Tag: M.W=250-300

Tintori, Cristina; Brai, Annalaura; Dasso Lang, Maria Chiara; Deodato, Davide; Greco, Antonia Michela; Bizzarri, Bruno Mattia; Cascone, Lorena; Casian, Alexandru; Zamperini, Claudio; Dreassi, Elena; Crespan, Emmanuele; Maga, Giovanni; Vanham, Guido; Ceresola, Elisa; Canducci, Filippo; Arien, Kevin K.; Botta, Maurizio published the artcile< Development and in Vitro Evaluation of a Microbicide Gel Formulation for a Novel Non-Nucleoside Reverse Transcriptase Inhibitor Belonging to the N-Dihydroalkyloxybenzyloxopyrimidines (N-DABOs) Family>, Synthetic Route of 197638-83-8, the main research area is HIV1 antiviral gel dihydroalkyloxybenzyl oxopyrimidine.

Preventing HIV transmission by the use of a vaginal microbicide is a topic of considerable interest in the fight against AIDS. Both a potent anti-HIV agent and an efficient formulation are required to develop a successful microbicide. In this regard, mols. able to inhibit the HIV replication before the integration of the viral DNA into the genetic material of the host cells, such as entry inhibitors or reverse transcriptase inhibitors (RTIs), are ideal candidates for prevention purpose. Among RTIs, S- and N-dihydroalkyloxybenzyloxopyrimidines (S-DABOs and N-DABOs) are interesting compounds active at nanomolar concentration against wild type of RT and with a very interesting activity against RT mutations. Herein, novel N-DABOs were synthesized and tested as anti-HIV agents. Furthermore, their mode of binding was studied by mol. modeling. At the same time, a vaginal microbicide gel formulation was developed and tested for one of the most promising candidates.

Journal of Medicinal Chemistry published new progress about Anti-HIV agents. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Synthetic Route of 197638-83-8.

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

Yin, Huanhuan; Dong, Jingjing; Cai, Yingchun; Shi, Ximeng; Wang, Hao; Liu, Guixia; Tang, Yun; Liu, Jianwen; Ma, Lei published the artcile< Design, synthesis and biological evaluation of chalcones as reversers of P-glycoprotein-mediated multidrug resistance>, Recommanded Product: 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is chalcone design synthesis anticancer reversers glycoprotein multidrug resistance; Chalcones; Inhibitors docking; Multidrug resistance reversers; P-glycoprotein inhibitors; Structure-activity relationship.

Overexpression of P-glycoprotein (P-gp) is one of the major causes for multidrug resistance (MDR), which has become a major obstacle in cancer therapy. One hopeful approach to reverse the MDR is to develop inhibitors of P-gp in expression and/or function. Here, we designed and synthesized a series of chalcone derivatives as P-gp inhibitors and evaluated their potential reversal activities against MDR. Among them, the most active compound I had little intrinsic cytotoxicity and showed the highest activity (RF = 50.19) in reversing DOX resistance in MCF-7/DOX cells. Further studies demonstrated that I could increase intracellular accumulation of DOX and inhibit expression of P-gp at mRNA and protein levels. More importantly, I significantly enhanced the efficacy of DOX against the tumor xenografts bearing MCF-7/DOX cells with the precondition of unchanged body weight Therefore, I might represent a promising lead to develop MDR reversal agents for cancer chemotherapy.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Recommanded Product: 1-Boc-4-(4-Formylphenyl)piperazine.

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

Hieke, Martina; Roedl, Carmen B.; Wisniewska, Joanna M.; Buscato, Estella; Stark, Holger; Schubert-Zsilavecz, Manfred; Steinhilber, Dieter; Hofmann, Bettina; Proschak, Ewgenij published the artcile< SAR-study on a new class of imidazo[1,2-a]pyridine-based inhibitors of 5-lipoxygenase>, Synthetic Route of 197638-83-8, the main research area is imidazopyridinamine cyclohexyl morpholinophenyl preparation lipoxygenase inhibitor.

A novel class of 5-lipoxygenase (5-LO) inhibitors characterized by a central imidazo[1,2-a]pyridine scaffold, a cyclohexyl moiety and an aromatic system, is presented. This scaffold was identified in a virtual screening study and exhibits promising inhibitory potential on the 5-LO. The structure-activity relationships of this compound class was investigated. N-Cyclohexyl-6-methyl-2-(4-morpholinophenyl)imidazo[1,2-a]pyridine-3-amine was identified as a potent 5-LO inhibitor [IC50 = 0.16 μM (intact cells) and 0.1 μM (cell-free)], which may possess potential as an effective lead compound intervening with inflammatory diseases and certain types of cancer.

Bioorganic & Medicinal Chemistry Letters published new progress about 197638-83-8. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Synthetic Route of 197638-83-8.

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

Yang, Xiaoguang; Zhou, Yibo; Zhang, Xiufang; Yang, Sheng; Chen, Yun; Guo, Jingru; Li, Xiaoxuan; Qing, Zhihe; Yang, Ronghua published the artcile< A TP-FRET-based two-photon fluorescent probe for ratiometric visualization of endogenous sulfur dioxide derivatives in mitochondria of living cells and tissues>, Safety of 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is sulfur dioxide fluorescence probe two photon FRET.

A ratiometric two-photon fluorescent probe for SO2 derivatives was first proposed based on acedan-merocyanine dyads (I) via a TP-FRET strategy. It was successfully applied to visualization of the fluctuations of enzymically generated SO2 derivatives in the mitochondria of HepG2 cells and rat liver tissues using two-photon fluorescence microscopy imaging.

Chemical Communications (Cambridge, United Kingdom) published new progress about Fluorescence imaging. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Safety of 1-Boc-4-(4-Formylphenyl)piperazine.

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

Matos, Ana M.; Man, Teresa; Idrissi, Imane; Souza, Cleide C.; Mead, Emma; Dunbar, Charlotte; Wolak, Joanna; Oliveira, Maria C.; Evans, David; Grayson, James; Partridge, Benjamin; Garwood, Claire; Ning, Ke; Sharman, Gary; Chen, Beining; Rauter, Amelia P. published the artcile< Discovery of N-methylpiperazinyl flavones as a novel class of compounds with therapeutic potential against Alzheimer's disease: synthesis, binding affinity towards amyloid β oligomers (Aβo) and ability to disrupt Aβo-PrPC interactions>, Product Details of C16H22N2O3, the main research area is methylpiperazinyl flavone amyloid beta oligomer cellular prion protein.

With no currently available disease-modifying drugs, Alzheimer’s disease is the most common type of dementia affecting over 47 million people worldwide. In light of the most recent discoveries placing the cellular prion protein (PrPC) as a key player in amyloid βoligomer (Aβo)-induced neurodegeneration, we investigated whether the neuroprotective potential of nature-inspired flavonoids against Aβo-promoted toxicity would translate into the ability to disrupt PrPC-Aβo interactions. Hence, we synthesized a small library of flavones and studied their binding affinity towards Aβo by STD-NMR. C-glucosyl flavones exhibited improved binding affinity with morpholine, thiomorpholine or N-methylpiperazine rings attached to the flavone skeleton in ring B para position. Moreover, a N-methylpiperazinyl flavone displayed suitable physicochem. properties and optimal water solubility even without the sugar moiety, and a high interaction with Aβo involving the whole flavone core. Its C-glucosyl derivative, was, however, the best compound to inhibit PrPC-Aβo interactions in a dose-dependent manner, with 41% of inhibition capacity at 10μM. The potential of C-glucosyl flavones and their aglycons as protein-protein interaction inhibitors able to tackle PrPC-Aβo interactions is here presented for the first time, and supports this class of compounds as new prototypes for further development in the treatment of Alzheimer’s disease.

Pure and Applied Chemistry published new progress about Aglycons Role: BSU (Biological Study, Unclassified), SPN (Synthetic Preparation), BIOL (Biological Study), PREP (Preparation). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Product Details of C16H22N2O3.

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

Matos, Ana M.; Man, Teresa; Idrissi, Imane; Souza, Cleide C.; Mead, Emma; Dunbar, Charlotte; Wolak, Joanna; Oliveira, Maria C.; Evans, David; Grayson, James; Partridge, Benjamin; Garwood, Claire; Ning, Ke; Sharman, Gary; Chen, Beining; Rauter, Amelia P. published the artcile< Discovery of N-methylpiperazinyl flavones as a novel class of compounds with therapeutic potential against Alzheimer's disease: synthesis, binding affinity towards amyloid β oligomers (Aβo) and ability to disrupt Aβo-PrPC interactions>, Category: piperazines, the main research area is methylpiperazinyl flavone amyloid beta oligomer cellular prion protein.

With no currently available disease-modifying drugs, Alzheimer’s disease is the most common type of dementia affecting over 47 million people worldwide. In light of the most recent discoveries placing the cellular prion protein (PrPC) as a key player in amyloid βoligomer (Aβo)-induced neurodegeneration, we investigated whether the neuroprotective potential of nature-inspired flavonoids against Aβo-promoted toxicity would translate into the ability to disrupt PrPC-Aβo interactions. Hence, we synthesized a small library of flavones and studied their binding affinity towards Aβo by STD-NMR. C-glucosyl flavones exhibited improved binding affinity with morpholine, thiomorpholine or N-methylpiperazine rings attached to the flavone skeleton in ring B para position. Moreover, a N-methylpiperazinyl flavone displayed suitable physicochem. properties and optimal water solubility even without the sugar moiety, and a high interaction with Aβo involving the whole flavone core. Its C-glucosyl derivative, was, however, the best compound to inhibit PrPC-Aβo interactions in a dose-dependent manner, with 41% of inhibition capacity at 10μM. The potential of C-glucosyl flavones and their aglycons as protein-protein interaction inhibitors able to tackle PrPC-Aβo interactions is here presented for the first time, and supports this class of compounds as new prototypes for further development in the treatment of Alzheimer’s disease.

Pure and Applied Chemistry published new progress about Aglycons Role: BSU (Biological Study, Unclassified), SPN (Synthetic Preparation), BIOL (Biological Study), PREP (Preparation). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Category: piperazines.

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

Yang, Xiaoguang; Zhou, Yibo; Zhang, Xiufang; Yang, Sheng; Chen, Yun; Guo, Jingru; Li, Xiaoxuan; Qing, Zhihe; Yang, Ronghua published the artcile< A TP-FRET-based two-photon fluorescent probe for ratiometric visualization of endogenous sulfur dioxide derivatives in mitochondria of living cells and tissues>, Computed Properties of 197638-83-8, the main research area is sulfur dioxide fluorescence probe two photon FRET.

A ratiometric two-photon fluorescent probe for SO2 derivatives was first proposed based on acedan-merocyanine dyads (I) via a TP-FRET strategy. It was successfully applied to visualization of the fluctuations of enzymically generated SO2 derivatives in the mitochondria of HepG2 cells and rat liver tissues using two-photon fluorescence microscopy imaging.

Chemical Communications (Cambridge, United Kingdom) published new progress about Fluorescence imaging. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Computed Properties of 197638-83-8.

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

Hieke, Martina; Roedl, Carmen B.; Wisniewska, Joanna M.; Buscato, Estella; Stark, Holger; Schubert-Zsilavecz, Manfred; Steinhilber, Dieter; Hofmann, Bettina; Proschak, Ewgenij published the artcile< SAR-study on a new class of imidazo[1,2-a]pyridine-based inhibitors of 5-lipoxygenase>, Safety of 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is imidazopyridinamine cyclohexyl morpholinophenyl preparation lipoxygenase inhibitor.

A novel class of 5-lipoxygenase (5-LO) inhibitors characterized by a central imidazo[1,2-a]pyridine scaffold, a cyclohexyl moiety and an aromatic system, is presented. This scaffold was identified in a virtual screening study and exhibits promising inhibitory potential on the 5-LO. The structure-activity relationships of this compound class was investigated. N-Cyclohexyl-6-methyl-2-(4-morpholinophenyl)imidazo[1,2-a]pyridine-3-amine was identified as a potent 5-LO inhibitor [IC50 = 0.16 μM (intact cells) and 0.1 μM (cell-free)], which may possess potential as an effective lead compound intervening with inflammatory diseases and certain types of cancer.

Bioorganic & Medicinal Chemistry Letters published new progress about 197638-83-8. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Safety of 1-Boc-4-(4-Formylphenyl)piperazine.

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

Yin, Huanhuan; Dong, Jingjing; Cai, Yingchun; Shi, Ximeng; Wang, Hao; Liu, Guixia; Tang, Yun; Liu, Jianwen; Ma, Lei published the artcile< Design, synthesis and biological evaluation of chalcones as reversers of P-glycoprotein-mediated multidrug resistance>, Application of C16H22N2O3, the main research area is chalcone design synthesis anticancer reversers glycoprotein multidrug resistance; Chalcones; Inhibitors docking; Multidrug resistance reversers; P-glycoprotein inhibitors; Structure-activity relationship.

Overexpression of P-glycoprotein (P-gp) is one of the major causes for multidrug resistance (MDR), which has become a major obstacle in cancer therapy. One hopeful approach to reverse the MDR is to develop inhibitors of P-gp in expression and/or function. Here, we designed and synthesized a series of chalcone derivatives as P-gp inhibitors and evaluated their potential reversal activities against MDR. Among them, the most active compound I had little intrinsic cytotoxicity and showed the highest activity (RF = 50.19) in reversing DOX resistance in MCF-7/DOX cells. Further studies demonstrated that I could increase intracellular accumulation of DOX and inhibit expression of P-gp at mRNA and protein levels. More importantly, I significantly enhanced the efficacy of DOX against the tumor xenografts bearing MCF-7/DOX cells with the precondition of unchanged body weight Therefore, I might represent a promising lead to develop MDR reversal agents for cancer chemotherapy.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Application of C16H22N2O3.

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

Papagni, Antonio; Del Buttero, Paola; Bertarelli, Chiara; Miozzo, Luciano; Moret, Massimo; Pryce, Mary T.; Rizzato, Silvia published the artcile< Novel fluorinated amino-stilbenes and their solid-state photodimerization>, Formula: C16H22N2O3, the main research area is fluorinated aminostilbene solid state photodimerization.

We synthesized a series of polyfluoroaminostilbenes in satisfactory yields by Wittig reaction of 4-piperazinylbenzalhehydes with pentafluorobenzylidenetriphenylphosphorane and we analyzed the photochem. behavior of these stilbenes in the solid state; thanks to arene-perfluoroarene π-π interactions, some of them have shown a good propensity to give the corresponding cyclobutane photodimers in quant. yields. The photocyclization is reversible both in solution and in polymeric matrix, affording the corresponding stilbenes with different cis-trans stereoselectivity.

New Journal of Chemistry published new progress about [2+2] Photocycloaddition reaction. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Formula: C16H22N2O3.

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