Amides-buliding-blocks

Tocco, Graziella; Esposito, Francesca; Caboni, Pierluigi; Laus, Antonio; Beutler, John A.; Wilson, Jennifer A.; Corona, Angela; Le Grice, Stuart F. J.; Tramontano, Enzo published the artcile< Scaffold hopping and optimisation of 3′,4′-dihydroxyphenyl- containing thienopyrimidinones: synthesis of quinazolinone derivatives as novel allosteric inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H>, SDS of cas: 5004-88-6, the main research area is HIV1 virus allosteric inhibitors reverse transcriptase RNase H; Bioisosters; HIV-1 virus; RNase H; RNase H allosteric inhibitors; integrase.

Bioisosteric replacement and scaffold hopping are powerful strategies in drug design useful for rationally modifying a hit compound towards novel lead therapeutic agents. Recently, we reported a series of thienopyrimidinones that compromise dynamics at the p66/p51 HIV-1 reverse transcriptase (RT)-associated RNase H (RNase H) dimer interface, thereby allosterically interrupting catalysis by altering the active site geometry. Although they exhibited good submicromolar activity, the isosteric replacement of the thiophene ring, a potential toxicophore, is warranted. Thus, in this article, the most active 2-(3,4-dihydroxyphenyl)-5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-one was selected as the hit scaffold and several isosteric substitutions of the thiophene ring were performed. A novel series of highly active RNase H allosteric quinazolinone inhibitors was thus obtained. To determine their target selectivity, they were tested against RT-associated RNA-dependent DNA polymerase (RDDP) and integrase (IN). Interestingly, none of the compounds were particularly active on (RDDP) but many displayed micromolar to submicromolar activity against IN.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Antiviral agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, SDS of cas: 5004-88-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Belenguer, Ana M.; Cruz-Cabeza, Aurora J.; Lampronti, Giulio I.; Sanders, Jeremy K. M. published the artcile< On the prevalence of smooth polymorphs at the nanoscale: implications for pharmaceuticals>, SDS of cas: 94-20-2, the main research area is polymorph D sorbitol chlorpropamide acetonitrile anthranilic acid nanoscale crystallite.

We demonstrate, for four different systems of pharmaceutical relevance, that ball mill grinding leads to different polymorphic transformations depending on the milling conditions. In all four cases, the com. polymorph converts to a different polymorph upon ball-mill neat grinding (NG). This transformation can be reversed by grinding the so obtained polymorph in the presence of small amounts of solvent (LAG), leading back to the com. polymorph. Scherrer particle size determinations reveal that NG conditions almost always lead to smaller particle sizes in the nanometer length scales. Computational studies confirm that polymorphs obtained by the specific ball mill LAG conditions reported correspond to the lowest lattice energy forms. Our study further confirms our earlier conclusions that, at the nanoscale, polymorphs with higher lattice energies can become the thermodynamically stable forms if their surfaces are more stable than those of the polymorphs obtained by LAG. We found, however, one exception to this trend in D-sorbitol. We observe that polymorphs with smoother surfaces (low roughness) are usually the ones observed by NG. This observation points to a link between surface roughness and surface stability.

CrystEngComm published new progress about Cell morphology. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, SDS of cas: 94-20-2.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Parekh, Vimal; Ramsden, James A.; Wills, Martin published the artcile< Asymmetric transfer hydrogenation of quinolines using tethered Ru(II) catalysts>, Recommanded Product: Chloro[N-[(1R,2R)-1,2-diphenyl-2-[[3-(η6-phenyl)propyl]amino-κN]ethyl]-4-methylbenzenesulfonamidato-κN]ruthenium, the main research area is asym transfer hydrogenation quinoline ruthenium catalyst.

The first report of an asym. transfer hydrogenation, in formic acid/triethylamine, of quinolines is described. Using a Ru(II) catalyst containing a 4-carbon tether, products of up to 73% ee were formed, while a Rh(III)-tethered catalyst gave products of up to 94% ee.

Tetrahedron: Asymmetry published new progress about Enantioselective synthesis. 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, Recommanded Product: Chloro[N-[(1R,2R)-1,2-diphenyl-2-[[3-(η6-phenyl)propyl]amino-κN]ethyl]-4-methylbenzenesulfonamidato-κN]ruthenium.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Zhou, Xiaqing; Chang, Tzu-Lan; Chen, Shuang; Liu, Tianchi; Wang, Haoyu; Liang, Jun F. published the artcile< Polydopamine-Decorated Orlistat-Loaded Hollow Capsules with an Enhanced Cytotoxicity against Cancer Cell Lines>, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is polydopamine orlistat capsule cancer antitumor; cancer therapy; controlled release; hollow capsule; nanoparticle; orlistat; polydopamine.

Orlistat, an FDA-approved antiobesity drug, has recently been shown to have anticancer effects. However, orlistat is extremely hydrophobic with low absorption. Therefore, new approaches are needed to effectively deliver orlistat for cancer therapy. Herein, we developed a fast and simple method to use polydopamine-coated hollow capsule (PHC) as a drug nanocarrier for enhancing the therapeutic effects of orlistat. Orlistat-loaded PHC had an average size of 200 nm, which was characterized by using dynamic light scattering and scanning electron microscope. Furthermore, the polydopamine layer provided an excellent control of orlistat release because it was extremely sensitive to pH values. The cellular uptake and cytotoxicity experiments were performed to show that orlistat packaged in PHC could be endocytosed into cells and then significantly improved the cytotoxic activity against cancer cell lines in a short time compared with free orlistat. Moreover, dynamic study of cell membrane lysis was performed by staining with the LIVE/DEAD kit to demonstrate the cancer-killing mechanism. The size of the cell surface area has also been proven to be a key parameter which affected drug efficacy. Taken all together, these results present that orlistat-loaded PHC is a very promising formula for cancer treatments.

Molecular Pharmaceutics published new progress about Antitumor agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Goodman, Patricia A.; Niehoff, Lisa B.; Uckun, Fatih M. published the artcile< Role of tyrosine kinases in induction of the c-jun proto-oncogene in irradiated B-lineage lymphoid cells>, Synthetic Route of 5004-88-6, the main research area is gamma irradiation cjun lymphocyte tyrosine kinase.

Exposure of B-lineage lymphoid cells to ionizing radiation induces an elevation of c-jun proto-oncogene mRNA levels. This signal is abrogated by protein-tyrosine kinase (PTK) inhibitors, indicating that activation of an as yet unidentified PTK is mandatory for radiation-induced c-jun expression. Here, we provide exptl. evidence that the cytoplasmic tyrosine kinases BTK, SYK, and LYN are not required for this signal. Lymphoma B-cells rendered deficient for LYN, SYK, or both by targeted gene disruption showed increased c-jun expression levels after radiation exposure, but the magnitude of the stimulation was lower than in wild-type cells. Thus, these PTKs may participate in the generation of an optimal signal. Notably, an inhibitor of JAK-3 (Janus family kinase-3) abrogated radiation-induced c-jun activation, prompting the hypothesis that a chicken homolog of JAK-3 may play a key role in initiation of the radiation-induced c-jun signal in B-lineage lymphoid cells.

Journal of Biological Chemistry published new progress about Animal gene, c-jun Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Synthetic Route of 5004-88-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Noori, Soheila; Mirzababaei, Atieh; Amini, Mohammad Reza; Clark, Cain C. T.; Mirzaei, Khadijeh published the artcile< Effect of orlistat on serum uric acid level in adults: A systematic review and meta-analysis of randomised controlled trials>, Quality Control of 96829-58-2, the main research area is meta analysis orlistat uric acid reducing agent hyperuricemia.

Hyperuricemia increases the risk of gout and cardiovascular diseases. Obesity increases the risk of hyperuricemia while weight loss (>5 kg) has been reported to decrease urate. The effects of orlistat on serum uric acid (SUA) are still controversial. The aim of this meta-anal. was to evaluate the influence of orlistat on SUA levels in adults. Relevant studies, published up to May 2020, were searched systematically through PubMed/Medline, Scopus and Google Scholar. All relevant randomised controlled clin. trials were included. Meta-anal. was performed using random-effect model. Subgroup anal., sensitivity anal. and meta-regression were also carried out. Overall 7 trials (9 datasets) that enrolled 1786 subjects were included. Orlistat showed in a significant change in SUA level (Difference in means: -17.661μmol, 95% CI: -31.615 to -3.707, P = .01). A low heterogeneity observed across the studies (I2 = 25.119%). After categorising studies on the basis of duration and sample size, the effect of orlistat on SUA was significant. The results of meta-regression were showed that significant relationships were not found between orlistat and SUA in the duration of intervention. We found a significant reduction in SUA following orlistat therapy in adults.

International Journal of Clinical Practice published new progress about Adult, mammalian. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Quality Control of 96829-58-2.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Mohiuddin, Ghulam; Reddy, Padala Satyanarayana; Ahmed, Khalil; Ratnam, Chengalvala Venkata published the artcile< Intramolecular 1,3-dipolar cycloadditions. Part 1. A facile synthesis of benzimidazo[1,2-d]- and quinazolino[3,2-d][1,2,3]triazolo[1,5-a][1,4]benzodiazepines>, SDS of cas: 112253-70-0, the main research area is cycloaddition propargyl bromide azidophenylbenzimidazole azidophenylquinazolinone; benzimidazotriazolobenzodiazepine; quinazolinotriazolobenzodiazepine; triazolobenzodiazepine; benzodiazepinotriazole; cyclization azidobenzoate phenylenediamine; aminobenzamide cyclization azidobenzoate; benzamidobenzamide cyclization.

Cyclization of x,2-R1(N3)C6H3CO2H (R1 = H, 5-Br, 4-NO2) with diamine I (R2, R3 = H, Me) gave benzimidazole II, which cyclized with BrCH2CCH to give 9 III. IV (R1 = H, Me, Br, Cl; R2 = H, Br) were similarly prepared

Journal of Chemical Research, Synopses published new progress about 1,3-Dipolar cycloaddition reaction, intramolecular. 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, SDS of cas: 112253-70-0.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Gou, Quan; Liu, Zining; Cao, Tuanwu; Tan, Xiaoping; Shi, Wenbing; Ran, Man; Cheng, Feixiang; Qin, Jun published the artcile< Copper-Catalyzed Coupling of Sulfonamides with Alkylamines: Synthesis of (E)-N-Sulfonylformamidines>, Synthetic Route of 1524-40-9, the main research area is sulfonamide alkylamine copper catalyst diastereoselective coupling; sulfonylformamidine.

Herein, we describe an efficient copper-catalyzed coupling of sulfonamides with alkylamines to synthesize (E)-N-sulfonylformamidines. The reaction is accomplished under mild conditions without the use of a corrosive acid or base as an additive. It tolerates a broad scope of substrates and generates the products with exclusive (E)-stereoselectivity.

Journal of Organic Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Synthetic Route of 1524-40-9.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Polyzos, Stergios A.; Kountouras, Jannis; Mantzoros, Christos S. published the artcile< Obesity and nonalcoholic fatty liver disease: From pathophysiology to therapeutics>, Safety of (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is review obesity nonalcoholic fatty liver disease pathophysiol therapeutic; Adipose tissue; Metabolic syndrome; Nonalcoholic fatty liver disease; Nonalcoholic steatohepatitis; Obesity; Treatment.

A review. The obesity epidemic is closely associated with the rising prevalence and severity of nonalcoholic fatty liver disease (NAFLD): obesity has been linked not only with simple steatosis (SS), but also with advanced disease, i.e., nonalcoholic steatohepatitis (NASH), NASH-related cirrhosis and hepatocellular carcinoma. As a consequence, apart from increasing all-cause mortality, obesity seems to increase liver-specific mortality in NAFLD patients. Given the lack of approved pharmacol. interventions for NAFLD, targeting obesity is a rational option for its management. As the first step, lifestyle modification (diet and exercise) is recommended, although it is difficult to achieve and sustain. When the first step fails, adding pharmacotherapy is recommended. Several anti-obesity medications have been investigated in NAFLD (e.g., orlistat, glucagon-like peptide-1 analogs), other anti-obesity medications have not been investigated (e.g., lorcaserin, phentermine hydrochloric, phentermine/topiramate and naltrexone/bupropion), whereas some medications with weight-lowering efficacy have not been approved for obesity (e.g., sodium-glucose cotransporter-2 inhibitors, farnesoid X receptor ligands). If the combination of lifestyle modification and pharmacotherapy also fails, then bariatric surgery should be considered in selected morbidly obese individuals. This review summarizes best evidence linking obesity with NAFLD and presents related therapeutic options.

Metabolism, Clinical and Experimental published new progress about Antiobesity agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Safety of (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Wang, Chao-Jie; Guo, Xinxin; Zhai, Rui-Qin; Sun, Changning; Xiao, Guokai; Chen, Jin; Wei, Mei-Yan; Shao, Chang-Lun; Gu, Yuchao published the artcile< Discovery of penipanoid C-inspired 2-(3,4,5-trimethoxybenzoyl)quinazolin-4(3H)-one derivatives as potential anticancer agents by inhibiting cell proliferation and inducing apoptosis in hepatocellular carcinoma cells>, SDS of cas: 112253-70-0, the main research area is trimethoxybenzoyl quinazolinone anticancer discovery preparation human apoptosis; Apoptosis; Cell cycle; Hepatocellular carcinoma; Penipanoid C; Quinazoline.

Hepatocellular carcinoma (HCC) is the most common form of liver cancer and the fourth leading cause of cancer-related death worldwide. First-line drugs such as sorafenib provide only a modest benefit to HCC patients. In this study, the gram-scale synthesis of 2-benzoylquinazolin-4(3H)-one skeleton was achieved successfully via the I2/DMSO catalytic system. A series of penipanoid C-inspired 2-(3,4,5-trimethoxybenzoyl)quinazolin-4(3H)-one derivatives was synthesized and evaluated for their cytotoxic activities against four cancer cell lines, HepG2, Bel-7402, A549, and U251. Among these compounds, I was the most effective one with IC50 values of 1.22μM and 1.71μM against HepG2 and Bel-7402 cells, resp. Mechanistic studies showed that I inhibited hepatocellular carcinoma cell proliferation via arresting cell cycle. Addnl., I induced HepG2 cells apoptosis by inducing reactive oxygen species production and elevating the expression of apoptosis-related proteins. More importantly, I displayed significant in vivo anticancer effects in the HepG2 xenograft models. This suggests that I is a promising lead compound with the potential to be developed as a chemotherapy agent for hepatocellular carcinoma.

European Journal of Medicinal Chemistry published new progress about Acetophenones Role: RCT (Reactant), RACT (Reactant or Reagent). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, SDS of cas: 112253-70-0.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics