Tag: 100-200

Electric Literature of C5H14Cl2N2On October 1, 2020 ,《Chlorine substituents and linker topology as factors of 5-HT6R activity for novel highly active 1,3,5-triazine derivatives with procognitive properties in vivo》 was published in European Journal of Medicinal Chemistry. The article was written by Sudol, Sylwia; Kucwaj-Brysz, Katarzyna; Kurczab, Rafal; Wilczynska, Natalia; Jastrzebska-Wiesek, Magdalena; Satala, Grzegorz; Latacz, Gniewomir; Gluch-Lutwin, Monika; Mordyl, Barbara; Zeslawska, Ewa; Nitek, Wojciech; Partyka, Anna; Buzun, Kamila; Doroz-Plonka, Agata; Wesolowska, Anna; Bielawska, Anna; Handzlik, Jadwiga. The article contains the following contents:

This study had supplied highly potent 5-HT6R agents with procognitive effects, which represent an original chem. class of 1,3,5-triazines, different than widely studied sulfone and indole-like 5-HT6R ligands. The new compounds I (R1 = Ph, 2,3-Cl2C6H3, 2,5-Cl2C6H3, 3,4-Cl2C6H3, 3,5-Cl2C6H3, 2,4-Cl2C6H3; R2 = H, Me, Et, n-Pr, n-Bu, X = nothing; R2 = H, X = CH2CH2) were rationally designed as modifications of lead, 4-(1-(2-chlorophenoxy)ethyl)-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine, involving an introduction of: (i) two chlorines at the benzene ring and (ii) varied linkers joining the triazine ring to aromatic ethers. Synthesis, in vitro and in vivo biol. tests and computer-aided SAR anal. for new compounds were carried out. Most of the new triazines displayed high affinity and selectivity toward 5-HT6R with respect to 5-HT2AR, 5-HT7R and D2R. The crystallog.-supported docking studies, including quantum-polarized ligand docking (QPLD), indicated that chlorine atoms might be involved in different type of halogen bonding, however, the linker properties seem to predominately affect the 5-HT6R affinity. Compound I (R1 = 2,5-Cl2C6H3; R2 = Et; X = nothing), which displayed: the highest affinity (Ki = 6 nM), very strong 5-HT6R antagonistic action (KB = 27 pM), procognitive effects in vivo in novel object recognition (NOR) test in rats, a very good permeability in PAMPA model and satisfying safety in vitro, was identified as the most potent 1,3,5-triazine agent so far, useful as a new lead for further research. In the experiment, the researchers used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Electric Literature 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..Electric Literature of C5H14Cl2N2

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

《Synthesis of new antimicrobials. IV. Synthesis of alkylenebis(thiourea) derivatives and their related compounds》 was published in Chemical & Pharmaceutical Bulletin in 1975. These research results belong to Yabuuchi, Takahiro; Hisaki, Masakatu; Matuda, Masahiro; Kimura, Ryuichi. Safety of 1-Methylpiperazine dihydrochloride The article mentions the following:

3,3′-Substituted 1,1′-alkylenebis(thiourea) derivatives, e.g. Et2NCH2CH2NHCSNHCH2CH2NHCSNHCH2CH2NEt2 were prepared from alkylenebis(isothiocyanates) and amines. Also, 3,3′-alkylenebis[2-thio-2,4(1H,3H)quinazolinediones] I (m = 3, 4, 6) were prepared by the reaction of alkylenebis(isothiocyanates) and anthranilic acid, or alkylene diamines and Et o-isothiocyanatobenzoate, resp. In the experiment, the researchers used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Safety of 1-Methylpiperazine dihydrochloride)

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..Safety of 1-Methylpiperazine dihydrochloride

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

Reference of 1-MethylpiperazineIn 2020 ,《The effect of novel 7-methyl-5-phenyl-pyrazolo[4,3-e]tetrazolo[4,5-b] [1,2,4]triazine sulfonamide derivatives on apoptosis and autophagy in DLD-1 and HT-29 colon cancer cells》 appeared in International Journal of Molecular Sciences. The author of the article were Gornowicz, Agnieszka; Szymanowska, Anna; Mojzych, Mariusz; Bielawski, Krzysztof; Bielawska, Anna. The article conveys some information:

The objective of this study was to synthesize title compounds I (R = [(2S)-1-hydroxy-4-methylpentan-2-yl]aminyl, 4-methylpiperazin-1-yl) by utilizing nucleophilic substitution reaction at the position N1. The biol. activity of tested compounds was assessed in DLD-1 and HT-29 cell lines. The induction of apoptosis was confirmed by Annexin V binding assay and acridine orange/ethidium bromide staining. The loss of mitochondrial membrane potential and caspase-8 activity was estimated using cytometer flow anal. The concentration of p53, LC3A, LC3B and beclin-1 was measured using the ELISA technique. The study revealed that anticancer activity of title compounds I is related with initiation of apoptosis occurred on the intrinsic pathway with mitochondrial membrane decrease and extrinsic with increase of activity of caspase-8. Moreover, a decrease in beclin-1, LC3A, and LC3B was observed in two cell lines after treatment with novel compounds This study showed that novel title compounds I might be a potential strategy in colon cancer treatment. The experimental process involved the reaction of 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

《Design, Synthesis, and Molecular Modeling Studies of Novel Coumarin Carboxamide Derivatives as eEF-2K Inhibitors》 was published in Journal of Chemical Information and Modeling in 2020. These research results belong to Comert Onder, Ferah; Durdagi, Serdar; Sahin, Kader; Ozpolat, Bulent; Ay, Mehmet. HPLC of Formula: 109-01-3 The article mentions the following:

Eukaryotic elongation factor-2 kinase (eEF-2K) is an unusual alpha kinase commonly upregulated in various human cancers, including breast, pancreatic, lung, and brain tumors. We have demonstrated that eEF-2K is relevant to poor prognosis and shorter patient survival in breast and lung cancers and validated it as a mol. target using genetic methods in related in vivo tumor models. Although several eEF-2K inhibitors have been published, none of them have shown to be potent and specific enough for translation into clin. trials. Therefore, development of highly effective novel inhibitors targeting eEF-2K is needed for clin. applications. However, currently, the crystal structure of eEF-2K is not known, limiting the efforts for designing novel inhibitor compounds Therefore, using homol. modeling of eEF-2K, we designed and synthesized novel coumarin-3-carboxamides including compounds (I) and (II) and evaluated their activity by performing in silico anal. and in vitro biol. assays in breast cancer cells (structures contained within. The Mol. Mechanics/Generalized Born Surface Area (MM/GBSA) area results showed that I have interaction energies with eEF-2K better than those of II compounds Our in vitro results indicated that compounds I were highly effective in inhibiting eEF-2K at 1.0 and 2.5μM concentrations compared to compounds II, supporting the in silico findings. In conclusion, the results of this study suggest that our homol. modeling along with in silico anal. may be effectively used to design inhibitors for eEF-2K. Our newly synthesized compounds I may be used as novel eEF-2K inhibitors with potential therapeutic applications.1-Methylpiperazine(cas: 109-01-3HPLC of Formula: 109-01-3) was used in this study.

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..HPLC of Formula: 109-01-3

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

The author of 《Synthesis and preliminary pharmacological assessment of novel 9-substituted pyrimidino[2,1-f]purines》 were Pawlowski, Maciej; Drabczynska, Anna; Gorczyca, Maria; Malec, Danuta; Modzelewski, Jerzy. And the article was published in Polish Journal of Pharmacology and Pharmacy in 1991. Recommanded Product: 1-Methylpiperazine dihydrochloride The author mentioned the following in the article:

Synthesis, chem. properties and results of preliminary pharmacol. evaluation of several new 9-substituted pyrimidino[2,1-f]purines (I, R1 = R2 = Me; NR1R2 = heterocyclo; n = 2-3) are described. The most interesting was I (NR1R2 = phenylpiperazino; n = 3) which exerted strong sedative, hypothermizing and cataleptogenic action and possessed some antiamphetamine and antiapomorphine (neuroleptic-like) properties. In addition to this study using 1-Methylpiperazine dihydrochloride, there are many other studies that have used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Recommanded Product: 1-Methylpiperazine dihydrochloride) was used in this study.

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..Recommanded Product: 1-Methylpiperazine dihydrochloride

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

Prasad, J. V. N. Vara; Markoski, Larry J.; Boyer, Fred E.; Domagala, John M.; Ellsworth, Edmund L.; Gajda, Christopher; Hagen, Susan E.; Tait, Bradley D.; Lunney, Elizabeth A.; Tummino, Peter J.; Ferguson, Donna; Holler, Tod; Hupe, Donald; Nouhan, Carolyn; Gracheck, Stephen J.; VanderRoest, Steven; Saunders, James; Iyer, K.; Sinz, M. published their research in Bioorganic & Medicinal Chemistry Letters on August 2 ,1999. The article was titled 《Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydro-2-pyranones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety》.Safety of 4-Methyl-1-piperazinesulfonyl Chloride The article contains the following contents:

Dihydropyran-2-ones possessing a sulfamate moiety at the 4-position of a phenylthio ring were designed to reach S3′ pocket of the HIV protease. Synthetic routes for the preparation of thiotosylates possessing 3-(2-tert-butyl-5-methyl-4-sulfamate) phenylthio moiety were established. SAR of various sulfamate analogs including HIV protease binding affinities, antiviral activities and therapeutic indexes will be described. An example compound thus prepared and tested was sulfamic acid 4-[[5,6-dihydro-4-hydroxy-6-[2-(4-hydroxyphenyl)ethyl]-6-methyl-2-oxo-2H-pyran-3-yl]thio]-5-(1,1-dimethylethyl)-2-methylphenyl ester. The experimental part of the paper was very detailed, including the reaction process of 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Safety of 4-Methyl-1-piperazinesulfonyl Chloride)

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Safety of 4-Methyl-1-piperazinesulfonyl Chloride

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

《Synthesis, characterization and carbonic anhydrase I and II inhibitory evaluation of new sulfonamide derivatives bearing dithiocarbamate》 was published in European Journal of Medicinal Chemistry in 2020. These research results belong to Saglik, Begum Nurpelin; Osmaniye, Derya; Cevik, Ulviye Acar; Levent, Serkan; Cavusoglu, Betul Kaya; Buyukemir, Oya; Nezir, Deniz; Karaduman, Abdullah Burak; Ozkay, Yusuf; Koparal, Ali Savas; Beydemir, Sukru; Kaplancikli, Zafer Asim. Formula: C5H12N2 The article mentions the following:

In this study, novel dithiocarbamate-sulfonamide derivatives I [R = Me, cyclohexyl, 4-O2NC6H4, etc.] were synthesized to investigate their inhibitory activity on purified human carbonic anhydrase (hCA) I and II. The IC50 and Ki values of the compounds were calculated to compare their inhibition profiles on hCA I and II isoenzymes. Acetazolamide was used as the standard inhibitor in the enzyme inhibition assay. Compounds I [R = Me, 4-MeC6H4CH2, CH2CH2NMe2, CH2CH2CH2NMe2, 2-pyridinyl, 2-pyrimidinyl] showed notable inhibitory effects against hCA I and II. Among these compounds, compound I [R = CH2CH2CH2NMe2] was found to be the most active derivate against both the hCA I and II enzymes with Ki values of 0.032 ± 0.001μM and 0.013 ± 0.0005μM, resp. The cytotoxicity of compounds I [R = Me, 4-MeC6H4CH2, CH2CH2NMe2, CH2CH2CH2NMe2, 2-pyridinyl, 2-pyrimidinyl] toward NIH/3T3 (mouse embryonic fibroblast cell line) was observed and the compounds were found to be non-cytotoxic. Furthermore, mol. docking studies were performed to investigate the interaction types between compound I [R = CH2CH2CH2NMe2] and the hCA I and II enzymes. As a result of this study a novel and potent class of CA inhibitors with good activity potential were identified. The experimental part of the paper was very detailed, including the reaction process of 1-Methylpiperazine(cas: 109-01-3Formula: C5H12N2)

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..Formula: C5H12N2

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

Product Details of 34352-59-5On October 20, 2015 ,《(2-Arylethenyl)-1,3,5-triazin-2-amines as a novel histamine H4 receptor ligands》 was published in European Journal of Medicinal Chemistry. The article was written by Kaminska, Katarzyna; Ziemba, Julia; Ner, Joanna; Schwed, Johannes Stephan; Lazewska, Dorota; Wiecek, Malgorzata; Karcz, Tadeusz; Olejarz, Agnieszka; Latacz, Gniewomir; Kuder, Kamil; Kottke, Tim; Zygmunt, Malgorzata; Sapa, Jacek; Karolak-Wojciechowska, Janina; Stark, Holger; Kiec-Kononowicz, Katarzyna. The article contains the following contents:

Within the constantly growing number of histamine H4 (H4R) receptor ligands there is a large group of azine derivatives A series of novel compounds in the group of 4-methylpiperazinyl-1,3,5-triazin-2-amines were designed and obtained. Structures were modified at the triazine 6-position by introduction of variously substituted arylethenyl moieties. Their affinities to histamine H4 receptors were evaluated in radioligand binding assays with use of Sf9 cells, transiently expressing human H4R. Pharmacol. studies identified 4-[(E)-2-(3-chlorophenyl)ethenyl]-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine (Ki = 253 nM) as the most potent compound in the present series. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Product Details of 34352-59-5)

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..Product Details of 34352-59-5

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

Onder, Ferah Comert; Sahin, Kader; Senturk, Murat; Durdagi, Serdar; Ay, Mehmet published an article in 2022. The article was titled 《Identifying highly effective coumarin-based novel cholinesterase inhibitors by in silico and in vitro studies》, and you may find the article in Journal of Molecular Graphics & Modelling.Recommanded Product: 1-Methylpiperazine The information in the text is summarized as follows:

Inhibition of high cholinesterase levels including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), is one of the most important strategies for the treatment of Alzheime′s disease (AD). Clin. limited drugs are used in the treatment of AD, so there is a need to find new effective inhibitors today. Therefore, in this study, synthesized six coumarin carboxamides (A1, A2, B1-B4) were evaluated against AChE and BChE by combined in silico and in vitro studies. The in vitro assessment of studied compounds revealed that A1, A2, B3, and B4 showed highest inhibition potential against AChE and BChE. As demonstrated with our structure activity relationship (SAR) study, the promising inhibition result of AChE at nanomolar concentrations was obtained with heterocyclic amines including pyrrolidine and N-Me piperazine moieties for tertiary amide substituted coumarin compounds B3 and B4, displaying KI values of 9.78 nM and 8.07 nM, resp. Thus, compounds B3 and B4 had around 5.7- and 6.9-fold more potency compared to the reference mol., neostigmine. Moreover, coumarin-3-carboxamide derivative A1 bearing benzylmorpholine moiety on coumarin scaffold at position 3 displayed stronger inhibition potential against BChE. Furthermore, in order to better understand their mol. mechanisms in these targets, we conducted mol. docking and MD simulations. Our promising preclin. results show that the lead compounds A1, A2, B3 and B4 have high potential as effective inhibitors for the treatment of AD. The experimental process involved the reaction of 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 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..Recommanded Product: 1-Methylpiperazine

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

Ayad, Magda Mohamed; Hosny, Mervat Mohamed; Metias, Youstina Mekhail published an article in 2022. The article was titled 《Green micellar liquid chromatographic analysis of alfuzosin hydrochloride and sildenafil citrate in a binary mixture compared to classical RPLC with stability indicating studies》, and you may find the article in Drug Development and Industrial Pharmacy.Quality Control of 1-Methylpiperazine The information in the text is summarized as follows:

Two simple and validated chromatog. studies were performed for simultaneous estimation of sildenafil citrate (SIL) and alfuzosin hydrochloride (ALF) in bulk, pharmaceuticals, and in the presence of their main degradation products. Two systems of mobile phase were applied isocratically for their first chromatog. separation using conventional and micellar mobile phases. Methanol, acetonitrile, and 0.02 M potassium dihydrogen phosphate (43:14:43 volume/volume; pH 4.66) were pumped at 1.3 mL/min in method I. Meanwhile, method II was based on less hazardous micellar mobile phase of nonionic surfactant (0.005 M Brij-35 in water; pH 2.5 adjusted with 0.1% orthophosphoric acid) with a flow rate of 1 mL/min. Both methods were carried on C18 column and coupled with UV detection at 225 nm at ambient temperature The first method was rectilinear over the concentration range of 5-62.5 μg/mL for both drugs, while the second method showed higher linearity ranges of 0.5-40, 2.5-62.5 μg/mL for ALF and (SIL), resp. The developed methods successfully enabled the quantification of the studied binary mixture in their tablets dosage form and evaluation their stabilities. Validation of the proposed methods according to ICH guidelines and system suitability were ascertained. Moreover, the applied methods were evaluated and compared from the perspective of green anal. chem., employing the National Environmental Methods Index, anal. Eco-Scale score, and Green Anal. Procedure Index, as three assessment tools. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3Quality Control 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..Quality Control of 1-Methylpiperazine

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