Tag: M.W=250-300

Arikawa, Yasuyoshi; Nishida, Haruyuki; Kurasawa, Osamu; Hasuoka, Atsushi; Hirase, Keizo; Inatomi, Nobuhiro; Hori, Yasunobu; Matsukawa, Jun; Imanishi, Akio; Kondo, Mitsuyo; Tarui, Naoki; Hamada, Teruki; Takagi, Terufumi; Takeuchi, Toshiyuki; Kajino, Masahiro published the artcile< Discovery of a Novel Pyrrole Derivative 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine Fumarate (TAK-438) as a Potassium-Competitive Acid Blocker (P-CAB)>, Recommanded Product: 3-(Methylsulfonyl)benzenesulfonyl Chloride, the main research area is pyrrole fluorophenylpyridinylsulfonyl preparation gastric acid secretion inhibitor; proton potassium ATPase gastric inhibitor pyrrole fluorophenylpyridinylsulfonyl.

In our pursuit of developing a novel and potent potassium-competitive acid blocker (P-CAB), we synthesized pyrrole derivatives focusing on compounds with low log D and high ligand-lipophilicity efficiency (LLE) values. Among the compounds synthesized, the compound I exhibited potent H+,K+-ATPase inhibitory activity and potent gastric acid secretion inhibitory action in vivo. Its maximum efficacy was more potent and its duration of action was much longer than those of proton pump inhibitors (PPIs). Therefore, compound I (1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate, TAK-438) was selected as a drug candidate for the treatment of gastroesophageal reflux disease (GERD), peptic ulcer, and other acid-related diseases.

Journal of Medicinal Chemistry published new progress about Digestive tract disease. 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, Recommanded Product: 3-(Methylsulfonyl)benzenesulfonyl Chloride.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Shao, Pengcheng P.; Ye, Feng; Chakravarty, Prasun K.; Varughese, Deepu J.; Herrington, James B.; Dai, Ge; Bugianesi, Randal M.; Haedo, Rodolfo J.; Swensen, Andrew M.; Warren, Vivien A.; Smith, McHardy M.; Garcia, Maria L.; McManus, Owen B.; Lyons, Kathryn A.; Li, Xiaohua; Green, Mitchell; Jochnowitz, Nina; McGowan, Erin; Mistry, Shruti; Sun, Shu-Yu; Abbadie, Catherine; Kaczorowski, Gregory J.; Duffy, Joseph L. published the artcile< Aminopiperidine Sulfonamide Cav2.2 Channel Inhibitors for the Treatment of Chronic Pain>, Electric Literature of 5335-40-0, the main research area is aminopiperidine sulfonamide preparation calcium channel analgesic SAR.

The voltage-gated calcium channel Cav2.2 (N-type calcium channel) is a critical regulator of synaptic transmission and has emerged as an attractive target for the treatment of chronic pain. We report here the discovery of sulfonamide-derived, state-dependent inhibitors of Cav2.2. In particular, 19 (I) is an inhibitor of Cav2.2 that is selective over cardiac ion channels, with a good preclin. PK and biodistribution profile. This compound exhibits dose-dependent efficacy in preclin. models of inflammatory hyperalgesia and neuropathic allodynia and is devoid of ancillary cardiovascular or CNS pharmacol. at the doses tested. Importantly, 19 exhibited no efficacy in Cav2.2 gene-deleted mice. The discovery of metabolite 26 confounds further development of members of this aminopiperidine sulfonamide series. This discovery also suggests specific structural liabilities of this class of compounds that must be addressed.

Journal of Medicinal Chemistry published new progress about Allodynia. 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, Electric Literature of 5335-40-0.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Nishimura, Yoko; Morikawa, Yuji; Kondo, Chiaki; Tonomura, Yutaka; Fukushima, Ryou; Torii, Mikinori; Uehara, Takeki published the artcile< Genomic biomarkers for cardiotoxicity in rats as a sensitive tool in preclinical studies>, HPLC of Formula: 6055-19-2, the main research area is isoproterenol hydrochloride cyclosporin A Spp1 gene biomarker; cardiac troponin; cardiotoxicity; drug development; genomic biomarker; toxicogenomics.

