Tag: M.W=350-400

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

Lei, Yiting published the artcileShear-responsive boundary-lubricated hydrogels attenuate osteoarthritis, SDS of cas: 169590-42-5, the publication is Bioactive Materials (2022), 472-484, database is CAplus and MEDLINE.

Lipid-based boundary layers formed on liposome-containing hydrogels can facilitate lubrication. However, these boundary layers can be damaged by shear, resulting in decreased lubrication. Here, a shear-responsive boundary-lubricated drug-loaded hydrogel is created by incorporating celecoxib (CLX)-loaded liposomes within dynamic covalent bond-based hyaluronic acid (HA) hydrogels (CLX@Lipo@HA-gel). The dynamic cross-linked network enables the hydrogel to get restructured in response to shear, and the HA matrix allows the accumulation of internal liposome microreservoirs on the sliding surfaces, which results in the formation of boundary layers to provide stable lubrication. Moreover, hydration shells formed surrounding the hydrogel can retard the degradation process, thus helping in sustaining lubrication. Furthermore, in vitro and in vivo experiments found that CLX@Lipo@HA-gels can maintain anabolic-catabolic balance, alleviate cartilage wear, and attenuate osteoarthritis progression by delivering CLX and shear-responsive boundary lubrication. Overall, CLX@Lipo@HA-gels can serve as shear-responsive boundary lubricants and drug-delivery vehicles to alleviate friction-related diseases like osteoarthritis.

Bioactive Materials 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, SDS of cas: 169590-42-5.

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

Wang, Shiru published the artcileSuspect screening to support source identification and risk assessment of organic micropollutants in the aquatic environment of a Sub-Saharan African urban center, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Water Research (2022), 118706, database is CAplus and MEDLINE.

Organic micropollutants (OMPs) are contaminants of global concern and have garnered increasing attention in Africa, particularly in urban and urbanizing areas of Sub-Saharan Africa (SSA). In this work, we coupled suspect screening enabled by liquid chromatog.-high-resolution mass spectrometry (LC-HRMS) with multivariate anal. to characterize OMPs in wastewater, surface water, and groundwater samples collected from Kampala, the capital and largest city of Uganda. Suspect screening prioritized and confirmed 157 OMPs in Kampala samples for target quantification. Many OMPs detected in Kampala samples occurred within concentration ranges similar to those documented in previous studies reporting OMP occurrence in SSA, but some have never or rarely been quantified in environmental water samples from SSA. Hierarchical cluster anal. established the source-related co-occurrence profiles of OMPs. Partial least squares regression and multiple linear regression analyses further pinpointed the concentration of nitrate and the content of a fluorescent organic matter component with excitation/emission maxima around 280/330 nm as predictors for the sample-specific cumulative concentrations of OMPs, suggesting the likely contribution of diffuse runoff and wastewater discharges to OMP occurrence in the aquatic environment of Kampala. Parallel calculations of exposure-activity ratios and multi-substance potentially affected fractions provided insights into the potential for biol. effects associated with OMPs and highlighted the importance of expanded anal. coverage for screening-level risk assessments. Overall, our study demonstrates a versatile database-driven screening and data anal. methodol. for the multipronged characterization of OMP contamination in a representative SSA urban center.

Water Research 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 C4H6O3, 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

Hammel, Emily published the artcileImplications of PFAS definitions using fluorinated pharmaceuticals, COA of Formula: C17H14F3N3O2S, the publication is iScience (2022), 25(4), 104020, database is CAplus and MEDLINE.

There are 9,000+ per- and polyfluoroalkyl substances (PFAS) in existence, which makes studying and regulating PFAS individually, or even as small mixtures, infeasible. Multiple PFAS definitions based on structure have been proposed, yet these definitions do not consider the implications for the full suite of organofluorine chems. For example, organofluorine pharmaceuticals, whose use may be essential and are found in human serum and wastewater, are not uniformly identified across all definitions. Using nine definitions prepared by various stakeholders, we screened the 360 organofluorine pharmaceuticals approved and used globally between 1954 and 2021. Definitions ranged in their inclusion of organofluorine pharmaceuticals (1%-100%). The most inclusive definitions include several top prescribed pharmaceuticals, e.g., Prozac and Lipitor. This anal. provides a framework against which organizations can make decisions about how best to proceed when defining PFAS.

iScience 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, COA of Formula: C17H14F3N3O2S.

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

Alcain, Francisco J. published the artcileSirtuin inhibitors, Recommanded Product: N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, the publication is Expert Opinion on Therapeutic Patents (2009), 19(3), 283-294, database is CAplus and MEDLINE.

A review. Background: The sirtuin family of deacetylase enzymes comprises seven proteins (SIRT1-7) that are dependent on NAD⁺ for their activity. Three proteins are located in the nucleus, three in the mitochondria and only one is predominantly cytoplasmic. Caloric restriction and oxidative stress generally up-regulate their expression. SIRT1, the ortholog of yeast Sir2, is the mammalian sirtuin that has been most extensively studied to date. Among other targets, SIRT1 down-regulates the activity of the nuclear transcription factor p53, being this related with an increase in lifespan and cell survival associated to stress resistance. Objective: Because sirtuin modulation could have beneficial effects on several human diseases, there is a growing interest in the discovery and development of small mols. that modify its activity. This review will be focused on sirtuin inhibitors. Conclusions: Several specific inhibitors of SIRT1 have been described. These compounds could be mainly useful for the treatment of cancers by increasing p53 activity that stops the formation of tumors and induces apoptosis. A p53-independent massive induction of apoptosis has been also described for one inhibitor. In addition, a potent and selective SIRT2 inhibitor that ameliorates the α-synuclein fibril formation in Parkinson disease has been proposed to treat this kind of neurodegenerative disease.

Expert Opinion on Therapeutic Patents 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, Recommanded Product: N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide.

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

Kaneguchi, Akinori published the artcileBilateral muscle atrophy after anterior cruciate ligament reconstruction in rats: Protective effects of anti-inflammatory drug celecoxib., Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is The Knee (2022), 201-212, database is MEDLINE.

BACKGROUND: Muscle atrophy after anterior cruciate ligament (ACL) reconstruction occurs bilaterally and contributes to a decrease in muscle strength. However, effective treatment strategies for ACL reconstruction-induced muscle atrophy have not been established. We examined the effects of anti-inflammatory drug on muscle atrophy after ACL reconstruction. MATERIALS AND METHODS: Rats were divided into groups according to treatment received: untreated control (n = 4), arthrotomy (n = 6), ACL transection (n = 7), ACL reconstruction (n = 8), and ACL reconstruction plus anti-inflammatory drug celecoxib (CBX; 50 mg/kg/day) administration (n = 8). At one-week post-surgery, the muscle fiber cross-sectional area (CSA) in the rectus femoris (RF) and semitendinosus (ST) was measured to assess muscle atrophy. In addition, we examined joint swelling and serum C‑reactive protein (CRP) levels to assess local and systemic inflammation, respectively. RESULTS: Each additional procedure (i.e., arthrotomy, ACL transection, and ACL reconstruction) gradually decreased the muscle fiber CSAs in the RF and ST on both operated and contralateral sides. The degree of muscle fiber atrophy on the operated side was larger than that detected on the contralateral side. Moreover, ACL reconstruction induced joint swelling on the operated side and tended to increase serum CRP levels. CBX lessened the RF atrophy on both sides and was associated with less joint swelling and a smaller increase CRP level; however, it did not affect ST atrophy on either side. CONCLUSIONS: Anti-inflammatory treatments after ACL reconstruction may be effective in lessening muscle atrophy in the quadriceps, but not in the hamstrings.

The Knee 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, 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

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

Karikalan, Natarajan published the artcileSimultaneous in-situ extraction and electrochemical detection of antidepressant drug imipramine and its active metabolite in human biofluid samples, COA of Formula: C17H14F3N3O2S, the publication is Sensors and Actuators, B: Chemical (2022), 131960, database is CAplus.

The rapidly advancing modern healthcare system necessitates the development of cutting-edge technologies for therapeutic drug monitoring. Protein-bound drugs challenge the rapid quantification of anal. methods that require addnl. separation and cleanup processes, which delay the development of point-of-care testing platform. Here, a human serum albumin (HSA)/iron molybdate (FeM;Fe2(MoO4)3)/reduced graphene oxide (rGO) is reported for the in-situ extraction and determination of imipramine (IMP) drug and its active metabolite desipramine (DMP) in human serum and plasma samples. HSA was used for the extraction of drugs from the complex plasma proteins, and the extracted drugs were directly detected by FeM/rGO without addnl. sample cleanup. The developed sensor, which was optimized for the drug therapeutic window under normal conditions, exhibited a linear range of 10-756 ng/mL as well as a remarkable limit of detection and sensitivity of approx. 4 ± 2 ng/mL and 0.0124 ± 0.0003μA cm-2 ng-1 mL, resp., for IMP-DMP. The spike-and-recovery method was used to validate the developed sensor in real sample anal. Based on the results, the sensing mechanism was elucidated: protein-protein interaction facilitates drug transportation from the plasma protein to electrode surface. Thereby, the HSA-FeM/rGO modified electrode recovered more drugs in biofluids compared with HSA unmodified electrode.

Sensors and Actuators, B: Chemical 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, COA of Formula: C17H14F3N3O2S.

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