Tag: M.W=200-350

Mogle, Prashant P. published the artcileThiazole derivatives containing compounds as curative agents for tuberculosis: a review, Computed Properties of 55981-09-4, the main research area is review tuberculosis thiazole derivative compound curative agent.

Tuberculosis disease is the second main cause of deaths worldwide & become more dangerous because of increasing resistance towards novel anti-tubercular agents. In the last few decades, the number of development & research acomplished for the synthesis and biol. studies of novel anti-tubercular agents. Among heterocycles, thiazole is a versatile building block useful in the field of medicinal chem. Recently these compounds used for lead generation of future anti-tubercular agents having high effectiveness, potent anti-tubercular activity & possessing less toxicity. In this review, our focal point is to investigate the recent developments in the synthesis of thiazole derivatives & evaluate their biol. importance in anti-tubercular drug discovery. This review accessible for researchers which involves the rational designing of more potent anti-tubercular drugs containing thiazole moiety.

Heterocyclic Letters published new progress about Alkaloids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Computed Properties of 55981-09-4.

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

Palos, Isidro published the artcileEsters of quinoxaline-7-carboxylate-1,4-di-N-oxide as Trichomonas vaginalis triosephosphate isomerase inhibitors, HPLC of Formula: 55981-09-4, the main research area is Trichomonas vaginalis Esters quinoxaline carboxylate 4diNoxide triosephosphate isomerase inhibitor.

Trichomoniasis is a public health problem worldwide. Trichomoniasis treatment consists of the use of nitroimidazole derivatives; however, therapeutic ineffectiveness occurs in 5 to 20% of the cases. Therefore, it is essential to propose new pharmacol. agents against this disease. In this work, esters of quinoxaline-7-carboxylate-1,4-di-N-oxide (EQX-NO) were evaluated in in vitro assays as novel trichomonicidal agents. Addnl., an in vitro enzyme assay and mol. docking anal. against triosephosphate isomerase of Trichomonas vaginalis to confirm their mechanism of action were performed. Et (compound 12) and Pr (compound 37) esters of quinoxaline-7-carboxy-late-1,4-di-N-oxide derivatives showed trichomonicidal activity comparable to nitazoxanide, whereas five Me (compounds 5, 15, 19, 20 and 22), four iso-Pr (compounds 28, 29, 30 and 34), three Et (compounds 4, 13 and 23) and one npropyl (compound 35) ester derivatives displayed activity comparable to albendazole. Compounds 6 and 20 decreased 100% of the enzyme activity of recombinant protein triosephosphate isomerase.

Acta Pharmaceutica (Warsaw, Poland) published new progress about Amino acids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, HPLC of Formula: 55981-09-4.

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

El-Fadeal, Noha M. Abd published the artcileAntitumor activity of nitazoxanide against colon cancers: molecular docking and experimental studies based on Wnt/beta-catenin signaling inhibition, Quality Control of 55981-09-4, the main research area is antitumor activity nitazoxanide colon cancer mol docking signaling inhibition; PCNA; Wnt/β-catenin signaling; apoptosis; molecular docking; mouse colon cancer; nitazoxanide.

In colon cancer, wingless (Wnt)/ β-catenin signaling is frequently upregulated; however, the creation of a mol. therapeutic agent targeting this pathway is still under investigation. This research aimed to study how nitazoxanide can affect Wnt/ β-catenin signaling in colon cancer cells (HCT-116) and a mouse colon cancer model. Our study included 2 experiments; the first was to test the cytotoxic activity of nitazoxanide in an in vitro study on a colon cancer cell line (HCT-116) vs. normal colon cells (FHC) and to highlight the proapoptotic effect by MTT assay, flow cytometry and real-time polymerase chain reaction (RT-PCR). The second experiment tested the in vivo cytotoxic effect of nitazoxanide against 1,2-dimethylhydrazine (DMH) prompted cancer in mice. Mice were grouped as saline, DMH control and DMH + nitazoxanide [100 or 200 mg per kg]. Colon levels of Wnt and β-catenin proteins were assessed by Western blotting while proliferation was measured via immunostaining for proliferating cell nuclear antigen (PCNA). Treating HCT-116 cells with nitazoxanide (inhibitory concentration 50 (IC50) = 11.07 μM) revealed that it has a more cytotoxic effect when compared to 5-flurouracil (IC50 = 11.36 μM). Moreover, it showed relatively high IC50 value (non-cytotoxic) against the normal colon cells. Nitazoxanide induced apoptosis by 15.86-fold compared to control and arrested the cell cycle. Furthermore, nitazoxanide upregulated proapoptotic proteins (P53 and BAX) and caspases but downregulated BCL-2. Nitazoxanide downregulated Wnt/ β-catenin/glycogen synthase kinase-3β (GSK-3β) signaling and PCNA staining in the current mouse model. Hence, our findings highlighted the cytotoxic effect of nitazoxanide and pointed out the effect on Wnt/ β-catenin/GSK-3β signaling.