The development of safer drugs is a high priority for pharmaceutical companies. Among the various toxicities caused by drugs, cardiotoxicity is an important issue because of its lethality. In addition, cardiovascular toxicity leads to the attrition of many drug candidates in both preclin. and clin. phases. Although histopathol. and blood chem. examinations are the current gold standards for detecting cardiotoxicity in preclin. studies, the large number of withdrawals from clin. studies owing to safety problems indicate that a more sensitive tool is required. We recently identified 32 genes that were candidate genomic biomarkers for cardiotoxicity in rats. Based on their functions, the present study focused on 8 of these 32 genes (Spp1, Fhl1, Timp1, Serpine1, Bcat1, Lmcd1, Rnd1 and Tgfb2). Diagnostic accuracy for the genes was determined by a receiver-operating characteristic (ROC) anal. using more cardiotoxic and non-cardiotoxic compounds In addition, an optimized support vector machine (SVM) model that was composed of Spp1 and Timp1 was newly constructed. This new multi-gene model exhibited a much higher diagnostic accuracy than that observed for plasma cardiac troponin I (cTnI), which is one of the most useful plasma biomarkers for cardiotoxicity detection. Furthermore, we determined that this multi-gene model could predict potential cardiotoxicity in rats in the absence of any cardiac histopathol. lesions or elevations of plasma cTnI. Overall, this multi-gene model exhibited advantages over classic tools commonly used for cardiotoxicity evaluations in rats. Our current results suggest that application of the model could potentially lead to the production of safer drugs. Copyright © 2013 John Wiley & Sons, Ltd.

Journal of Applied Toxicology published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (Bcat1). 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, HPLC of Formula: 6055-19-2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Jiang, Yansong; Lu, Zijing; Wang, Pengcheng; Xu, Jianing; Wang, Li; Fan, Yong published the artcile< Immobilized dyes within anionic indium coordination polymer for photocatalytic 1O2 generation>, Product Details of Cl3H8InO4, the main research area is immobilized dye anionic indium coordination polymer photocatalytic singlet oxygen.

A new anionic indium coordination polymer, (Me2NH2)[In(OH-BDC)2]·H2O (1), has been designed and synthesized under solvothermal conditions based on organic ligand 5-hydroxyisophthalic acid. 1 exhibits a 2D layered structure with rhombic windows, which is stacked to form 3D supramol. network by the π-π stacking interactions of Ph rings of ligand in adjacent layers. It not only shows excellent resistance to acid or basic conditions but also has good tolerance to various common solvents. Moreover, due to the neg. charge of the host framework, it shows remarkable selective adsorption for pos. charge dyes such as methylene blue (MB), rhodamine B (RhB) and crystal violet (CV), and the removal rates are higher than 90%. In particular, the adsorption capability of 1 to RhB is higher than most CPs based adsorbents. In addition, MB@1 is a high-efficiency reactive oxygen species (ROS) producer with good photocatalytic activity for the oxidation of 1,5-dihydroxynaphthalene (1,5-DHN) and can be recycled five times without loss of activity. To our knowledge, it is the first time that dye@CP was used for ROS production and photooxidation of 1,5-DHN.

Microporous and Mesoporous Materials published new progress about Adsorption. 22519-64-8 belongs to class chlorides-buliding-blocks, and the molecular formula is Cl3H8InO4, Product Details of Cl3H8InO4.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Wei, Chang; Wei, Xian; Hu, Zhe; Yang, Dan; Mei, Shiliang; Zhang, Guilin; Su, Danlu; Zhang, Wanlu; Guo, Ruiqian published the artcile< A fluorescent probe for Cd2+ detection based on the aggregation-induced emission enhancement of aqueous Zn-Ag-In-S quantum dots>, Quality Control of 22519-64-8, the main research area is zinc silver indium sulfur quantum dot fluorescent probe cadmium.

