Tag: 100-200

In 1993,Bulletin of the Faculty of Pharmacy (Cairo University) included an article by Al-Deeb, O. A.; Al-Rashood, K. A.; Khalil, A. A.. Category: piperazines. The article was titled 《Synthesis of new (1-phenylcyclohexyl)piperazine derivatives as potential analgesics》. The information in the text is summarized as follows:

A series of phencyclidine isostere derivatives was prepared by replacement of the piperidine ring by N-substituted piperazines. The Strecker synthesis was employed for synthesis of the intermediate carbonitriles I [R = (un)substituted Ph, Me, PhCH2; R1 = CN]. The synthesis of the target compounds I (same R; R1 = Ph) was accomplished by treatment of the carbonitrile with phenylmagnesium bromide. These compounds were tested for analgesic activity, but none were effective. The experimental part of the paper was very detailed, including the reaction process of 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Category: piperazines)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Category: piperazines

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

Computed Properties of C5H14Cl2N2On May 31, 1981, Valenta, Vladimir; Bartosova, Marie; Protiva, Miroslav published an article in Collection of Czechoslovak Chemical Communications. The article was 《Neurotropic and psychotropic agents. CLI. 1-[3-(2-Alkoxyphenoxy)-3-phenylpropyl]piperazines and some related compounds》. The article mentions the following:

Mannich bases PhCOCH2CH2NRR1 (NRR1 = NMe2, 4-methylpiperazino, 4-benzylpiperazino) were reduced to the alc. HOCHPhCH2CH2NRR1 which were transformed with SOCl2 to PhCHClCH2CH2NRR1. Substitution reactions with Na salts of guaiacol, 2-ethoxyphenol and 2-benzyloxyphenol gave 2-R2OC6H4OCHPhCH2CH2NRR1 (RR1 = NMe2, 4-methylpiperazino, 4-benzylpiperazino; R2 = Me, Et, CH2Ph). 2-PhCH2OC6H4OCHPhCH2CH2NMe2 was partially demethylated by treatment with ClCO2Et followed by alk. hydrolysis to 2-PhCH2OCHPhCH2CH2NHMe. The products in high doses exhibited central excitation but did not show antireserpine activity; they had several structurally less specific effects (hypotensive, local anesthetic, spasmolytic (LD and ED given). In the experimental materials used by the author, we found 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Computed Properties of C5H14Cl2N2)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Computed Properties of C5H14Cl2N2

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

Safety of 1-MethylpiperazineIn 2020 ,《Design and optimization of quinazoline derivatives: new non-nucleoside inhibitors of bovine viral diarrhea virus》 appeared in Frontiers in Chemistry (Lausanne, Switzerland). The author of the article were Fernandez, Gabriela A.; Castro, Eliana F.; Rosas, Rocio A.; Fidalgo, Daniela M.; Adler, Natalia S.; Battini, Leandro; Espana de Marco, Maria J.; Fabiani, Matias; Bruno, Ana M.; Bollini, Mariela; Cavallaro, Lucia V.. The article conveys some information:

In a previous work, potential mols. that dock into an allosteric binding pocket of BVDV RdRp via a structure-based virtual screening approach was identified. One of them, N-(2-morpholinoethyl)-2-phenylquinazolin-4-amine I [R2 = Ph; R4 = 2-morpholinoethylamino; R7 = H] [50% effective concentration (EC50) = 9.7 ± 0.5μM], was selected to perform different chem. modifications. Among synthesized derivatives I [R2 = H, Ph, 4-MeC6H4, etc.; R4 = 4-methylpiperazin-1-yl, HN(CH2)5CH3, 4-methoxyanilino, etc.; R7 = H, Cl], compound I [R2 = H, Ph, 4-(Me)2NC6H4; R4 = 4-methylpiperazin-1-yl, 3-(dimethylamino)propylamino, 4-(2-hydroxyethyl)piperazin-1-yl, (2-morpholinoethylamino), 2-(1-piperidyl)ethylamino, 2-(1-piperidyl)ethylamino, (2,2,6,6-tetramethyl-4-piperidyl)amino, ; R7 = H, Cl] of them showed considerable antiviral activity. Mol. modeling of the most active compounds I [R2 = H, Ph, 4-MeC6H4, 4-MeOC6H4, 4-O2NC6H4, 4-(Me)2NC6H4; R4 = 4-methylpiperazin-1-yl, 3-(dimethylamino)propylamino, 4-(2-hydroxyethyl)piperazin-1-yl, 2-morpholinoethylamino, 2-(1-piperidyl)ethylamino, (2,2,6,6-tetramethyl-4-piperidyl)amino; R7 = H, Cl] showed that they bind to a pocket located in the fingers and thumb domains in BVDV RdRp, which was different than that identified for other non-nucleoside inhibitors (NNIs) such as thiosemicarbazone (TSC). Compound 2-[4-(2-phenylquinazolin-4-yl)piperazin-1-yl]ethanol I [R2 = Ph; R4 = 4-(2-hydroxyethyl)piperazin-1-yl; R7 = H] ( EC50 = 1.7 ± 0.4μM) was selected for further anal. Compound I [R2 = Ph; R4 = 4-(2-hydroxyethyl)piperazin-1-yl; R7 = H] was found to inhibit the in vitro replication of TSC-resistant BVDV variants, which carry the N264D mutation in the RdRp. In addition, I [R2 = Ph; R4 = 4-(2-hydroxyethyl)piperazin-1-yl; R7 = H] presented adequate solubility in different media and a high-stability profile in murine and bovine plasma. In the experiment, the researchers used 1-Methylpiperazine(cas: 109-01-3Safety of 1-Methylpiperazine)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Safety of 1-Methylpiperazine

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

Zak, Agnieszka; Lemaire, Lucas; Chalon, Sylvie; Chicheri, Gabrielle; Marzag, Hamid; Bodard, Sylvie; Serriere, Sophie; Routier, Sylvain; Buron, Frederic; Vercouillie, Johnny published an article in 2021. The article was titled 《[18F]-labeled positron emission tomography ligand for the histamine H4 receptor》, and you may find the article in Journal of Labelled Compounds and Radiopharmaceuticals.Recommanded Product: 109-01-3 The information in the text is summarized as follows:

We synthesized 5-[18F]-fluoro-1H-indol-2-yl)(4-methyl-1-piperazinyl)methanone ([18F]5) via a Suzuki approach starting from a protected pinacol borane precursor followed by acidic hydrolysis of the t-Boc protecting group. The non-optimized radiochem. yield was 5.7 ± 1.35%, radiochem. purity was over 99%, and molar activity was 100.7 ± 34.5 GBq/μmol (n = 3). [18F]5 was stable in rat plasma for at least 4 h and was evaluated by μPET imaging and biodistribution using a unilateral quinolinic acid rat model of neuroinflammation. The time-activity curve showed that [18F]5 entered the brain immediately after i.v. injection and then left it progressively with a very low level reached from 30 min after injection. The biodistribution study showed no difference in the accumulation of [18F]5 between the lesioned and intact side of the brain and between control rats and animals pretreated with a saturating dose of JNJ-7777120 as a specific H4R antagonist. Hence, despite its in vitro nanomolar affinity for H4R, and its ability to cross the blood-brain barrier in rats, [18F]5 does not appear suitable to image in vivo the receptor by PET. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 109-01-3)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Recommanded Product: 109-01-3

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

Dalmijn, Joost A.; Poursat, Baptiste A. J.; van Spanning, Rob J. M.; Brandt, Bernd W.; de Voogt, Pim; Parsons, John R. published their research in Environmental Science: Water Research & Technology in 2021. The article was titled 《Influence of short- and long-term exposure on the biodegradation capacity of activated sludge microbial communities in ready biodegradability tests》.Category: piperazines The article contains the following contents:

Ready biodegradability tests (RBTs) are extensively used to screen the potential of chems. to be biodegraded. The use of RBT protocols often results in large variations of test results that may lead to wrong interpretations. The present study aims to obtain a fundamental understanding of this variability. For this, we subjected the compounds 4-chloroaniline (4CA), carbamazepine (CBZ), metformin (MET), and N-methylpiperazine (NMP) to a variety of different test conditions. Inocula from five local wastewater treatment plants (WWTPs) were used in an attempt to enhance the Organization for Economic Co-operation and Development (OECD) 310 biodegradability tests. The biodegradation capacity in RBTs, community composition and adaptation of the communities were compared after one week of pre-exposure in batch and four months exposure in chemostat. The results confirm that none of the test compounds is readily biodegradable in the standard OECD 310 RBT. However, when pre-exposure under either batch or chemostat conditions was included, 4CA was degraded in some cases and less variability among different inocula was observed for the transformation of MET. Bacterial communities from the five locations were found to be significantly different in composition from one another. In addition, pre-treatment performed before the RBT significantly changed the composition of each community. Results of this experiment show that short-term pre-exposure may increase the absolute number of degraders and deserves to be further investigated as a potential method to reduce the outcome variability of RBTs. In the experiment, the researchers used 1-Methylpiperazine(cas: 109-01-3Category: piperazines)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Category: piperazines

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

In 2019,Analytical Chemistry (Washington, DC, United States) included an article by Wang, Shan-Shan; Wang, Yun-Jun; Zhang, Jing; Sun, Tuan-Qi; Guo, Yin-Long. Reference of 1-Methylpiperazine. The article was titled 《Derivatization Strategy for Simultaneous Molecular Imaging of Phospholipids and Low-Abundance Free Fatty Acids in Thyroid Cancer Tissue Sections》. The information in the text is summarized as follows:

Matrix-assisted laser desorption/ionization (MALDI) mass spectrometry imaging (MSI) has been applied in many fields for detecting and imaging a variety of metabolites. In cancer research, this fast-growing imaging method also helps to elucidate the connection between the changes of metabolites in the microenvironment and the proliferation and survival of cancer cells. Free fatty acids (FFAs) are a vital building block of phospholipids (PLs) that can serve as a second cellular messenger and provide nutrients in the cancer microenvironment. The metabolism process of FFAs and PLs is highly relevant to the initiation and progression of different cancers. To better understand the metabolism process in cancer tissues, simultaneously detecting and imaging FFAs and PLs is essential. Despite the crucial developments that have been performed in the field of lipids imaging, FFAs and PLs have rarely been detected and imaged simultaneously in pos. ion mode with good detection sensitivity. In this work, an on-tissue derivatization method was used to add a permanently quaternary amine onto FFAs; then, the FFAs and PLs were simultaneously imaged in pos. ion mode. The derivatized FFAs are suitable for detection in pos. ion mode. In comparison with the traditional matrix and the previous derivatization method, the derivatization reagent has a higher sensitivity for imaging FFAs. In addition, for simultaneous imaging anal. of FFAs and PLs, the number of imaged FFAs and PLs is greater than that with the previous on-tissue derivatization method. This high-sensitivity on-tissue derivatization method was applied to detect and image PLs and fatty acids in thyroid cancer tissues. In the MSI experiment, FFA derivatives and PLs were imaged while mol. localization and tissue integrity were maintained. Meanwhile, the correlation between PLs and FFAs was also studied, and the results showed that the correlations between saturated FFAs of C16:0 and C18:0 and PLs are better than the correlations of unsaturated FFAs with PLs. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine(cas: 109-01-3Reference of 1-Methylpiperazine)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Reference of 1-Methylpiperazine

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