Tag: 370.5745

Allosteric Activators of Protein Phosphatase 2A Display Broad Antitumor Activity Mediated by Dephosphorylation of MYBL2 was written by Morita, Ken;He, Shuning;Nowak, Radoslaw P.;Wang, Jinhua;Zimmerman, Mark W.;Fu, Cong;Durbin, Adam D.;Martel, Megan W.;Prutsch, Nicole;Gray, Nathanael S.;Fischer, Eric S.;Look, A. Thomas. And the article was included in Cell (Cambridge, MA, United States) in 2020.Recommanded Product: 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine This article mentions the following:

Protein phosphatase 2A (PP2A) enzymes can suppress tumors, but they are often inactivated in human cancers overexpressing inhibitory proteins. Here, we identify a class of small-mol. iHAPs (improved heterocyclic activators of PP2A) that kill leukemia cells by allosterically assembling a specific heterotrimeric PP2A holoenzyme consisting of PPP2R1A (scaffold), PPP2R5E (B56蔚, regulatory), and PPP2CA (catalytic) subunits. One compound, iHAP1, activates this complex but does not inhibit dopamine receptor D2, a mediator of neurol. toxicity induced by perphenazine and related neuroleptics. The PP2A complex activated by iHAP1 dephosphorylates the MYBL2 transcription factor on Ser241, causing irreversible arrest of leukemia and other cancer cells in prometaphase. In contrast, SMAPs, a sep. class of compounds, activate PP2A holoenzymes containing a different regulatory subunit, do not dephosphorylate MYBL2, and arrest tumor cells in G1 phase. Our findings demonstrate that small mols. can serve as allosteric switches to activate distinct PP2A complexes with unique substrates. In the experiment, the researchers used many compounds, for example, 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2Recommanded Product: 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine).

10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Recommanded Product: 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis of the Enantiomers of Thioridazine was written by Antonsen, Simen;Monsen, Erling B.;Ovchinnikov, Kirill;Nolsoee, Jens M. J.;Ekeberg, Dag;Kristiansen, Jette E.;Diep, Dzung B.;Stenstroem, Yngve. And the article was included in SynOpen in 2020.Quality Control of 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine This article mentions the following:

Herein, an auxiliary-based strategy is used for the total synthesis of both enantiomers (+)-thioridazine and (-)-thioridazine in high optical purity and good overall yield. The strategy can easily be scaled up. Both enantiomers were tested against several bacteria. Comparison of the racemic mixture, (-)-thioridazine and its (+)-antipode revealed that they have the same antimicrobial effects. Thus, the non-toxic enantiomer, (-)-thioridazine, can prove useful in this role and should be investigated further. In the experiment, the researchers used many compounds, for example, 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2Quality Control of 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine).

10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Quality Control of 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Roles of lysosomotropic agents on LRRK2 activation and Rab10 phosphorylation was written by Kuwahara, Tomoki;Funakawa, Kai;Komori, Tadayuki;Sakurai, Maria;Yoshii, Gen;Eguchi, Tomoya;Fukuda, Mitsunori;Iwatsubo, Takeshi. And the article was included in Neurobiology of Disease in 2020.Computed Properties of C21H26N2S2 This article mentions the following:

Leucine-rich repeat kinase 2 (LRRK2), the major causative gene product of autosomal-dominant Parkinson′s disease, is a protein kinase that phosphorylates a subset of Rab GTPases. Since pathogenic LRRK2 mutations increase its ability to phosphorylate Rab GTPases, elucidating the mechanisms of how Rab phosphorylation is regulated by LRRK2 is of great importance. We have previously reported that chloroquine-induced lysosomal stress facilitates LRRK2 phosphorylation of Rab10 to maintain lysosomal homeostasis. Here we reveal that Rab10 phosphorylation by LRRK2 is potently stimulated by treatment of cells with a set of lysosome stressors and clin. used lysosomotropic drugs. These agents commonly promoted the formation of LRRK2-coated enlarged lysosomes and extracellular release of lysosomal enzyme cathepsin B, the latter being dependent on LRRK2 kinase activity. In contrast to the increase in Rab10 phosphorylation, treatment with lysosomotropic drugs did not increase the enzymic activity of LRRK2, as monitored by its autophosphorylation at Ser1292 residue, but rather enhanced the mol. proximity between LRRK2 and its substrate Rab GTPases on the cytosolic surface of lysosomes. Lysosomotropic drug-induced upregulation of Rab10 phosphorylation was likely a downstream event of Rab29 (Rab7L1)-mediated enzymic activation of LRRK2. These results suggest a regulated process of Rab10 phosphorylation by LRRK2 that is associated with lysosomal overload stress, and provide insights into the novel strategies to halt the aberrant upregulation of LRRK2 kinase activity. In the experiment, the researchers used many compounds, for example, 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2Computed Properties of C21H26N2S2).

10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Computed Properties of C21H26N2S2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Absence, loss-of-function, or inhibition of Escherichia coli AcrB does not increase expression of other efflux pump genes supporting the discovery of AcrB inhibitors as antibiotic adjuvants was written by Ciusa, Maria Laura;Marshall, Robert L.;Ricci, Vito;Stone, Jack W.;Piddock, Laura J. V.. And the article was included in Journal of Antimicrobial Chemotherapy in 2022.HPLC of Formula: 50-52-2 This article mentions the following:

To determine whether expression of efflux pumps and antibiotic susceptibility are altered in Escherichia coli in response to efflux inhibition. The promoter regions of nine efflux pump genes (acrAB, acrD, acrEF, emrAB, macAB, cusCFBA, mdtK, mdtABC, mdfA) were fused to gfp in pMW82 and fluorescence from each reporter construct was used as a measure of the transcriptional response to conditions in which AcrB was inhibited, absent or made non-functional. Expression was also determined by RT-qPCR. Drug susceptibility of efflux pump mutants with missense mutations known or predicted to cause loss of function of the encoded efflux pump was investigated. Data from the GFP reporter constructs revealed that no increased expression of the tested efflux pump genes was observed when AcrB was absent, made non-functional, or inhibited by an efflux pump inhibitor/competitive substrate, such as PAβN or chlorpromazine. This was confirmed by RT-qPCR for PAβN and chlorpromazine; however, a small but significant increase in macB gene expression was seen when acrB is deleted. Efflux inhibitors only synergized with antibiotics in the presence of a functional AcrB. When AcrB was absent or non-functional, there was no impact on MICs when other efflux pumps were also made non-functional. Absence, loss-of-function, or inhibition of E. coli AcrB did not significantly increase expression of other efflux pump genes, which suggests there is no compensatory mechanism to overcome efflux inhibition and supports the discovery of inhibitors of AcrB as antibiotic adjuvants. In the experiment, the researchers used many compounds, for example, 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2HPLC of Formula: 50-52-2).

10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.HPLC of Formula: 50-52-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Diterpenoid Vinigrol specifically activates ATF4/DDIT3-mediated PERK arm of unfolded protein response to drive non-apoptotic death of breast cancer cells was written by Wei, Wencheng;Li, Yunfei;Wang, Chuanxi;Gao, Sanxing;Zhao, Yan;Yang, Zhenyu;Wang, Hao;Gao, Ziying;Jiang, Yanxiang;He, Yuan;Zhao, Li;Gao, Hao;Yao, Xinsheng;Hu, Yuhui. And the article was included in Pharmacological Research in 2022.HPLC of Formula: 50-52-2 This article mentions the following:

Vinigrol is a natural diterpenoid with unprecedented chem. structure, driving great efforts into its total synthesis in the past decades. Despite anti-hypertension and anti-clot ever reported, comprehensive investigations on bioactions and mol. mechanisms of Vinigrol are entirely missing. Here we firstly carried out a complete functional prediction of Vinigrol using a transcriptome-based strategy coupled with multiple bioinformatic analyses and identified “anti-cancer” as the most prominent biofunction ahead of anti-hypertension and anti-depression/psychosis. Broad cytotoxicity was subsequently confirmed on multiple cancer types. Further mechanistic investigation on several breast cancer cells revealed that its anti-cancer effect was mainly through activating PERK/eIF2α arm of unfolded protein response (UPR) and subsequent non-apoptotic cell death independent of caspase activities. The other two branches of UPR, IRE1α and ATF6, were functionally irrelevant to Vinigrol-induced cell death. Using CRISPR/Cas9-based gene activation, repression, and knockout systems, we identified the essential contribution of ATF4 and DDIT3, not ATF6, to the death process. This study unraveled a broad anti-cancer function of Vinigrol and its underlying targets and regulatory mechanisms. It paved the way for further inspection on the structure-efficacy relationship of the whole compound family, making them a novel cluster of PERK-specific stress activators for exptl. and clin. uses. In the experiment, the researchers used many compounds, for example, 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2HPLC of Formula: 50-52-2).

10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.HPLC of Formula: 50-52-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Screened antipsychotic drugs inhibit SARS-CoV-2 binding with ACE2 in vitro was written by Lu, Jiayu;Hou, Yajing;Ge, Shuai;Wang, Xiangjun;Wang, Jue;Hu, Tian;Lv, Yuexin;He, Huaizhen;Wang, Cheng. And the article was included in Life Sciences in 2021.HPLC of Formula: 50-52-2 This article mentions the following:

The coronavirus disease 2019 (COVID-19) pandemic has swept the globe and no specific effective drug has been identified. Drug repurposing is a well-known method to address the crisis in a time-critical fashion. Antipsychotic drugs (APDs) have been reported to inhibit DNA replication of hepatitis B virus, measles virus germination, and HIV infection, along with replication of SARS-CoV and MERS-CoV, both of which interact with host cells as SARS-CoV-2. Nineteen APDs were screened using ACE2-HEK293T cell membrane chromatog. (ACE2-HEK293T/CMC). Cytotoxicity assay, coronavirus spike pseudotype virus entry assay, surface plasmon resonance, and virtual mol. docking were applied to detect affinity between ACE2 protein and drugs and a potential antiviral property of the screened compounds After the CMC screening, 8 of the 19 APDs were well-retained on ACE2-HEK293T/CMC column and showed significant antiviral activities in vitro. Three quarters of them belong to phenothiazine and could significantly inhibit the entrance of coronavirus into ACE2-HEK293T cells. Two other drugs, aripiprazole and tiapride, exhibited weaker inhibition. We selected 5 of the drugs for subsequent evaluation. All 5 showed similar affinity to ACE2 and virtual mol. docking demonstrated they bound with different amino acids resp. on ACE2 which SARS-CoV-2 binds to. Eight APDs were screened for binding with ACE2, 5 of which demonstrated potential protective effects against SARS-CoV-2 through acting on ACE2. Although the 5 drugs have a weak ability to block SARS-CoV-2 with a single binding site, they may provide a synergistic effect in adjuvant therapy of COVID-19 infection. In the experiment, the researchers used many compounds, for example, 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2HPLC of Formula: 50-52-2).

10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.HPLC of Formula: 50-52-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Clinical predictors of the hypoglycemic effect of sodium-glucose co-transporter-2 inhibitors in hyperuricemic patients: a retrospective descriptive observational study was written by Hirai, Toshinori;Kawagoe, Yuya;Kei, Motoki;Ogawa, Ryuichi;Itoh, Toshimasa. And the article was included in Biological & Pharmaceutical Bulletin in 2020.Name: 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine This article mentions the following:

Sodium-glucose co-transporter-2 (SGLT2) inhibitors decrease glycated Hb (HbA1c) and prevent the progression of cardiovascular and kidney diseases. Because uric acid and electrolytes are physiol. similar to blood glucose in renal excretion, we assessed predictors for the hypoglycemic effect of SGLT2 inhibitor treatment by focusing on serum uric acid and serum electrolytes. We performed a retrospective descriptive observational study at the Tokyo Women’s Medical University, Medical Center East, from June 2015 to July 2018. Patients who received treatment with any type of SGLT2 inhibitor were selected, which included a total of 165 patients. The response to SGLT2 inhibitors defined as changes in HbA1c after SGLT2 inhibitor treatment was the main outcome measure. Multiple linear regression anal. was used to assess predictors for the hypoglycemic effect by SGLT2 inhibitors. Among the 165 patients, SGLT2 inhibitor treatment decreased HbA1c from 8.2 to 7.6% after 12 wk (p < 0.01). Furthermore, late response to SGLT2 inhibitors was associated with serum uric acid value (p = 0.047) and baseline HbA1c (p < 0.001). Serum uric acid did not vary during SGLT2 inhibitor treatment; specifically, the SGLT2 inhibitors did not reduce serum uric acid levels. There was no correlation between changes in serum uric acid and HbA1c (p = 0.13). Thus, this study showed that serum uric acid value is associated with the control of diabetes mellitus during SGLT2 inhibitor treatment. In the experiment, the researchers used many compounds, for example, 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2Name: 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine).

10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Name: 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Comparative study on retention behaviour and enantioresolution of basic and neutral structurally unrelated compounds with cellulose-based chiral stationary phases in reversed phase liquid chromatography-mass spectrometry conditions was written by Perez-Baeza, Mireia;Escuder-Gilabert, Laura;Martin-Biosca, Yolanda;Sagrado, Salvador;Medina-Hernandez, Maria Jose. And the article was included in Journal of Chromatography A in 2022.Category: piperidines This article mentions the following:

A comparative study on the retention behavior and enantioresoln. of 54 structurally unrelated neutral and basic compounds using five com. cellulose-based chiral stationary phases (CSPs) and hydro-organic mobile phases compatible with MS detection is performed. Four phenylcarbamate-type cellulose CSPs (cellulose tris(3,5-dimethylphenylcarbamate), Cell1; cellulose tris(3-chloro-4-methylphenylcarbamate), Cell2; cellulose tris(4-chloro-3-methylphenylcarbamate), Cell4 and cellulose tris(3,5- dichlorophenylcarbamate), Cell5) and one benzoate-type cellulose CSP (cellulose tris(4-methylbenzoate), Cell3) are assayed. Mobile phases consist of binary mixtures of methanol (30-90% MeOH) or acetonitrile (10-98% ACN) with 5 mM ammonium bicarbonate (pH = 8.0). The existence of reversed phase (RPLC) and hydrophilic interaction liquid chromatog. (HILIC) retention behavior domains is explored. In MeOH/H₂O mobile phases, for all compounds and CSPs, the typical RPLC retention behavior is observed When using ACN/H₂O mobile phases, for all compounds in all CSPs (even in the non-chlorinated CSPs) a U-shaped retention behavior depending on the ACN/H₂O content is observed which indicates the coexistence of the RPLC- (< 80% ACN) and HILIC- (∼80-98% ACN) domains. The magnitude of retention changes in both domains is related to the hydrophobicity of the compound as well as to the nature of the CSP. The study of the effect of the nature and concentration of the organic solvent, as well as the nature of the CSP on the enantioresoln. reveals that: (i) the use of MeOH/H₂O or ACN/H₂O greatly affects the enantioselectivity and enantioresoln. degree of the chromatog. systems, being, in general, better the results obtained with ACN/H₂O mobile phases. (ii) The ACN-RPLC-domain provides much better enantioresoln. than HILIC-domain. (iii) Cell2, especially with ACN/H₂O mobile phases, is the CSP that allows baseline enantioresoln. for a higher number of compounds (iv) Phenylcarbamate-type CSPs do not offer clear complementary enantioselectivity to that of Cell2. (v) Cell3 is the only CSP that provides marked complementary enantioselectivity to that of Cell2, almost orthogonal in MeOH/H₂O mobile phases. In the experiment, the researchers used many compounds, for example, 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2Category: piperidines).

10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Overcoming epithelial-mesenchymal transition-mediated drug resistance with monensin-based combined therapy in non-small cell lung cancer was written by Ochi, Kosuke;Suzawa, Ken;Tomida, Shuta;Shien, Kazuhiko;Takano, Jui;Miyauchi, Shunsaku;Takeda, Tatsuaki;Miura, Akihiro;Araki, Kota;Nakata, Kentaro;Yamamoto, Hiromasa;Okazaki, Mikio;Sugimoto, Seiichiro;Shien, Tadahiko;Yamane, Masaomi;Azuma, Kazuo;Okamoto, Yoshiharu;Toyooka, Shinichi. And the article was included in Biochemical and Biophysical Research Communications in 2020.Synthetic Route of C21H26N2S2 This article mentions the following:

The epithelial-mesenchymal transition (EMT) is a key process in tumor progression and metastasis and is also associated with drug resistance. Thus, controlling EMT status is a research of interest to conquer the malignant tumors. A drug repositioning anal. of transcriptomic data from a public cell line database identified monensin, a widely used in veterinary medicine, as a candidate EMT inhibitor that suppresses the conversion of the EMT phenotype. Using TGF-induced EMT cell line models, the effects of monensin on the EMT status and EMT-mediated drug resistance were assessed. Tgf treatment induced EMT in non-small cell lung cancer (NSCLC) cell lines and the EGFR-mutant NSCLC cell lines with TGF-induced EMT acquired resistance to EGFR-tyrosine kinase inhibitor. The addition of monensin effectively suppressed the TGF-induced-EMT conversion, and restored the growth inhibition and the induction of apoptosis by the EGFR-tyrosine kinase inhibitor. Our data suggested that combined therapy with monensin might be a useful strategy for preventing EMT-mediated acquired drug resistance. In the experiment, the researchers used many compounds, for example, 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2Synthetic Route of C21H26N2S2).

10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Synthetic Route of C21H26N2S2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Ethidium bromide exposure unmasks an antibiotic efflux system in Rhodococcus equi was written by Rampacci, Elisa;Marenzoni, Maria Luisa;Cannalire, Rolando;Pietrella, Donatella;Sabatini, Stefano;Giovagnoli, Stefano;Felicetti, Tommaso;Pepe, Marco;Passamonti, Fabrizio. And the article was included in Journal of Antimicrobial Chemotherapy in 2021.Application In Synthesis of 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine This article mentions the following:

This study introduces a newly created strain (Rhodococcus equiEtBr25) by exposing R. equi ATCC 33701 to ethidium bromide (EtBr), a substrate for MDR transporters. Such an approach allowed us to investigate the resulting phenotype and genetic mechanisms underlying the efflux-mediated resistance in R. equi. R. equi ATCC 33701 was stimulated with increasing concentrations of EtBr. The antimicrobial susceptibility of the parental strain and R. equiEtBr25 was investigated in the presence/absence of efflux pump inhibitors (EPIs). EtBr efflux was evaluated by EtBr-agar method and flow cytometry. The presence of efflux pump genes was determined by conventional PCR before to quantify the expression of 30 genes coding for membrane transporters by qPCR. The presence of erm(46) and mutations in 23S rRNA, and gyrA/gyrB was assessed by PCR and DNA sequencing to exclude the occurrence of resistance mechanisms other than efflux. R. equiEtBr25 showed an increased EtBr efflux. Against this strain, the activity of EtBr, azithromycin and ciprofloxacin was more affected than that of rifampicin and azithromycin/rifampicin combinations. Resistances were reversed by combining the antimicrobials with EPIs. Gene expression anal. detected a marked up-regulation of REQ_RS13460 encoding for a Major Facilitator Superfamily (MFS) transporter. G→A transition occurred in the transcriptional repressor tetR/acrR adjacent to REQ_RS13460. Exposure of R. equi to EtBr unmasked an efflux-mediated defense against azithromycin and ciprofloxacin, which seemingly correlates with the overexpression of a specific MFS transporter. This genotype may mirror an insidious low-level resistance of clin. important isolates that could be countered by EPI-based therapies. In the experiment, the researchers used many compounds, for example, 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2Application In Synthesis of 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine).

10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Application In Synthesis of 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem