Month: November 2022

Design, synthesis, and biological activity of novel factor Xa inhibitors: Improving metabolic stability by S1 and S4 ligand modification was written by Komoriya, Satoshi;Kobayashi, Shozo;Osanai, Ken;Yoshino, Toshiharu;Nagata, Tsutomu;Haginoya, Noriyasu;Nakamoto, Yumi;Mochizuki, Akiyoshi;Nagahara, Takayasu;Suzuki, Makoto;Shimada, Takashi;Watanabe, Kengo;Isobe, Yumiko;Furugoori, Taketoshi. And the article was included in Bioorganic & Medicinal Chemistry in 2006.Category: piperazines The following contents are mentioned in the article:

Serine protease factor Xa (fXa) inhibitor I showed good ex vivo anti-fXa activity upon oral administration in rats. However, it has been revealed that I had low metabolic stability against human liver microsomes. To improve the metabolic stability, we attempted to modify the S1 and S4 ligands of I. These modifications resulted in a compound which exhibited selective anti-fXa activity and excellent anti-coagulation activity. This study involved multiple reactions and reactants, such as Methyl 2-(1,4-dibenzylpiperazin-2-yl)acetate (cas: 183742-32-7Category: piperazines).

Methyl 2-(1,4-dibenzylpiperazin-2-yl)acetate (cas: 183742-32-7) 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.Category: piperazines

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

New intermediates for the selective synthesis of 1-methyl-3-phenylpiperazine and some phenylpiperazine derivatives was written by Rao, Divvela V. N. Srinivasa;Dandala, Ramesh;Handa, Vijay Kumar;Sivakumaran, Meenakshisunderam;Naidu, Andra. And the article was included in ARKIVOC (Gainesville, FL, United States) in 2006.Electric Literature of C15H20N2O3 The following contents are mentioned in the article:

New intermediates 4-protected-1-alkyl-2-oxo-3-phenylpiperazines and 1-alkyl-2-oxo-3-phenylpiperazines for the selective synthesis of 1-alkyl-3-phenylpiperazines, e.g., I, are described. First method involves the reduction of the 4-protected-1-alkyl-2-oxo-3-phenylpiperazines followed by deprotection giving the 1-alkyl-3-phenylpiperazines. Second method involves the deprotection of 4-protected-1-alkyl-2-oxo-3-phenylpiperazines followed by reduction giving the 1-alkyl-3-phenylpiperazines. This study involved multiple reactions and reactants, such as tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3Electric Literature of C15H20N2O3).

tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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.Electric Literature of C15H20N2O3

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

Novel Phenyl-Substituted 5,6-Dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 Antagonists with Robust Target Engagement in Rat Brain was written by Chrovian, Christa C.;Soyode-Johnson, Akinola;Ao, Hong;Bacani, Genesis M.;Carruthers, Nicholas I.;Lord, Brian;Nguyen, Leslie;Rech, Jason C.;Wang, Qi;Bhattacharya, Anindya;Letavic, Michael A.. And the article was included in ACS Chemical Neuroscience in 2016.Category: piperazines The following contents are mentioned in the article:

Novel 5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 antagonists were optimized to allow for good blood-brain barrier permeability and high P2X7 target engagement in the brain of rats. Compound I (huP2X7 IC₅₀ = 9 nM; rat P2X7 IC₅₀ = 42 nM) achieved 80% receptor occupancy for 6 h when dosed orally at 10 mg/kg in rats as measured by ex vivo radioligand binding autoradiog. Structure-activity relationships within this series are described, as well as in vitro ADME results. In vivo pharmacokinetic data for key compounds is also included. This study involved multiple reactions and reactants, such as tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3Category: piperazines).

tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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.Category: piperazines

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

Lowering the UV Absorbance Detection Limit in Capillary Zone Electrophoresis Using a Single Linear Photodiode Array Detector was written by Culbertson, Christopher T.;Jorgenson, James W.. And the article was included in Analytical Chemistry in 1998.Safety of Sodium bis(2-(4-(2-hydroxyethyl)piperazin-1-yl)ethanesulfonate) The following contents are mentioned in the article:

A new approach for lowering the UV absorbance detection limit in capillary electrophoresis is presented. This approach involves the use of a photodiode array in which each of the diodes in the array is treated as an independent detector. Over a run, therefore, an electropherogram is generated for each diode in the array. Averaging the electropherograms generated from 1500 diodes in a diode array resulted in a signal-to-noise ratio 85 times that of an electropherogram generated from any one diode in the array. These signal-to-noise improvements are discussed, and the detection limits are compared to the detection limits obtained from a com. single-point detector. The array detector improves the detection limit by a factor of 3.8 (±0.4). This study involved multiple reactions and reactants, such as Sodium bis(2-(4-(2-hydroxyethyl)piperazin-1-yl)ethanesulfonate) (cas: 103404-87-1Safety of Sodium bis(2-(4-(2-hydroxyethyl)piperazin-1-yl)ethanesulfonate)).

Sodium bis(2-(4-(2-hydroxyethyl)piperazin-1-yl)ethanesulfonate) (cas: 103404-87-1) 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 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.Safety of Sodium bis(2-(4-(2-hydroxyethyl)piperazin-1-yl)ethanesulfonate)

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

Discovery of novel 2-(3-phenylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3β inhibitors was written by Usui, Yoshihiro;Uehara, Fumiaki;Hiki, Shinsuke;Watanabe, Kazutoshi;Tanaka, Hiroshi;Shouda, Aya;Yokoshima, Satoshi;Aritomo, Keiichi;Adachi, Takashi;Fukunaga, Kenji;Sunada, Shinji;Nabeno, Mika;Saito, Ken-ichi;Eguchi, Jun-ichi;Yamagami, Keiji;Asano, Shouichi;Tanaka, Shinji;Yuki, Satoshi;Yoshii, Narihiko;Fujimura, Masatake;Horikawa, Takashi. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2017.Electric Literature of C15H20N2O3 The following contents are mentioned in the article:

The results of further evolution of glycogen synthase kinase (GSK)-3β inhibitors from authors’ promising compounds containing a 2-phenylmorpholine moiety are described. Transformation of the morpholine moiety into a piperazine moiety resulted in potent GSK-3β inhibitors. SAR studies focused on the Ph moiety revealed that a 4-fluoro-2-methoxy group afforded potent inhibitory activity toward GSK-3β. Based on docking studies of (S)-isomer of I, new hydrogen bonding between the nitrogen atom of the piperazine moiety and the oxygen atom of the main chain of Gln185 has been indicated, which may contribute to increased activity compared with that of the corresponding phenylmorpholine analogs. Effect of the stereochem. of the phenylpiperazine moiety is also discussed. This study involved multiple reactions and reactants, such as tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3Electric Literature of C15H20N2O3).

tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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.Electric Literature of C15H20N2O3

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

The dehydration of ureas by two-phase dichlorocarbene reaction, a synthetic access to substituted cyanamides was written by Schroth, W.;Kluge, H.;Frach, R.;Hodek, W.;Schaedler, H. D.. And the article was included in Journal fuer Praktische Chemie (Leipzig) in 1983.SDS of cas: 89026-59-5 The following contents are mentioned in the article:

A wide variety of N,N-disubstituted ureas were dehydrated in the CHCl₃/NaOH catalytic 2-phase system under mild conditions. The sequence of urea transamidation and dehydration offers a profitable approach to aprotic cyanamides. Among various phase-transfer catalysts tertiary amines prove to be the most efficient. Tertiary amines may also be used in the transformation of carboxamides and thioamides to the corresponding nitriles. The application of the same technique is less suitable in the case of N-monosubstituted ureas, N,N‘-disubstituted ureas, and N-(dialkylaminomethylene)ureas, since subsequent reactions of the cyanamides predominate. The dehydration mechanism is elucidated in terms of HOMO-perturbation theory. This study involved multiple reactions and reactants, such as 4-(4-Methoxyphenyl)piperazine-1-carboxamide (cas: 89026-59-5SDS of cas: 89026-59-5).

4-(4-Methoxyphenyl)piperazine-1-carboxamide (cas: 89026-59-5) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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.SDS of cas: 89026-59-5

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

Statistical optimization and validation of a novel ultra-performance liquid chromatography method for estimation of nintedanib in rat and human plasma was written by Shukla, Snehal K.;Kadry, Hossam;Bhatt, Jayshil A.;Elbatanony, Rasha;Ahsan, Fakhrul;Gupta, Vivek. And the article was included in Bioanalysis in 2020.Category: piperazines The following contents are mentioned in the article:

A high throughput ultra-performance liquid chromatog. (UPLC)-UV method for quantification of nintedanib in rat and human plasma was developed and optimized using chemometrical approach. Design of experiment and multivariate statistical approach was used for definition of optimized method. Final separation was performed using protein precipitation method on ACQUITY HSS T3 C18 column in isocratic mode using potassium phosphate buffer (pH 7.5): acetonitrile. Method was validated as per US-FDA guidelines linearly from 15-750 ng/mL. All quality control samples showed <15% relative standard deviation for precision and 85-115% accuracy along with >98% extraction recovery. The developed method is easily applicable in determining pharmacokinetic parameters in preclin. subjects along with successful implementation for quantification in human plasma samples. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6Category: piperazines).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) 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 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.Category: piperazines

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

Two Cd(II)-based metal-organic frameworks as difunctional fluorescence sensors to detect enrofloxacin and Fe³⁺ was written by Wen, Ming-Yue;Fu, Lianshe;Dong, Gui-Ying. And the article was included in Journal of Solid State Chemistry in 2022.Computed Properties of C16H18FN3O3 The following contents are mentioned in the article:

Two ternary Cd(II) metal-organic frameworks [Cd₄(L)₂(2,6-NDA)₄·5H₂O]_n (1) and [Cd(L)_0.5(1,8-NDA)·0.75H₂O]_n (2) (L = 1,4-bis(1-(piperidin-4-ylmethyl)-1H-benzo[d]imidazole-2-yl)butane, 2,6-H₂NDA = 2,6-naphthalenedicarboxylic acid, 1,8-H₂NDA = 1,8-naphthalenedicarboxylic acid) were synthesized based on the L and two isomeric naphthalene dicarboxylic acids. 1 And 2 exhibit a 3D 4,4T11 and a 2D 3,4L13 network, resp. Both 1 and 2 show remarkable thermal stability and can be used as difunctional fluorescence sensors for Fe³⁺ and enrofloxacin via a fluorescence quenching process with high sensitivity and selectivity. In addition, the fluorescence sensing mechanism was discussed in detail. This study involved multiple reactions and reactants, such as 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7Computed Properties of C16H18FN3O3).

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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.Computed Properties of C16H18FN3O3

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

Tetracycline sensitizes TiO₂ for visible light photocatalytic degradation via ligand-to-metal charge transfer was written by Qin, Caidie;Tang, Juanjuan;Qiao, Ruxia;Lin, Sijie. And the article was included in Chinese Chemical Letters in 2022.Product Details of 70458-96-7 The following contents are mentioned in the article:

Treatment of antibiotics contaminated water remains a global environmental challenge. In this study, tetracycline (TC) was found to effectively sensitize pure TiO₂ for visible light photocatalytic degradation via a ligand-to-metal charge transfer mechanism. The sensitization was attributed to the formation of TC-TiO₂ complex and the overlap of the MOs of TC and the conduction band of TiO₂. The intermediate degradation products of TC, however, did not sensitize TiO₂, which was the reason for the low mineralization rate. Nevertheless, our results showed that the intermediate degradation products of TC had significantly reduced bactericidal effects and less induction of antibiotic-resistance genes (ARGs). This study showcases an effective treatment of antibiotics-containing wastewater using the most common photocatalyst TiO₂ with reduced risk in the spread of ARGs. This study involved multiple reactions and reactants, such as 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7Product Details of 70458-96-7).

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) 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. 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.Product Details of 70458-96-7

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

Prevalence, Antimicrobial Susceptibility and Resistance Gene Detection in Bacteria Isolated from Goldfish and Tiger Barb from Ornamental Fish Farms of Tamil Nadu was written by Hemamalini, Nallaiah;Shanmugam, Seerappalli Aran;Kathirvelpandian, Ayyathurai;Deepak, Agarwal;Kaliyamurthi, Venkatachalam;Suresh, Eswaran;Ezhilmathi, Selvaram. And the article was included in Indian Journal of Microbiology in 2022.Computed Properties of C16H18FN3O3 The following contents are mentioned in the article:

This study aims to determine the antimicrobial resistance (AMR) pattern in freshwater ornamental cyprinids, such as Goldfish and Tiger barb. Mol. characterization of bacterial isolates confirmed the presence of 7 bacterial isolates in Goldfish and 6 in Tiger barb. Antimicrobial susceptibility test using 36 antibiotics revealed a higher resistance pattern for bacitracin, rifampicin, trimethoprim, cefalexin, ampicillin, amoxicillin, nalidixic acid and nitrofurantoin. Sulphafurazole, norfloxacin and ciprofloxacin were effective against all the bacterial isolates derived from Goldfish and Tiger barb. Most bacterial isolates exhibited > 0.2 multi-drug resistance index (MDR), indicating the severity of antibiotic use in the culture system. The finding of the present study suggests that ornamental fish may act as the reservoir of MDR bacteria and dissemination of resistance genes to clin. and human commensal bacteria through horizontal gene transfer. This study involved multiple reactions and reactants, such as 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7Computed Properties of C16H18FN3O3).

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) 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. Computed Properties of C16H18FN3O3

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