International Journal of Molecular Sciences published new progress about Amino acids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Quality Control of 55981-09-4.

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

Omolabi, Kehinde F. published the artcileA Mechanistic Probe into the Dual Inhibition of T. cruzi Glucokinase and Hexokinase in Chagas Disease Treatment – A Stone Killing Two Birds?, Product Details of C12H9N3O5S, the main research area is GLK2003 GLK2004 glucokinase hexokinase Chagas disease Trypanosoma; ADMET compliance.; Chagas disease; bioactive compounds; molecular dynamics simulation; thermodynamics calculation.

Glucokinase (GLK) and Hexokinase (HK) have been characterized as essential targets in Trypanosoma cruzi (Tc)-mediated infection. A recent study reported the propensity of the concomitant inhibition of TcGLK and TcHK by compounds GLK2-003 and GLK2-004, thereby presenting an efficient approach in Chagas disease treatment. We investigated this possibility using at. and mol. scaling methods. Sequence alignment of TcGLK and TcHK revealed that both proteins shared approx. 33.3% homol. in their glucose/inhibitor binding sites. The total binding free energies of GLK2-003 and GLK2-004 were favorable in both proteins. PRO92 and THR185 were pivotal to the binding and stabilization of the ligands in TcGLK, likewise their conserved counterparts, PRO163 and THR237 in TcHK. Both compounds also induced a similar pattern of perturbations in both TcGLK and TcHK secondary structure. Findings from this study therefore provide insights into the underlying mechanisms of dual inhibition exhibited by the compounds These results can pave way to discover and optimize novel dual Tc inhibitors with favorable pharmacokinetics properties eventuating in the mitigation of Chagas disease.

Chemistry & Biodiversity published new progress about Amino acids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Product Details of C12H9N3O5S.

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

Mifsud, Edin J. published the artcileProphylaxis of ferrets with nitazoxanide and oseltamivir combinations is more effective at reducing the impact of influenza a virus infection compared to oseltamivir monotherapy, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is influenza A virus infection kidney cell oseltamivir nitazoxanide.

Combination therapy is an alternative approach to reduce viral shedding and improve clin. outcomes following influenza virus infections. In this study we used oseltamivir (OST), a neuraminidase inhibitor and nitazoxanide (NTZ), a host directed drug, and found in vitro that the combination of these two antivirals have a synergistic relationship. Using the ferret model of (A/Perth/265/2009, (H1N1)pdm09), virus infections, we found that the combination of NTZ and OST was more effective than either NTZ or OST independently in preventing infection and reducing duration of viral shedding. However, these benefits were only seen if treatment was administered prophylactically, as opposed to therapeutically. We also found that if prophylactically treated ferrets that had detectable virus in the upper respiratory tract, no virus was detected in the lower respiratory tract. This benefit was not observed with NTZ or OST alone. The combination of NTZ and OST enhances the antiviral effect of OST, which is the standard of care in most settings.

Antiviral Research published new progress about Antiviral agents Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Fan, Lei published the artcileNitazoxanide, an anti-parasitic drug, efficiently ameliorates learning and memory impairments in AD model mice, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is nitazoxanide antiparasitic agent learning memory Alzheimer disease; APP/PS1 transgenic mice; Alzheimer’s disease; autophagy; inflammation; nitazoxanide.

The pathogenesis of Alzheimer′s disease (AD) is characterized by both accumulation of β-amyloid (Aβ) plaque and formation of neurofibrillary tangles in the brain. Recent evidence shows that autophagy activation may potently promote intracellular Aβ clearance. Thus targeting autophagy becomes a promising strategy for discovery of drug leads against AD. In the present study, we established a platform to discover autophagy stimulator and screened the lab inhouse FDA-approved drug library. We found that anti-parasitic drug nitazoxanide (NTZ) was an autophagy activator and could efficiently improve learning and memory impairments in APP/PS1 transgenic mice. In BV2 cells and primary cortical astrocytes, NTZ stimulated autophagy and promoted Aβ clearance by inhibiting both PI3K/AKT/mTOR/ULK1 and NQO1/mTOR/ULK1 signaling pathways; NTZ treatment attenuated LPS-induced inflammation by inhibiting PI3K/AKT/IκB/NFκB signaling. In SH-SY5Y cells and primary cortical neurons, NTZ treatment restrained tau hyperphosphorylation through inhibition of PI3K/AKT/GSK3β pathway. The beneficial effects and related signaling mechanisms from the in vitro studies were also observed in APP/PS1 transgenic mice following administration of NTZ (90 mg·kg-1·d-1, ig) for 100 days. Furthermore, NTZ administration decreased Aβ level and senile plaque formation in the hippocampus and cerebral cortex of APP/PS1 transgenic mice, and improved learning and memory impairments in Morris water maze assay. In conclusion, our results highlight the potential of NTZ in the treatment of AD.

