Month: February 2023

Adverse events secondary to cetuximab therapy in head & neck cancer therapy and risk factors for serious outcomes was written by Stanbouly, Dani;Philipone, Elizabeth;Morlandt, Anthony B.;Kaleem, Arshad;Chuang, Sung-Kiang;Patel, Neel. And the article was included in Oral Oncology in 2022.Name: 6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one This article mentions the following:

The objective of this study is to illustrate the adverse events secondary to cetuximab therapy for head and neck cancer and elucidate risk factors for serious outcomes. This retrospective study was conducted using the FDA Adverse Event Reporting System (FAERS). The predictor variables were patient characteristics, country of treatment, and adverse events. The outcome variable was the rate of serious outcomes. Multivariate logistic regression was created to identify all significant risk factors of the outcome. P < 0.05 was considered statistically significant. The final sample consisted of 3,086 reports of adverse events from cetuximab therapy in head and neck cancer treatment, of which 2,746 reports were considered serious (89.0%) per the FAERS criteria. Mucosal inflammation was the most common adverse event. The strongest risk factor for a serious outcome was cetuximab therapy in countries outside the US (OR 105.2, P < 0.01). Polytherapy (OR 7.6, P < 0.01) was also a risk factor for serious outcome. Health-care providers should be aware of potential complications following cetuximab administration, particularly when administered in countries outside the US and in conjunction with other medications. In the experiment, the researchers used many compounds, for example, 6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2Name: 6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one).

6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Name: 6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Population pharmacokinetic modelling of aripiprazole and its active metabolite, dehydroaripiprazole, in psychiatric patients was written by Kim, Jung-Ryul;Seo, Hyo-Bum;Cho, Joo-Youn;Kang, Do-Hyung;Kim, Yong Ku;Bahk, Won-Myong;Yu, Kyung-Sang;Shin, Sang-Goo;Kwon, Jun Soo;Jang, In-Jin. And the article was included in British Journal of Clinical Pharmacology in 2008.Safety of 7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one This article mentions the following:

The aims of this study were to develop a combined population pharmacokinetic model for both aripiprazole and its active metabolite, dehydroaripiprazole, in psychiatric patients and to identify to what extent the genetic polymorphisms of cytochrome P 450 (CYP) enzymes contribute to the variability in pharmacokinetics (PK). A population pharmacokinetic anal. was performed using NONMEM software based on 141 plasma concentrations at steady state from 80 patients receiving multiple oral doses of aripiprazole (10-30 mg day^-1). A one-compartment model with first-order kinetics for aripiprazole and dehydroaripiprazole each was developed to describe simultaneously the concentration data. The absorption rate constant was fixed to 1.06 h^-1. The typical value of apparent distribution volume of aripiprazole was estimated to be 192 I. Covariate anal. showed that CYP2D6 genetic polymorphisms significantly influenced the apparent clearance of aripiprazole (CL/F), reducing the interindividual variability on CL/F from 37.8% CV (coefficient of variation) to 30.5%. The CL/F in the CYP2D6 IMs was approx. 60% of that in CYP2D6 EMs having two functional alleles. Based on the CYP2D6 genotype, the metabolic ratios were calculated at 0.20-0.34. However, the plasma concentration: dose ratios of dehydroaripiprazole were not different across the CYP2D6 genotype. :This population pharmacokinetic model provided an adequate fit to the data for both aripiprazole and dehydroaripiprazole in psychiatric patients. The usefulness of CYP genotyping as an aid to select the starting dose should be further investigated. In the experiment, the researchers used many compounds, for example, 7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one (cas: 129722-25-4Safety of 7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one).

7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one (cas: 129722-25-4) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Safety of 7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Targeting the Src pathway enhances the efficacy of selective FGFR inhibitors in urothelial cancers with FGFR3 alterations was written by Lima, Nadia Carvalho;Atkinson, Eliza;Bunney, Tom D.;Katan, Matilda;Huang, Paul H.. And the article was included in International Journal of Molecular Sciences in 2020.Name: 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea This article mentions the following:

Selective FGFR inhibitors such as infigratinib (BGJ398) and erdafitinib (JNJ-42756493) have been evaluated in clin. trials for cancers with FGFR3 mol. alterations, particularly in urothelial carcinoma patients. However, a substantial proportion of these patients (up to 50%) display intrinsic resistance to these drugs and receive minimal clin. benefit. There is thus an unmet need for alternative therapeutic strategies to overcome primary resistance to selective FGFR inhibitors. In this study, we demonstrate that cells expressing cancer-associated activating FGFR3 mutants and the FGFR3-TACC3 fusion showed primary resistance to infigratinib in long-term colony formation assays in both NIH-3T3 and urothelial carcinoma models. We find that expression of these FGFR3 mol. alterations resulted in elevated constitutive Src activation compared to wildtype FGFR3 and that cells co-opted this pathway as a means to achieve intrinsic resistance to infigratinib. Targeting the Src pathway with low doses of the kinase inhibitor dasatinib synergistically sensitized multiple urothelial carcinoma lines harbouring endogenous FGFR3 alterations to infigratinib. Our data provide preclin. rationale that supports the use of dasatinib in combination with selective FGFR inhibitors as a means to overcome intrinsic drug resistance in the salvage therapy setting in urothelial cancer patients with FGFR3 mol. alterations. In the experiment, the researchers used many compounds, for example, 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea (cas: 872511-34-7Name: 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea).

3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea (cas: 872511-34-7) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Name: 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

A non-randomized study to investigate the effects of the atypical antipsychotic aripiprazole on the steady-state pharmacokinetics of lamotrigine in patients with bipolar I disorder was written by Schieber, Frank C.;Boulton, David W.;Balch, Alfred H.;Croop, Robert;Mallikaarjun, Suresh;Benson, Jeannine;Carlson, Berit X.. And the article was included in Human Psychopharmacology in 2009.Reference of 129722-25-4 This article mentions the following:

To determine the effect of aripiprazole on steady-state pharmacokinetics of lamotrigine in patients with bipolar I disorder who were clin. stable on lamotrigine (100-400 mg/day) for ≥4 wk. In this open-label study, aripiprazole was administered at 10 mg/day for 3 days, 20 mg/day for 3 days, then 30 mg/day for 8 days. Blood samples were collected on Days -1 and 14 for determination of lamotrigine steady-state pharmacokinetic parameters. Safety and tolerability were assessed. Eighteen patients were administered aripiprazole in combination with lamotrigine. Geometric mean (GM) values for lamotrigine maximum plasma concentration were similar for lamotrigine alone (26 ng/mL) and with co-administered aripiprazole (23 ng/mL). GM values for plasma lamotrigine area under the concentration-time curve (AUC*au) were comparable for lamotrigine alone (434 ng/h/mL) and with co-administered aripiprazole (394 ng/h/mL). Median T_max of lamotrigine alone and combined with aripiprazole was 1.98 and 0.77 h, resp. No changes to lamotrigine dose-normalized plasma trough concentrations were observed with co-administered aripiprazole. Sixteen patients (88.9%) experienced ≥1 adverse event (AE), the most common of which was insomnia (n = 6). Aripiprazole had no meaningful effect on lamotrigine steady-state pharmacokinetics in patients with bipolar I disorder. No dosage adjustment of lamotrigine is required and the combination was generally safe and well tolerated. In the experiment, the researchers used many compounds, for example, 7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one (cas: 129722-25-4Reference of 129722-25-4).

7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one (cas: 129722-25-4) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Reference of 129722-25-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Expression of GALNT8 and O-glycosylation of BMP receptor 1A suppress breast cancer cell proliferation by upregulating ERα levels was written by Huang, Tianmiao;Wu, Qiong;Huang, Huang;Zhang, Cheng;Wang, Liping;Wang, Lingyan;Liu, Yangzhi;Li, Wenli;Zhang, Jianing;Liu, Yubo. And the article was included in Biochimica et Biophysica Acta, General Subjects in 2022.Recommanded Product: 1062368-24-4 This article mentions the following:

Mucin-type O-glycosylation is one of the most abundant types of O-glycosylation and plays important roles in various human carcinomas, including breast cancer. A large family of polypeptide N-acetyl-α-galactosaminyltransferases (GALNTs) initiate and define sites of mucin-type O-glycosylation. However, the specific mechanisms underlying GALNT8 expression and its roles in tumorigenesis remain poorly characterized. GALNT8 expression was assessed in 140 breast cancer patients. Immunofluorescence, immunoprecipitation, lectin blot and quant. real-time PCR were used to investigate the expression of GALNT8 and its role in regulating estrogen receptor α (ERα) via bone morphogenetic protein (BMP) signaling. The expression of GALNT8 was associated with breast cancer patient survival. GALNT8 downregulation was associated with a reduction in ERα levels, while GALNT8 overexpression elevated the transcription and protein levels of ERα and suppressed colony formation, suggesting an important role of GALNT8 in cancer cell proliferation. Conversely, GALNT8 knockdown led to the inhibition of BMP/SMAD/RUNX2 axis, which decreased ERα transcription. Further anal. suggested that BMP receptor 1A (BMPR1A) was O-GalNAcylated. Sites mutation of BMPR1A indicated that Thr137 and Ser37/Ser39/Ser44/Thr49 of BMPR1A were the main O-glycosylation sites. Although we cannot exclude the indirect effect of GALNT8, our results demonstrated that the expression of GALNT8 and O-glycosylation of BMPR1A play key roles in regulating the activity of BMP/SMAD/RUNX2 signaling and ERα expression. These findings suggest that GALNT8 expression and abnormal O-GalNAcylation of BMPR1A increase ERα expression and suppress breast cancer cell proliferation by modulating the BMP signaling pathway. Our results identify the involvement of GALNT8 in regulating ERα expression. In the experiment, the researchers used many compounds, for example, 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline (cas: 1062368-24-4Recommanded Product: 1062368-24-4).

4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline (cas: 1062368-24-4) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Recommanded Product: 1062368-24-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

COVID-19 inpatients with psychiatric disorders: Real-world clinical recommendations from an expert team in consultation-liaison psychiatry was written by Anmella, G.;Arbelo, N.;Fico, G.;Murru, A.;Llach, C. D.;Madero, S.;Gomes-da-Costa, S.;Imaz, M. L.;Lopez-Pelayo, H.;Vieta, E.;Pintor, L.. And the article was included in Journal of Affective Disorders in 2020.Recommanded Product: 839712-12-8 This article mentions the following:

Background: The management of coronavirus disease 2019 (COVID-19) in patients with comorbid psychiatric disorders poses several challenges, especially regarding drug interactions. Methods: We report three representative case-scenarios on patients with psychiatric disorders and COVID-19 to provide a practical approach based on the existing literature and the clin. experience of an expert team in consultation-liaison psychiatry. Case-centered recommendations: Psychopharmacol. ongoing treatments should be prioritized and most doses should be reduced 25-50% of original dose if the patient receives lopinavir/ritonavir, with some exceptions including quetiapine, asenapine, olanzapine, sertraline, lamotrigine, bupropion, and methadone. If the psychopharmacol. usual doses are in the low-to-median range levels, a dose change during COVID-19 drugs co-administration is not recommended, but only ECG and clin. monitoring of adverse effects and drug levels if required. Furthermore, when introducing a psychopharmacol. drug, dose titration should be progressive, with ECG monitoring if cardiotoxic interactions are present. (A) In agitated delirium, olanzapine is recommended as first-line antipsychotic and quetiapine should be avoided. (B) In severe mental illness (SMI), essential treatments should be maintained. (C) In non-SMI with depressive/anxiety symptoms, psychol. support should be provided and symptoms identified and treated. Limitations: Most recommendations on pharmacol. interactions provide only a limited qual. approach and quant. recommendations are lacking. Conclusions: Patients with psychiatric disorders and COVID-19 should be managed on a personalized basis considering several clin. criteria and, should not be excluded from receiving COVID-19 treatments. Risks of pharmacol. interaction are not absolute and should be contextualized, and most psychopharmacol. treatments should include an ECG with special attention to QTc interval. In the experiment, the researchers used many compounds, for example, 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8Recommanded Product: 839712-12-8).

3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Recommanded Product: 839712-12-8

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Multimodal antidepressant vortioxetine increases frontal cortical oscillations unlike escitalopram and duloxetine – a quantitative EEG study in rats was written by Leiser, S. C.;Pehrson, A. L.;Robichaud, P. J.;Sanchez, C.. And the article was included in British Journal of Pharmacology in 2014.Name: (R)-3-((2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)phenol hydrochloride This article mentions the following:

Background and Purpose : EEG studies show that 5-HT is involved in regulation of sleep-wake state and modulates cortical oscillations. Vortioxetine is a 5-HT3, 5-HT7, and 5-HT1D receptor antagonist, 5-HT1B partial agonist, 5-HT1A agonist, and 5-HT transporter inhibitor. Preclin. (animal) and clin. studies with vortioxetine show pos. impact on cognitive metrics involving cortical function. Here we assess vortioxetine’s effect on cortical neuronal oscillations in actively awake rats. Exptl. Approach : Telemetric EEG recordings were obtained with the following treatments (mg·kg^-1, s.c.): vehicle, vortioxetine (0.1, 1.0, 3.0, 10), 5-HT1A agonist flesinoxan (2.5), 5-HT3 antagonist ondansetron (0.30), 5-HT7 antagonist SB-269970-A (10), escitalopram (2.0), duloxetine (10) and vortioxetine plus flesinoxan. Target occupancies were determined by ex vivo autoradiog. Key Results : Vortioxetine dose-dependently increased wakefulness. Flesinoxan, duloxetine, ondansetron, but not escitalopram or SB-269970-A increased wakefulness. Quant. spectral analyses showed vortioxetine alone and with flesinoxan increased θ (4-8 Hz), α (8-12 Hz) and γ (30-50 Hz) power. Duloxetine had no effect on θ and γ, but decreased α power, while escitalopram produced no changes. Ondansetron and SB-269970 (≈31-35% occupancy) increased θ power. Flesinoxan (≈41% occupancy) increased θ and γ power. Conclusions and Implications : Vortioxetine increased wakefulness and increased frontal cortical activity, most likely because of its 5-HT7 and 5-HT3 antagonism and 5-HT1A agonism. Vortioxetine differs from escitalopram and duloxetine by increasing cortical θ, α and γ oscillations. These preclin. findings suggest a role of vortioxetine in modulating cortical circuits known to be recruited during cognitive behaviors and warrant further investigation as to their clin. impact. In the experiment, the researchers used many compounds, for example, (R)-3-((2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)phenol hydrochloride (cas: 261901-57-9Name: (R)-3-((2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)phenol hydrochloride).

(R)-3-((2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)phenol hydrochloride (cas: 261901-57-9) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Name: (R)-3-((2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)phenol hydrochloride

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

In vitro activity of eravacycline and cefoperazone/ sulbactam against extensively-drug resistant and pan-drug resistant Acinetobacter baumannii isolates from a tertiary hospital in Greece. was written by Meletis, Georgios;Protonotariou, Efthymia;Gkeka, Ioanna;Kassomenaki, Angeliki;Mantzana, Paraskevi;Tychala, Areti;Vlachodimou, Nikoletta;Kourti, Anastasia;Skoura, Lemonia. And the article was included in The new microbiologica in 2022.Computed Properties of C25H27N9O8S2 This article mentions the following:

We evaluated the in vitro activity of eravacycline and cefoperazone/sulbactam against 42 XDR and 58 PDR Acinetobacter baumannii isolates from blood and bronchoalveolar infections. The minimum and maximum MICs for eravacycline were 0.125 and 4 mg/L, respectively. The MIC50 was 2 mg/L and the MIC90 was 3 mg/L. The minimum and maximum MICs for cefoperazone/sulbactam were 24 and >256 mg/L, respectively. The MIC50 and MIC90 were both >256 mg/L. These novel agents were not adequate for the treatment of A. baumannii infections in our hospital and we recommend that mi- crobiology laboratories perform their own evaluations before including them in clinical practice. In the experiment, the researchers used many compounds, for example, (6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (cas: 62893-19-0Computed Properties of C25H27N9O8S2).

(6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (cas: 62893-19-0) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Computed Properties of C25H27N9O8S2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Synthesis and in-vitro study of novel (Z)-1-benzhydryl-4-cinnamylpiperazine derivatives as potential anticancer agents was written by Shivaprakash, S.;Kiran, K. R.;Diwakar, Latha;Reddy, G. Chandrasekara. And the article was included in International Journal of Pharmacy and Pharmaceutical Sciences in 2015.Related Products of 27469-60-9 This article mentions the following:

A series of novel (Z)-1-benzhydryl-4-cinnamylpiperazines I [R¹ = R² = Ph, 4-ClC₆H₄, 4-MeC₆H₄, 4-FC₆H₄; R¹ = Ph, R² = 4-ClC₆H₄, 4-BrC₆H₄; R³ = Ph, 4-MeOC₆H₄, 3,5-(MeO)₂C₆H₃, piperonyl, etc.] was synthesized in six steps starting from the corresponding benzophenones R¹COR². The final step was Wittig condensation of the appropriate benzyltriphenylphosphonium halides R³CH₂P⁺Ph₃ X^– (X = Cl, Br) with 1-benzhydryl-4-(formylmethyl)piperazines, which afforded pure (Z)-1-benzhydryl-4-cinnamylpiperazines I. The anticancer potential (MTT assay) of the synthesized compounds was tested against human cervical cancer (HeLa) and murine microglial (BV-2) cell lines. The compound I (R¹ = R² = 4-FC₆H₄; R³ = Ph) (cis-flunarizine) exhibited exceptionally superior activity against both HeLa and BV-2 cell lines with IC₅₀ value of 13.23±3.51 μM and 23.1±4.12 μM, resp. Hence, this compound may be considered as a potential lead mol. for further development. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9Related Products of 27469-60-9).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Related Products of 27469-60-9

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Targeted AntiBiotics for Chronic pulmonary diseases (TARGET ABC): can targeted antibiotic therapy improve the prognosis of Pseudomonas aeruginosa-infected patients with chronic pulmonary obstructive disease, non-cystic fibrosis bronchiectasis, and asthma? A multicenter, randomized, controlled, open-label trial was written by Eklof, Josefin;Alispahic, Imane Achir;Sivapalan, Pradeesh;Wilcke, Torgny;Seersholm, Niels;Armbruster, Karin;Kjaergaard, Jakob Lyngby;Saeed, Mohamad Isam;Nielsen, Thyge Lynghoej;Browatzki, Andrea;Overgaard, Rikke Holmen;Fenlev, Camilla Sund;Harboe, Zitta Barella;Andreassen, Helle Frost;Lapperre, Therese Sophie;Pedersen, Lars;Johnsen, Stine;Ulrik, Charlotte Suppli;Janner, Julie;Moberg, Mia;Heidemann, Maria;Weinreich, Ulla Moeller;Vijdea, Roxana;Linde, Hans;Titlestad, Ingrid;Johansson, Sofie Lock;Rosenvinge, Flemming Schoenning;Oestergaard, Christian;Ghathian, Khaled Saoud Ali;Gundersen, Lise;Christensen, Christina Wellendorph;Bangsborg, Jette;Jensen, Torben Tranborg;Soerensen, Vibeke Muff;Ellingsgaard, Thilde;Datcu, Raluca;Coia, John Eugenio;Bodtger, Uffe;Jensen, Jens Ulrik Staehr. And the article was included in Trials in 2022.Synthetic Route of C17H18FN3O3 This article mentions the following:

Abstract: Background: Pseudomonas aeruginosa infection is seen in chronic pulmonary disease and is associated with exacerbations and poor long-term prognosis. However, evidence-based guidelines for the management and treatment of P. aeruginosa infection in chronic, non-cystic fibrosis (CF) pulmonary disease are lacking. The aim of this study is to investigate whether targeted antibiotic treatment against P. aeruginosa can reduce exacerbations and mortality in patients with chronic obstructive pulmonary disease (COPD), non-CF bronchiectasis, and asthma. Methods: This study is an ongoing multicenter, randomized, controlled, open-label trial. A total of 150 patients with COPD, non-CF bronchiectasis or asthma, and P. aeruginosa-pos. lower respiratory tract samples will be randomly assigned with a 1:1 ratio to either no antibiotic treatment or anti-pseudomonal antibiotic treatment with i.v. beta-lactam and oral ciprofloxacin for 14 days. The primary outcome, analyzed with two co-primary endpoints, is (i) time to prednisolone and/or antibiotic requiring exacerbation or death, in the primary or secondary health sector, within days 20-365 from study allocation and (ii) days alive and without exacerbation within days 20-365 from the study allocation. Discussion: This trial will determine whether targeted antibiotics can benefit future patients with chronic, non-CF pulmonary disease and P. aeruginosa infection in terms of reduced morbidity and mortality, thus optimizing therapeutic approaches in this large group of chronic patients. Trial registration: ClinicalTrials.gov NCT03262142. Registered on August 25, 2017. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 85721-33-1Synthetic Route of C17H18FN3O3).

1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 85721-33-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Synthetic Route of C17H18FN3O3

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics