Tag: 100-200

Tabushi, Iwao; Shimokawa, Kazuhiro published an article in Journal of the American Chemical Society. The title of the article was 《Model approach to retinal pigments. Remarkable red shift due to proximal ammonium ion》.Synthetic Route of C5H14Cl2N2 The author mentioned the following in the article:

Retinal derivs, I and II, were prepared and the absorption characteristics of a series of retinal derivatives (I, II, III, IV, and V) were investigated as a model study for the remarkable red shift observed for the native retinal pigments such as rhodopsins or bacteriorhodopsins. Remarkable red shifts observed in the following 2 derivatives were interpreted mechanistically; in retinal N’-methylpiperidinium perchlorate, 526 nm in CHCl3, as the electrostatic destabilization of the ground state by the proximal NH4 with a loose counter-anion in a less polar solvent; and in III chloride, 497 nm in water, as the balance between the electrostatic destabilization and the twist of the chromophore. In addition to this study using 1-Methylpiperazine dihydrochloride, there are many other studies that have used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Synthetic Route of C5H14Cl2N2) 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..Synthetic Route of C5H14Cl2N2

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

Dow, Robert L.; Paight, Ernest S.; Schneider, Steven R.; Hadcock, John R.; Hargrove, Diane M.; Martin, Kelly A.; Maurer, Tristan S.; Nardone, Nancy A.; Tess, David A.; DaSilva-Jardine, Paul published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Potent and selective, sulfamide-based human β3-adrenergic receptor agonists》.Name: 4-Methyl-1-piperazinesulfonyl Chloride The author mentioned the following in the article:

A series of sulfamide-based analogs, e.g., I, related to L-796568 were prepared and evaluated for their biol. activity at the human β3-adrenergic receptor (AR). This modification allows for a significant reduction in mol. weight, while maintaining single-digit nanomolar potencies at the β3-AR and high selectivities vs. the β1- or β2-AR.4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Name: 4-Methyl-1-piperazinesulfonyl Chloride) was used in this study.

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.Name: 4-Methyl-1-piperazinesulfonyl Chloride

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

Related Products of 109-01-3In 2021 ,《Discovery and optimization of novel pyrazole-benzimidazole CPL304110 as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3)》 appeared in European Journal of Medicinal Chemistry. The author of the article were Yamani, Abdellah; Zdzalik-Bielecka, Daria; Lipner, Joanna; Stanczak, Aleksandra; Piorkowska, Natalia; Stanczak, Paulina Seweryna; Olejkowska, Patrycja; Hucz-Kalitowska, Joanna; Magdycz, Marta; Dzwonek, Karolina; Dubiel, Krzysztof; Lamparska-Przybysz, Monika; Popiel, Delfina; Pieczykolan, Jerzy; Wieczorek, Maciej. The article conveys some information:

The scaffolds hybridization approach, scaffold-hopping concept, has been employed to synthesize a series of novel pyrazole-benzimidazoles I [R1 = H, Cl; R2 = morpholin-4-yl, 4-methylpiperazin-1-ylcarbonyl, tetrahydropyran-4-ylcarbamoyl, etc.; R3 = H, F]. Compound I [R1 = R3 = H; R2 = 4-methylpiperazin-1-yl] (CPL304110) was identified as a selective and potent pan-FGFR inhibitor for FGFR1, FGFR2, FGFR3 with IC50 of 0.75 nM, 0.50 nM, 3.05 nM resp., and IC50 of 87.90 nM for FGFR4. Due to its favorable pharmacokinetic profile, low toxicity and potent anti-tumor activity in-vivo, this compound I is currently under evaluation in phase I clin. trial for the treatment of bladder, gastric and squamous cell lung cancers (01FGFR2018; NCT04149691). In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine(cas: 109-01-3Related Products of 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..Related Products of 109-01-3

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

《Synthesis, biological evaluation and molecular docking studies of some new 2-(2-(substituted piperazin-1-yl)-phenyl)-1H-benzo[d]imidazoles as potential antibacterial, anticancer and antifungal agents》 was written by Bhardwaj, Harsh; Sharma, C. S.. Related Products of 109-01-3 And the article was included in Indian Journal of Heterocyclic Chemistry in 2020. The article conveys some information:

Some new 2-(2-(substituted piperazin-1-yl)-phenyl)-1H-benzo[d]imidazoles I [R = H, 2-Me, 4-Et, etc.] were designed, synthesized and evaluated by the docking studies using glide tool for their antimicrobial and anticancer activities. The structures of these compounds I were characterized by IR, proton NMR, mass spectral data, and elemental anal. Each analog was tested in-vitro for various types of pharmacol. activities, including antibacterial, antifungal and anticancer activity. The compound I [R = 3-Me] was found to be most active against Escherichia coli and Pseudomonas aeruginosa and compound I [R = 2-Et] against Bacillus subtilis and Staphylococcus aureus. The derivative I [R = 4-Et] showed good activity against Candida albicans and Aspergillus niger. Among all the tested compounds, I [R = H, 2-Me] were found with significant anticancer activity in comparison to Adriamycin standard drug. The obtained results revealed that most of the synthesized compounds I exhibited significant antifungal, antibacterial and anticancer activity. It was deduced that these synthesized compounds I can be regarded as a promising starting point for developing a single mol. with multiple targets.1-Methylpiperazine(cas: 109-01-3Related Products of 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..Related Products of 109-01-3

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

Product Details of 34352-59-5On 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: 34352-59-5Product 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

《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. Formula: C5H14Cl2N2 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: 34352-59-5Formula: 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..Formula: C5H14Cl2N2

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

Computed Properties of C5H12N2In 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: 109-01-3Computed Properties of 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..Computed Properties of C5H12N2

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. Related Products of 34352-59-5 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: 34352-59-5Related Products of 34352-59-5) 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..Related Products of 34352-59-5

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》.Product Details of 1688-95-5 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: 1688-95-5Product Details of 1688-95-5)

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.Product Details of 1688-95-5

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