Acta Pharmacologica Sinica published new progress about Alzheimer disease Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Siricilla, Shajila published the artcileComparative analysis of myometrial and vascular smooth muscle cells to determine optimal cells for use in drug discovery, Synthetic Route of 55981-09-4, the main research area is myometrial vascular smooth muscle cell drug discovery; Druggable transcriptome; High throughput; Intracellular calcium; Myometrium; Oxytocin; PHM1; Pregnancy; Preterm labor; RNA-sequencing; Tocolytic; Uterotonic; Vascular smooth muscle cells; hTERT-HM.

Novel therapeutic regulators of uterine contractility are needed to manage preterm labor, induce labor and control postpartum hemorrhage. Therefore, we previously developed a high-throughput assay for large-scale screening of small mol. compounds to regulate calcium-mobilization in primary mouse uterine myometrial cells. The goal of this study was to select the optimal myometrial cells for our high-throughput drug discovery assay, as well as determine the similarity or differences of myometrial cells to vascular smooth muscle cells (VSMCs)-the most common off-target of current myometrial therapeutics. Mol. and pharmacol. assays were used to compare myometrial cells from four sources: primary cells isolated from term pregnant human and murine myometrium, immortalized pregnant human myometrial (PHM-1) cells and immortalized non-pregnant human myometrial (hTERT-HM) cells. In addition, myometrial cells were compared to vascular SMCs. We found that the transcriptome profiles of hTERT-HM and PHM1 cells were most similar (r = 0.93 and 0.90, resp.) to human primary myometrial cells. Comparative transcriptome profiling of primary human myometrial transcriptome and VSMCs revealed 498 upregulated (p ≤ 0.01, log2FC≥1) genes, of which 142 can serve as uterine-selective druggable targets. In the high-throughput Ca2+-assay, PHM1 cells had the most similar response to primary human myometrial cells in OT-induced Ca2+-release (Emax = 195% and 143%, EC50 = 30 nM and 120 nM, resp.), while all sources of myometrial cells showed excellent and similar robustness and reproducibility (Z = 0.52 to 0.77). After testing a panel of 61 compounds, we found that the stimulatory and inhibitory responses of hTERT-HM cells were highly-correlated (r = 0.94 and 0.95, resp.) to human primary cells. Moreover, ten compounds were identified that displayed uterine-selectivity (≥5-fold Emax or EC50 compared to VSMCs). Collectively, this study found that hTERT-HM cells exhibited the most similarity to primary human myometrial cells and, therefore, is an optimal substitute for large-scale screening to identify novel therapeutic regulators of myometrial contractility. Moreover, VSMCs can serve as an important counter-screening tool to assess uterine-selectivity of targets and drugs given the similarity observed in the transcriptome and response to compounds

Pharmacological Research published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (CALD1). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Synthetic Route of 55981-09-4.

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

Kausar, Sharba published the artcileAntifilarial effect of nanocomposite of silver nanoparticles with nitazoxanide against the microfilariae of Setaria cervi-infected albino rats, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is diethylcarbamazine silver nanoparticle nitazoxanide Setaria filariasis; Anthelmintics; Antioxidant enzymes; Microfilariae; Nanoparticles; Setaria cervi.

Abstract: The aim of the present study was to assess the effect of diethylcarbamazine (DEC), siver nanoparticles (AgNPs), nitazoxanide (NTZ), and a combination of nitazoxanide with silver nanoparticle (NTZ+AgNPs) against the microfilariae of Setaria cervi in exptl. infected albino rats. The NTZ+AgNPs was synthesized and subsequently characterized by SEM (SEM), transmission electron microscopy (TEM), UV-visible absorption Spectra (UV-VIS), Fourier transforms IR spectroscopy (FTIR), and energy dispersive X-ray (EDX) spectra. Twenty male albino rats were divided into 5 groups. Groups I, II, III, and IV were treated with DEC, AgNPs, NTZ, and NTZ+AgNPs, while group V was taken as untreated infected control. After the establishment of infection, microfilaremic rats were treated with aforesaid drugs for 6 days at 100 mg/kg body weight Efficacy of drugs was observed by counting the microfilariae in the blood of albino rats every 3rd day till microfilariae disappeared. Blood was taken at every 10 days interval till 40 days for biochem. studies to assess the level of antioxidant enzymes. NTZ+AgNPs proved to be the most effective drug which cleared the microfilariae within 18 days of infection when compared with DEC, AgNPs and NTZ where microfilariae persisted up to 24, 36, and 33 days, resp. Oxidative stress is common inflammatory process associated with many diseases including filariasis. An enhanced antioxidant activity of NTZ+AgNPs was observed in the infected rats which was evident by quick disappearance of microfilariae due to increased oxidative stress. It clearly indicated pos. contribution of the NTZ+AgNPs to the host together with harmful effect on the parasite. Hence, AgNPs improved the NTZ efficacy against S. cervi infection in albino rats and proved as a successful synergistic combination.

Naunyn-Schmiedeberg’s Archives of Pharmacology published new progress about Combination chemotherapy. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Yu, Junhui published the artcileSynergistic tumor inhibition of colon cancer cells by nitazoxanide and obeticholic acid, a farnesoid X receptor ligand, SDS of cas: 55981-09-4, the main research area is nitazoxanide obeticholic acid synergistic tumor colon cancer FXR ligand.

The tumor-suppressive role of Farnesoid X receptor (FXR) in colorectal tumorigenesis supports restoring FXR expression as a novel therapeutic strategy. However, the complicated signaling network and tumor heterogeneity hinder the effectiveness of FXR agonists in the clin. setting. These difficulties highlight the importance of identifying drug combinations with potency and specificity to enhance the antitumor effects of FXR agonists. In this study, we found that the β-catenin level affected the antitumor effects of the FXR agonist OCA on colon cancer cells. Mechanistic studies identified a novel FXR/β-catenin complex in colon cancer cells. Furthermore, the depletion of β-catenin expedited FXR nuclear localization and enhanced its occupancy of the SHP promoter and thereby sensitized colon cancer cells to OCA. Furthermore, we utilized a drug combination study and identified that the antiparasitic drug nitazoxanide (NTZ) abrogated β-catenin expression and acted synergistically with OCA in colon cancer cells. The combination of OCA plus NTZ exerts synergistic tumor inhibition in CRC both in vitro and in vivo by cooperatively upregulating SHP expression. In conclusion, our study offers useful evidence for the clin. use of FXR agonists combined with β-catenin inhibitors in combating CRC.

Cancer Gene Therapy published new progress about Animal gene, c-myc Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, SDS of cas: 55981-09-4.

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

Hemmati-Dinarvand, Mohsen published the artcileNitazoxanide and Cancer Drug Resistance: Targeting Wnt/β-catenin Signaling Pathway, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is cancer nitazoxanide oxaliplatin drug resistance Wnt beta catenin chemotherapy; Colorectal cancer; Multidrug resistance; Nitazoxanid; Oxaliplatin; Wnt/β-catenin.

One of the most important complications that lead to unsuccessful treatment of cancer is resistance against chemotherapy agents, so called multidrug resistance (MDR). Thus, identification of the novel medications with low side effects and high efficacy to reverse MDR is highly required. Accordingly, the current study was performed to investigate the mol. mechanism of MDR in LS174T and LS174T/Oxaliplatin (OXP) cell lines during treatment with Nitazoxanide (NTZ) in combination with OXP. In the present in vitro study, we evaluated the effects of NTZ on the cytotoxicity of OXP using Thiazolyl Blue Tetrazolium Blue (MTT) assay in LS174T and LS174T/OXP cell lines when treated with OXP and NTZ, alone or in combination, for 24 and 48 h incubation. Then, we assessed the changes in the expression level of CTNNB1, ABCB1, c-Myc, and cyclin D1 genes in different treated groups. Exposure of LS174T/OXP cells to NTZ led to the elevation of cell sensitivity to OXP and induced caspase-3/7 activity, which results in apoptosis. Furthermore, NTZ downregulated Wnt/β-catenin signaling pathway through significant decrease of CTNNB1, c-Myc, ABCB1, and cyclin D1 genes and resulted in drug resistance reversal and inhibition of cell proliferation. These results indicate that Wnt/β-catenin pathway is important in developing cancer and MDR. In this regard, NTZ could reverse MDR in colorectal cancer (CRC) cells by downregulation of Wnt/β-catenin signaling pathway, suggesting that NTZ should be more considered in future studies as a potent adjuvant in CRC chemotherapy.

Archives of Medical Research published new progress about Animal gene, c-myc Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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