Month: February 2023

Antimicrobial resistance among Escherichia coli isolates from dogs presented with urinary tract infections at a veterinary teaching hospital in South Africa was written by Qekwana, Daniel Nenene;Phophi, Lufuno;Naidoo, Vinny;Oguttu, James Wabwire;Odoi, Agricola. And the article was included in BMC Veterinary Research in 2018.SDS of cas: 113617-63-3 This article mentions the following:

This study investigated the burden and predictors of canine E. coli urinary tract infections (UTI) and antimicrobial resistance among dogs presented at a veterinary teaching hospital in South Africa, 2007-2012. The Cochran-Armitage trend test was used to investigate temporal trends while logistic regression models were used to investigate predictors (age, sex, breed, year) of E. coli infections and antimicrobial resistance (AMR). A total of 22.3% (168/755) of the urinary specimens tested pos. for E. coli. A significant (p = 0.0004) decreasing temporal trend in the percentage of E. coli pos. isolates was observed over the study period. There were high levels of AMR to penicillin-G (99%), clindamycin (100%), tylosine (95%), cephalothin (84%) but relatively low levels of resistance to enrofloxacin (16%), orbifloxacin (21%). Almost all (98%, 164/167) the isolates exhibited multidrug resistance (MDR), while only 11% (19/167) and 2% (4/167) exhibited extensive drug resistance (XDR) and pan-drug resistance (PDR), resp. Although, the risk of E. coli UTI declined during the study period, the risk of AMR increased. The high levels of AMR and MDR as well as the presence of XDR and PDR is concerning as these have the potential of affecting prognosis of UTI treatments. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3SDS of cas: 113617-63-3).

1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳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. SDS of cas: 113617-63-3

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

Preparation and quality control of lomerizine hydrochloride capsules was written by Liu, Min-hong;Ding, Jian;Yao, Xiao-min;Li, Chen. And the article was included in Yaoxue Jinzhan in 2005.Reference of 101477-54-7 This article mentions the following:

A method for the preparation and quality control of lomerizine hydrochloride capsules was established. The preparation method for the capsules has been improved and the stability was also studied. The amount of lomerizine hydrochloride in capsules was determined by HPLC with an average recovery 99.7% (RSD=0.64%). The preparation procedure for lomerizine hydrochloride capsules is practicable and the quality control methods are reliable. In the experiment, the researchers used many compounds, for example, 1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride (cas: 101477-54-7Reference of 101477-54-7).

1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride (cas: 101477-54-7) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Reference of 101477-54-7

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

ODM-203, a selective inhibitor of FGFR and VEGFR, shows strong antitumor activity, and induces antitumor immunity was written by Holmstrom, Tim H.;Moilanen, Anu-Maarit;Ikonen, Tarja;Bjorkman, Mari L.;Linnanen, Tero;Wohlfahrt, Gerd;Karlsson, Stefan;Oksala, Riikka;Korjamo, Timo;Samajdar, Susanta;Rajagopalan, Srinivasan;Chelur, Shekar;Narayanan, Kishore;Ramachandra, Raghuveer K.;Mani, Jiju;Nair, Rashmi;Gowda, Nagaraj;Anthony, Thomas;Dhodheri, Samiulla;Mukherjee, Subhendu;Ujjinamatada, Ravi K.;Srinivas, Nanduri;Ramachandra, Murali;Kallio, Pekka J.. And the article was included in Molecular Cancer Therapeutics in 2019.Related Products of 1035270-39-3 This article mentions the following:

Alterations in the gene encoding for the FGFR and upregulation of the VEGFR are found often in cancer, which correlate with disease progression and unfavorable survival. In addition, FGFR and VEGFR signaling synergistically promote tumor angiogenesis, and activation of FGFR signaling has been described as functional compensatory angiogenic signal following development of resistance to VEGFR inhibition. Several selective small-mol. FGFR kinase inhibitors are currently in clin. development. ODM-203 is a novel, selective, and equipotent inhibitor of the FGFR and VEGFR families. In this report we show that ODM-203 inhibits FGFR and VEGFR family kinases selectively and with equal potency in the low nanomolar range (IC50 6-35 nmol/L) in biochem. assays. In cellular assays, ODM-203 inhibits VEGFR-induced tube formation (IC50 33 nmol/L) with similar potency as it inhibits proliferation in FGFR-dependent cell lines (IC50 50-150 nmol/L). In vivo, ODM-203 shows strong antitumor activity in both FGFR-dependent xenograft models and in an angiogenic xenograft model at similar well-tolerated doses. In addition, ODM-203 inhibits metastatic tumor growth in a highly angiogenesis-dependent kidney capsule syngenic model. In the experiment, the researchers used many compounds, for example, rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide (cas: 1035270-39-3Related Products of 1035270-39-3).

rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide (cas: 1035270-39-3) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Related Products of 1035270-39-3

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

The histamine H₁ receptor antagonist hydroxyzine enhances sevoflurane and propofol anesthesia: A quantitative EEG study. was written by Tanaka, Ryusuke;Tanaka, Satoshi;Hayashi, Kazuko;Iida, Keisuke;Sawa, Teiji;Kawamata, Mikito. And the article was included in Clinical neurophysiology in 2021.Recommanded Product: 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol This article mentions the following:

OBJECTIVE: The aim of this study was to determine the anesthesia-promoting effects of hydroxyzine on electroencephalograms during sevoflurane anesthesia and during propofol anesthesia. METHODS: We analyzed 40 patients scheduled for elective surgery under sevoflurane anesthesia (n鈥?鈥?0) or propofol anesthesia (n鈥?鈥?0). Anesthesia was adjusted at a bispectral index value of 50-60, and then 0.5鈥痬g/kg of hydroxyzine was administered intravenously. We analyzed frontal electroencephalograms before and after hydroxyzine injection with power spectral and bicoherence analyses, which are suitable for assessing the anesthetic depth induced by 纬-aminobutyric acid (GABA)ergic anesthetics. RESULTS: Hydroxyzine increased the 伪 bicoherence peaks in both sevoflurane anesthesia (mean difference, 11.2%; 95% confidence interval (CI), 7.6 to 14.8; P鈥?lt;鈥?.001) and propofol anesthesia (mean difference, 5.6%; 95% CI, 1.7 to 9.4; P鈥?鈥?.008). Hydroxyzine increased the averaged 未 bicoherence values in both sevoflurane anesthesia (mean difference, 5.5%; 95% CI, 2.1 to 8.8; P鈥?鈥?.003) and propofol anesthesia (mean difference, 3.9%; 95% CI, 1.0 to 6.8; P鈥?鈥?.011). CONCLUSIONS: Hydroxyzine enhances both sevoflurane anesthesia and propofol anesthesia probably by facilitation of GABAergic neural circuit mechanisms. SIGNIFICANCE: The findings provide a new insight into the role of histaminergic neurons during general anesthesia in humans. In the experiment, the researchers used many compounds, for example, 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol (cas: 68-88-2Recommanded Product: 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol).

2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol (cas: 68-88-2) 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. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Recommanded Product: 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol

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

Restoring order at the cell cycle border: Co-targeting CDK4/6 and CDK2 was written by Jeselsohn, Rinath;Schiff, Rachel;Grinshpun, Albert. And the article was included in Cancer Cell in 2021.Synthetic Route of C23H30N8O This article mentions the following:

Overcoming resistance to CDK4/6 inhibitors is a major clin. challenge. In this issue of Cancer Cell, Freeman-Cook et al. study mechanisms of resistance to CDK4/6 inhibitors by employing a CRISPRa screen. They identify the cyclin E-CDK2 axis and Myc signaling as key pathways of resistance and develop PF-06873600, a selective CDK2/4/6 inhibitor. In the experiment, the researchers used many compounds, for example, 7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide (cas: 1211441-98-3Synthetic Route of C23H30N8O).

7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide (cas: 1211441-98-3) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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. Synthetic Route of C23H30N8O

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

Synthesis of lomerizine dihydrochloride was written by Xu, Changsheng;Chen, Guohua;Luo, Xiaochuan. And the article was included in Zhongguo Yaoke Daxue Xuebao in 2002.Formula: C27H32Cl2F2N2O3 This article mentions the following:

Lomerizine dihydrochloride, a calcium antagonist used as antimigraine drug, was synthesized by methylating pyrogallic acid with di-Me sulfate to afford 1,2,3-trimethoxybenzene, chloromethylating with paraformaldehyde to afford 2,3,4-trimethoxybenzyl chloride, substituting with bis(4-fluorobenzyl)methylpiperazine in presence of triethylamine. Lomerizine dihydrochloride was obtained with 43% overall yield from pyrogallic acid. The structure of the compound was confirmed by IR, ¹H-NMR, MS, and elemental anal. In the experiment, the researchers used many compounds, for example, 1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride (cas: 101477-54-7Formula: C27H32Cl2F2N2O3).

1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride (cas: 101477-54-7) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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).Formula: C27H32Cl2F2N2O3

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

Optimization for QuEChERS extraction of mycotoxins and veterinary drugs by response surface methodology for application to egg and milk was written by Zhou, Jian;Xu, Jiao-Jiao;Cong, Jin-Mi;Cai, Zeng-Xuan;Zhang, Jing-Shun;Wang, Jun-Lin;Ren, Yi-Ping. And the article was included in Journal of Chromatography A in 2018.Formula: C19H20F3N3O3 This article mentions the following:

A multiclass method was proposed for the simultaneous determination of various classes of veterinary drugs (n = 65), mycotoxins and metabolites (n = 39) in egg and milk by ultra-high performance liquid chromatog.-tandem mass spectrometry. The contaminants were extracted by QuEChERS-based strategy including salt-out partitioning and dispersive solid-phase extraction for cleanup further. With the aim of maximizing throughput and extraction efficiency, Plackett-Burman design was employed initially for screening significant variables. And response surface methodol. based on central composite design was conducted to achieve optimal conditions in details: 3.35% (volume/volume) of formic acid in acetonitrile, 1.2 g of NaCl, 0.5 g of anhydrous NaAc, 300 mg of C18 and 140 mg of primary secondary amine. Satisfactory anal. characteristics in validation, in aspects of accuracy (70%-105% for mycotoxins and quinolones, 55%-80% for sulfonamides and 40%-105% for other veterinary drugs), precision (inter-day RSDs < 14%) and sensitivity (LOQs ranged from 0.01 渭g/kg to 31 渭g/kg), were achieved under the optimized conditions. The matrix effects were evaluated and compensated by the use of matrix-matched calibration curves (R² > 0.987). In practice, 45 eggs and 30 milk samples were investigated by the established method, of which pos. finding aflatoxin in milk and sterigmatocystin in eggs. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3Formula: C19H20F3N3O3).

1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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.Formula: C19H20F3N3O3

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

Copper iodide nanoparticles supported on magnetic aminomethylpyridine functionalized cellulose: a new heterogeneous and recyclable nanomagnetic catalyst for facile access to N-sulfonylamidines under solvent free conditions was written by Ghasemi, Zarrin;Shojaei, Salman;Shahrisa, Aziz. And the article was included in RSC Advances in 2016.Application of 14172-55-5 This article mentions the following:

In this study, a highly active catalyst based on copper iodide nanoparticles supported on magnetic aminomethylpyridine functionalized cellulose has been synthesized and characterized. Its catalytic activity was investigated in the multicomponent synthesis of N-sulfonylamidines via an in situ generated sulfonyl ketenimine intermediate under solvent free conditions at room temperature The desired products were obtained in good to excellent yields at short reaction times. Based on observed results, the synthesized catalyst was an efficient, magnetically separable, recyclable and green catalyst from a natural source. In the experiment, the researchers used many compounds, for example, 1-(Phenylsulfonyl)piperazine (cas: 14172-55-5Application of 14172-55-5).

1-(Phenylsulfonyl)piperazine (cas: 14172-55-5) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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).Application of 14172-55-5

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

Identification of Binding Specificity-Determining Features in Protein Families was written by Anderson, Peter C.;De Sapio, Vincent;Turner, Kevin B.;Elmer, Sidney P.;Roe, Diana C.;Schoeniger, Joseph S.. And the article was included in Journal of Medicinal Chemistry in 2012.Formula: C24H27FN6O4 This article mentions the following:

The authors present a new approach for identifying features of ligand-protein binding interfaces that predict binding selectivity and demonstrate its effectiveness for predicting kinase inhibitor specificity. The authors analyzed a large set of human kinases and kinase inhibitors using clustering of exptl. determined inhibition constants (to define specificity classes of kinases and inhibitors) and virtual ligand docking (to extract structural and chem. features of the ligand-protein binding interfaces). The authors then used statistical methods to identify features characteristic of each class. Machine learning was employed to determine which combinations of characteristic features were predictive of class membership and to predict binding specificities and affinities of new compounds Experiments showed predictions were 70% accurate. The authors’ method can automatically pinpoint on the three-dimensional binding interfaces pharmacophore-like features that act as selectivity filters. The method is not restricted to kinases, requires no prior hypotheses about specific interactions, and can be applied to any protein families for which sets of structures and ligand binding data are available. In the experiment, the researchers used many compounds, for example, 4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hydroxypropanoate (cas: 692737-80-7Formula: C24H27FN6O4).

4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hydroxypropanoate (cas: 692737-80-7) 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. 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.Formula: C24H27FN6O4

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

Efficacy of cariprazine on negative symptoms in patients with acute schizophrenia: A post hoc analysis of pooled data. was written by Earley, Willie;Guo, Hua;Daniel, David;Nasrallah, Henry;Durgam, Suresh;Zhong, Yan;Patel, Mehul;Barab谩ssy, 脕gota;Szatm谩ri, Bal谩zs;N茅meth, Gy枚rgy. And the article was included in Schizophrenia research in 2019.Safety of 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea This article mentions the following:

Although currently approved antipsychotics exert efficacy on positive symptoms of schizophrenia, treatments for negative symptoms remain a major unmet need. Post hoc analyses were used to investigate the possible efficacy of cariprazine in patients with moderate/severe negative symptoms of schizophrenia and no predominance of positive symptoms. Data were pooled from 2 randomized, double-blind, placebo- and active-controlled cariprazine studies in patients with acute schizophrenia (NCT00694707, NCT01104766). Analyses included data from a subset of patients with a Positive and Negative Syndrome Scale factor score for negative symptoms (PANSS-FSNS) 鈮?4, PANSS factor score for positive symptoms (PANSS-FSPS) 鈮?9, and scores of 鈮? on 鈮? of 3 PANSS items (blunted affect [N1], passive/apathetic social withdrawal [N4], lack of spontaneity/flow of conversation [N6]). Changes from baseline to week 6 in PANSS-FSNS were evaluated in the following treatment groups: placebo (n鈥?鈥?9), cariprazine 1.5-3 (n鈥?鈥?4) and 4.5-6鈥痬g/d (n鈥?鈥?6), risperidone 4鈥痬g/d (n鈥?鈥?4), or aripiprazole 10鈥痬g/d (n鈥?鈥?4). Significant differences were observed versus placebo for cariprazine (1.5-3鈥痬g/d, P鈥?鈥?0179; 4.5-6鈥痬g/d, P鈥?鈥?0002) and risperidone (P鈥?鈥?0149), but not aripiprazole (P鈥?鈥?3265), and versus aripiprazole for cariprazine 4.5-6鈥痬g/d (P鈥?鈥?0197). After adjusting for positive symptom changes, differences versus placebo remained statistically significant for cariprazine (1.5-3鈥痬g/d, P鈥?鈥?0322; 4.5-6鈥痬g/d, P鈥?鈥?0038) but not for risperidone (P鈥?鈥?2204). PANSS-FSNS response (鈮?0% reduction from baseline) rates were significantly higher with cariprazine (1.5-3鈥痬g/d鈥?鈥?4.3%, P鈥?鈥?0194; 4.5-6鈥痬g/d鈥?鈥?9.7%, P鈥?鈥?0001) than placebo (35.4%). In patients with acute schizophrenia and moderate/severe negative symptoms, cariprazine was associated with significantly greater improvement in negative symptoms compared with placebo and aripiprazole, warranting further exploration of the efficacy of cariprazine on negative symptoms. 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: 839712-12-8Safety of 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea).

3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳C. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Safety of 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea

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