation of a reductive transformation of peptide azides during SPPS cleavage was yet reported. In the present study, the reduction of peptide azides during SPPS cleavage was investigated depending on the choice of thioscavenger, reacting as reductive species. First observed for short PNA/peptide conjugates the occurring extensive side reaction was also validated for one of the applied azide amino acid building blocks and was further investigated by applying different cleavage cocktails to a series of peptides varying in hydrophobicity and position of the azide moiety in the oligomer sequence. Copyright © 2009 European Peptide Society and John Wiley & Sons, Ltd.

Journal of Peptide Science published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C40H35N7O8, Application In Synthesis of 186046-83-3.

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

Sun, Yadong published the artcileCopper(II)-mediated homocoupling of thioamides for the synthesis of 1,2,4-thiadiazoles, Application of Morpholine-4-carbothioamide, the publication is European Journal of Organic Chemistry (2014), 2014(20), 4239-4243, database is CAplus.

A copper(II)-mediated highly selective oxidative cyclization reaction of thioamides to provide 3,5-disubstituted 1,2,4-thiadiazoles was developed. The copper species played a key role in this transformation and different functional groups were tolerated under the optimal reaction conditions.

European Journal of Organic 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 C11H22N2O4, Application of Morpholine-4-carbothioamide.

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

Wan, Yihong published the artcileTenovin-1 inhibited dengue virus replication through SIRT2, Name: N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, the publication is European Journal of Pharmacology (2021), 174264, database is CAplus and MEDLINE.

Dengue fever is a common arbovirus disease, which has been spread to the entire tropical world. At present, effective drugs for the treatment of dengue fever have not yet appeared, and the dengue vaccines studied in various countries have also experienced severe adverse reactions. Thus it is urgent to find new chems. against dengue virus. Now we found Sirtuins (SIRTs) were increased during dengue virus infection and tenovin-1, a SIRT1/2 inhibitor, showed an impressive antiviral ability in vitro. In BHK-21 cells, tenovin-1 inhibited the replication of DENV2 with an EC50 at 3.41 ± 1.10μM, also inhibited other three types of dengue viruses with EC50 at 0.97 ± 1.11μM, 1.81 ± 1.08μM, 3.81 ± 1.34μM resp. Moreover, the cytopathic effect-induced DENV2 was largely improved by tenovin-1 treatment and the release of progeny viruses was inhibited by tenovin-1 treatment. At the same time, the viral protein level and mRNA level were decreased with tenovin-1 treatment after dengue virus infection. From the drug-addition assay, the tenovin-1 played its antiviral after viral infection, which indicated tenovin-1 was not a microbicide. Apart from its antiviral effect, tenovin-1 inhibited the inflammatory response caused by DENV2, reducing the release of inflammatory factors during viral infection. The antiviral effect of tenovin-1 was abrogated with SIRT agonist or SIRT2 knockdown treatment, which indicated the effect of tenovin-1 was on-target. In conclusion, tenovin-1 was proved to be a promising compound against flavivirus infection through SIRT2, which should be pay more attention for further study.

European Journal of Pharmacology 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 C5H6BNO2, Name: N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide.

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

Peng, L Q published the artcileEffects of Wenyang Zhenshuai Granules on the Expression of Key Mitochondrial Autophagy Proteins in the Doxorubicin-Induced Model of H9c2 Cardiomyocyte Injury., Quality Control of 137862-53-4, the publication is Bulletin of experimental biology and medicine (2022), 173(3), 335-340, database is MEDLINE.

This study aimed to explore the effects of Wenyang Zhenshuai granules (WZG) on the morphology of cardiomyocytes, cell viability, and the expression of key mitochondrial autophagy proteins in the doxorubicin-induced model of H9c2 cardiomyocyte injury. Cardiomyocytes were cultured for 44 h and divided into 4 groups: intact control, doxorubicin-injured cells (DOX), doxorubicin-injured cells treated with WZG (DOX+WZG), and doxorubicin-injured cells treated with valsartan (DOX+valsartan; reference group). The morphology of cardiomyocytes was analyzed under an inverted microscope; cardiomyocyte survival rate was determined by MTT assay. The expression of the key mitochondrial autophagy proteins (PINK1, parkin, LC3-II, and prohibitin-2) was analyzed by Western blotting. WZG down-regulated the expression of the key mitochondrial autophagy proteins in DOX-injured cells, which may be one of the important mechanisms for regulating ventricular remodeling and cardiomyocyte apoptosis.

Bulletin of experimental biology and medicine 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, Quality Control of 137862-53-4.

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

Li, Bing published the artcileEfficient synthesis of amino acid polymers for protein stabilization, Formula: C11H22N2O4, the publication is Biomaterials Science (2019), 7(9), 3675-3682, database is CAplus and MEDLINE.

Proteins are fragile such that even freezing, drying and dehydration may induce their denaturation, aggregation, and activity loss. To protect proteins from these kinds of damage, we prepared two types of amino acid polymers, PLG-r-PLL and PLG, from the efficient ring-opening polymerization of α-amino acid N-carboxyanhydride using LiHMDS as the initiator. β-Galactosidase was used in this study to examine the protein protecting effect of the synthesized amino acid polymers during lyophilization. The results indicate that both PLG-r-PLL and PLG exert significant protection on β-Gal during lyophilization and improve the activity of the resulting protein from 40%, without using a protecting agent during lyophilization, to 80% of the original protein activity. Nevertheless, PLG generally performs better than PLG-r-PLL independent of the chain length. Our studies also show that PLG and PLG-r-PLL with a high content of PLG subunits display no observable cytotoxicity and hemolytic effect. Furthermore, DLS and TEM characterization indicate that PLG protects β-Gal upon lyophilization by preventing the aggregation of β-Gal. Our studies demonstrate that amino acid polymers, such as PLG, can exert potent activity for protein stabilization. The easy operation of LiHMDS-initiated and efficient NCA polymerization implies the great potential of this strategy to prepare amino acid polymers quickly for the screening of protein stabilization and mechanism study.

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, Formula: C11H22N2O4.

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