A sensitive and selective fluorescent probe for the cadmium ion (Cd2+) was developed based on the aggregation-induced emission enhancement (AIEE) of Zn-Ag-In-S quantum dots (ZAIS QDs). The QDs were synthesized by a convenient hydrothermal method with L-cysteine as ligands, with the average size of 3.2 nm and the emission peak at 520 nm. The interference study indicated the good selectivity of the probe. It has a broad detection range from 25μM to 2 mM and the detection limit is 1.56μM. AIEE is triggered by the interaction between Cd2+ and thiol groups on the surface of QDs, which causes weaker electrostatic repulsion between QDs and the passivation of surface defects. To the best of our knowledge, this is the first report on the AIEE of quaternary QDs. The method was successfully applied to the determination of Cd2+ in water samples with recoveries between 98.1% and 103.3%. This work shows its potential as a candidate for Cd2+ detection and provides a new understanding of AIEE.

Analytical Methods published new progress about Absorption. 22519-64-8 belongs to class chlorides-buliding-blocks, and the molecular formula is Cl3H8InO4, Quality Control of 22519-64-8.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Franquet-Griell, Helena; Medina, Andres; Sans, Carme; Lacorte, Silvia published the artcile< Biological and photochemical degradation of cytostatic drugs under laboratory conditions>, Safety of 2-(Bis(2-chloroethyl)amino)-1,3,2-oxazaphosphinane 2-oxide hydrate, the main research area is biol photochem degradation cytostatic drug water wastewater; Advanced oxidation processes; Biodegradation; Cytostatic drugs; Kinetics; Photolysis.

Cytostatic drugs, used in chemotherapy, have emerged as new environmental contaminants due to their recurrent presence in surface waters and genotoxic effects. Yet, their degradability and environmental fate is largely unknown. The aim was to determine the degradation kinetics of 16 cytostatic drugs, prioritized according to their usage and occurrence in hospital and wastewater treatment plants (WWTP) effluents, through the following laboratory scale processes: hydrolysis, aerobic biodegradation, UV-C photolysis, UV-C/H2O2 and simulated solar radiation. Some drugs were unstable in milli-Q water (vincristine, vinblastine, daunorubicin, doxorubicin and irinotecan); others were photodegraded under UV-C light (melphalan and etoposide) but some others were recalcitrant to biodegradation and/or UV-C, making necessary the use of advanced oxidation processes (AOPs) such as UV-C/H2O2 for complete elimination (cytarabine, ifosfamide and cyclophosphamide). Radiation in a solar box was used to simulate the fate of cytostatic drugs in surface waters under natural radiation and complete removal was not observed for any drug. The degradation process was monitored using liquid chromatog. coupled to high resolution mass spectrometry and pseudo-1st order kinetic degradation constants were calculated This study provides new data on the degradability of cytostatic compounds in water, thus contributing to the existing knowledge on their fate and risk in the environment.

Journal of Hazardous Materials published new progress about Antiproliferative agents. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Safety of 2-(Bis(2-chloroethyl)amino)-1,3,2-oxazaphosphinane 2-oxide hydrate.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Jiang, Zhongyong; Li, Kun; Cai, Xiaoyan; Chubenko, Eugene; Bondarenko, Vitaly; Mao, Liang; Zhao, Yulong; Gu, Xiuquan published the artcile< Enhanced performance of FeOOH/ZnIn2S4/Au nanosheet arrays for visible light water splitting>, Computed Properties of 22519-64-8, the main research area is iron oxyhydroxide zinc indium sulfide gold nanosheet water splitting.

Carrier separation, charge transport, and visible light absorption are the main factors affecting the solar water splitting performance of a semiconductor photoanode. In this work, ZnIn2S4 (ZIS) nanosheet arrays (NSAs) were prepared by a hydrothermal route on a transparent fluorine-doped tin oxide (FTO) substrate, which was followed by a modification with an amorphous FeOOH thin layer. The surface morphol. of ZIS NSAs was shown not to change regardless of whether Au was used as the seeding layer. Besides, the effect of the FeSO4 solution concentration on the morphol., optical absorption, and photoelectrochem. (PEC) performance was investigated. The PEC measurements showed that at the 1.23 V bias relative to RHE (VRHE), the FeOOH/ZIS/Au optical photoanodes exhibited a 4.5 and 1.9 times higher photocurrent d. than the ZIS/FTO and ZIS/Au/FTO electrodes, resp. For the 0.05Fe/ZIS/Au/FTO samples, the 0.91 mA cm-2 initial photocurrent d. was achieved at VRHE of 1.23 V. The FeOOH/Au/ZIS photoanodes also displayed a maximum H2 yield amount of 26.2μmol cm-2 h-1. It was also observed that the enhanced PEC performance may be resulted from the synergistic effect of the FeOOH top decoration and Au under layer. Specifically, FeOOH facilitated the hole injection into the electrolyte, while Au NPs provided a number of sinks for the electron transport to the FTO substrates.

Journal of Materials Science: Materials in Electronics published new progress about Band gap. 22519-64-8 belongs to class chlorides-buliding-blocks, and the molecular formula is Cl3H8InO4, Computed Properties of 22519-64-8.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Nakahara, Takako; Sakaeda, Toshiyuki; Nakamura, Tsutomu; Tamura, Takao; Nishioka, Chiharu; Aoyama, Nobuo; Okamura, Noboru; Shirakawa, Toshiro; Gotoh, Akinobu; Kamigaki, Takashi; Ohno, Masakazu; Kuroda, Yoshikazu; Matsuo, Masafumi; Kasuga, Masato; Okumura, Katsuhiko published the artcile< Chemosensitivity Assessed by Collagen Gel Droplet Embedded Culture Drug Sensitivity Test, and MDR1, MRP1, and MRP2 mRNA Expression in Human Colorectal Adenocarcinomas>, Safety of 2-(Bis(2-chloroethyl)amino)-1,3,2-oxazaphosphinane 2-oxide hydrate, the main research area is chemosensitivity test multidrug resistance antitumor colorectal adenocarcinomas.

Purpose: To evaluate chemosensitivity and its correlation with expression levels of the multidrug resistant transporter (MDR1) and the multidrug resistance-associated proteins 1 and 2 (MRP1, MRP2) mRNA in human colorectal adenocarcinomas. Methods: Colorectal adenocarcinomas were obtained as surgical samples from 25 patients. The chemosensitivity of 12 anticancer drugs was assessed by the collagen gel droplet embedded culture drug sensitivity test (CD-DST). The expression levels of MDR1, MRP1, and MRP2 mRNA in colorectal adenocarcinomas were also evaluated by real-time quant. reverse transcription-polymerase chain reaction (RT-PCR). Results: The chemosensitivity was successfully evaluated for 16 of 25 patients, and the anticancer drugs were effective against the samples showing a relatively high growth rate. Gemcitabine hydrochloride was found to be more promising than those often prescribed for the treatment of colorectal adenocarcinoma. There was no correlation of the mRNA expression levels of MDR1 and MRP1 with the chemosensitivity of any anticancer drugs tested, but mitomycin C was found to be more effective for the colorectal adenocarcinoma with relatively high expression of MRP2 mRNA.

Pharmaceutical Research published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (MRP1). 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Safety of 2-(Bis(2-chloroethyl)amino)-1,3,2-oxazaphosphinane 2-oxide hydrate.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Atli Sekeroglu, Zulal; Gediz Erturk, Aliye; Kontas Yedier, Seval; Sekeroglu, Vedat published the artcile< In vitro cytogenetic activity of 3-amino-4-[4-(dimethylamino)phenyl]-4,5-dihydro-1,2,5-thiadiazole 1,1-dioxide>, Reference of 6055-19-2, the main research area is amino dimethylamino phenyl dihydro thiadiazole dioxide cytogenetic activity; 1,2,5-Thiadiazole 1,1-dioxide; chromosome aberrations; cytotoxicity; lymphocytes; micronucleus.

In a previous study, 3-amino-4-[4-(dimethylamino)phenyl]-4,5-dihydro-1,2,5-thiadiazole 1,1-dioxide (DPTD), which is five-membered cyclosulfamide, was synthesized and structurally characterized. The aim of this study was to investigate the cytotoxic and genotoxic effects of DPTD on cultured human lymphocytes in the presence and absence of a metabolic activation system (S9 mix). The cytotoxicity and genotoxicity of DPTD in human peripheral blood lymphocytes were examined in vitro by using chromosomal aberration (CA) and micronucleus (MN) tests. Mitomycin-C (MMC) for cultures without S9 mix and cyclophosphamide monohydrate (CP) for cultures with S9 mix were used as pos. controls. The cultures were treated with DPTD (45, 90, and 180μg/mL) in the absence and presence of S9 mix. The cells were also co-treated with DPTD together with MMC or CP. DPTD showed cytotoxic activity due to decreases in mitotic index (MI) and nuclear division index (NDI) in the absence and presence of S9 mix. DPTD also increased the CAs, aberrant cells with CAs and MN values in cultures with and without S9 mix. When DPTD and MMC or CP were used together, lower MI and NDI values and higher CA and MN values were found than those DPTD treated alone. Both DPTD and its metabolites have cytotoxic, cytostatic and genotoxic potential on human peripheral blood lymphocyte cultures under the exptl. conditions. Furthermore, co-treatment of DPTD and MMC or CP can cause more cytotoxicity and genotoxicity. Our results indicated that the use of DPTD with other chemotherapeutic drugs may display more effective results.

Drug and Chemical Toxicology (1977) published new progress about Genotoxicity. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Reference of 6055-19-2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Hsu, Ya- Ling; Hung, Jen-Yu; Tsai, Eing-Mei; Wu, Cheng-Ying; Ho, Ya-Wen; Jian, Shu-Fang; Yen, Meng-Chi; Chang, Wei-An; Hou, Ming-Feng; Kuo, Po-Lin published the artcile< Benzyl butyl phthalate increases the chemoresistance to doxorubicin/cyclophosphamide by increasing breast cancer-associated dendritic cell-derived CXCL1/GROα and S100A8/A9>, Formula: C7H17Cl2N2O3P, the main research area is benzyl butyl phthalate doxorubicin cyclophosphamide chemoresistance breast cancer; CXCL1 GFO S100A8A9 dendritic cell breast cancer chemoresistance.

Phthalates are used as plasticizers in the manufacture of flexible vinyl, which is used in food contact applications. Phthalates have been demonstrated to have an adverse impact on human health, particularly in terms of cancer development. In the present study, we showed for the first time that benzyl Bu phthalate (BBP) potentiates the effect of tumor-associated dendritic cells (TADCs) on the chemoresistance of breast cancer. Specific knockdown anal. revealed that S100A9 is the major factor responsible for the chemoresistance of doxorubicin/cyclophosphamide induced by BBP-stimulated TADCs in breast cancer. BBP exposure also increased tumor infiltrating myeloid-derived suppressor cell (MDSC) secretion of S100A8/A9, thereby exacerbating the resistance of breast cancer to doxorubicin with cyclophosphamide. In addition, BBP also stimulated the production of CXCL1/GROα by TADCs, which increased the angiogenesis of breast cancer in a mouse model. Inhibition of CXCL1/GROα by a neutralizing antibody, decreased the BBP-induced angiogenesis induced by BBP after chemotherapy in the mouse model. These results, for the first time, provide evidence that BBP influences the efficacy of chemotherapy by remodeling the tumor microenvironment of breast cancer.

Oncology Reports published new progress about Angiogenesis. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Formula: C7H17Cl2N2O3P.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics