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Chemical & Pharmaceutical Bulletin

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https://www.readbyqxmd.com/read/28163272/a-study-of-the-strength-of-a-template-molecule-a-functional-monomer-interaction-that-affects-the-performance-of-molecularly-imprinted-polymers-and-its-application-to-chiral-amplification
#1
Takuro Yasuyama, Hirofumi Matsunaga, Shin Ando, Tadao Ishizuka
A novel type of molecularly imprinted polymer (MIP), N-benzoyl-(S)-valine anilide-imprinted polymer (IP-2), was prepared using hydrogen-bonding interactions as a main force in the pre-polymerization step. The performance of the IP-2 was evaluated via batch procedure and compared with a (S)-valine anilide-imprinted polymer (IP-1) that was prepared using an ionic interaction that is stronger than hydrogen bonding. Although both polymers showed a preferential adsorbability for (S)-amino acid derivatives, different performances were observed in terms of adsorbability and enantioselectivity...
February 4, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28132960/selective-targeting-of-cancer-stem-cells-by-2-aminodihydroquinoline-analogs
#2
Heejoo Park, Yeongji Yu, Hyejin Kim, Eun Lee, Hani Lee, Raok Jeon, Woo-Young Kim
Many aminodihydroquinoline compounds have been studied to determine their cytotoxicity to cancer cells. However, anti- cancer stem cells (CSCs) activity of aminodihydroquinoline has not been tested in spite that CSC is believed to do an important roles in chemotherapy resistance and recurrence. The CSC selective targeting activities of 10 recently synthesized 2-aminodihydroquinoline analogs were examined on CSCs and bulk culture of a glioblastoma cell line. A diethylaminopropyl substituted aminodihydroquinoline, 5h, showed a strong anti-CSC effect and general cytotoxicity...
January 27, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28090067/discovery-and-synthesis-of-amino-acids-modified-deoxycholic-acid-derivatives-and-in-vitro-antiproliferative-evaluation
#3
Chunhui Zhao, Peizhe Zhao, Bin Feng, Xiyan Hou, Longxuan Zhao
A series of deoxycholic acid (DCA) derivatives bearing amino acid moiety has been synthesized and investigated for their potential antiproliferative activities. DCA derivative compounds were synthesized by a two or three step synthetic approach. Their bioactivities were evaluated using MTT method and Western blotting analysis on three tumor cell lines A549, MCF-7 and HeLa. The novel derivatives DCA3d, DCA5a, DCA5b, DCA5c, and DCA5d were found to be promising antiproliferative agents. Furthermore, DCA5b showed the greatest cytotoxic activity by induction of apoptosis...
January 13, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28077809/cytotoxic-steroids-from-the-vietnamese-soft-coral-sinularia-conferta
#4
Ninh Thi Ngoc, Pham Thi Mai Huong, Nguyen Van Thanh, Nguyen Thi Phuong Chi, Nguyen Hai Dang, Nguyen Xuan Cuong, Nguyen Hoai Nam, Do Cong Thung, Phan Van Kiem, Chau Van Minh
Twelve steroids, including five new compounds 1-5, were isolated and structurally elucidated from a methanol extract of the Vietnamese soft coral Sinularia conferta. Their cytotoxic effects against three human cancer cell lines, lung carcinoma (A-549), cervical adenocarcinoma (Hela), and pancreatic epithelioid carcinoma (PANC-1), were evaluated using 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide (MTT) assays. Among isolated compounds, 10 exhibited potent cytotoxic effects on all three tested cell lines with IC50 values of 3...
January 12, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27980251/preparation-and-characterization-of-hydroxypropyl-methylcellulose-polycarbophil-mucoadhesive-blend-films-using-a-mixture-design-approach
#5
Pakorn Kraisit, Sontaya Limmatvapirat, Jurairat Nunthanid, Pornsak Sriamornsak, Manee Luangtana-Anan
The objectives of this study were to prepare the hydroxypropyl methylcellulose (HPMC)/polycarbophil (PC) mucoadhesive blend film and to investigate the main and interaction effect of HPMC and PC mixtures on the physicochemical and mechanical properties of blend films using a simplex lattice mixture design approach. The cubic and quadratic models were selected to analyze mucoadhesive properties in terms of work of adhesion and maximum detachment force, respectively. It was shown that HPMC/PC blend film had higher mucoadhesive properties than pure HPMC film...
December 16, 2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27928130/application-of-terahertz-attenuated-total-reflection-spectroscopy-to-detect-changes-in-the-physical-properties-of-lactose-during-the-lubrication-process-required-for-drug-formulation
#6
Masafumi Dohi, Wataru Momose, Kazunari Yamashita, Tadashi Hakomori, Shusaku Sato, Shuji Noguchi, Katsuhide Terada
Manufacturing the solid dosage form of an orally administered drug requires lubrication to enhance manufacturability, ensuring that critical quality attributes such as disintegration and dissolution of the drug product are maintained during manufacture. Here, to evaluate lubrication performance during manufacture, we used terahertz attenuated total reflection (THz-ATR) spectroscopy to detect differences in the physical characteristics of the lubricated powder. We applied a simple formulation prepared by blending granulated lactose as filler with magnesium stearate as lubricant...
December 6, 2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27916782/cytotoxic-homoisoflavonoids-from-ophiopogon-japonicus-tubers
#7
Nguyen Hai Dang, Nguyen Dinh Chung, Ha Manh Tuan, Nguyen Tuan Hiep, Nguyen Tien Dat
A phytochemical fractionation of a methanol extract of Ophiopogon japonicus tubers led to the isolation of a new homoisoflavanone, homoisopogon A (1), and three new homoisoflavanes, homoisopogon B-D (2-4). Their chemical structures were elucidated by mass, NMR, and CD spectroscopic methods. Homoisopogon A (1) exhibited potent cytotoxicity against LU-1, KB, and SK-Mel-2 cancer cells with IC50 values ranging from 0.51 to 0.66 μM.
December 3, 2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27904016/the-measurement-of-meloxicam-and-meloxicam-metabolites-in-rat-plasma-using-a-high-performance-liquid-chromatography-ultraviolet-spectrophotometry-method
#8
Aoi Miyamoto, Takahiko Aoyama, Yoshiaki Matsumoto
A high-performance liquid chromatography-ultraviolet spectrophotometry (HPLC-UV) method for the determination of meloxicam (MEL) and meloxicam metabolites (5'-hydroxy meloxicam (5-HMEL) and 5'-carboxy meloxicam (5-CMEL)) has been developed. After extraction of MEL, 5-HMEL, and 5-CMEL from rat plasma using Oasis HLB cartridges, the extracts were separated with a Luna C18 (2) 100 A column (5 μm, 4.6 × 150 mm, Phenomenex) using a mobile phase of 50 mM phosphate buffer (pH 2.15, solvent A) and acetonitrile (solvent B) at a flow rate of 0...
December 1, 2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27904030/formulation-optimization-and-in-vitro-characterization-of-orally-disintegrating-films-using-a-factorial-design-and-mathematical-modeling-for-drug-release
#9
Yeongbin Lee, Prakash Thapa, Seong Hoon Jeong, Mi Hee Woo, Du Hyung Choi
Even though experimental designs are becoming popular especially for conventional dosage forms, limited studies have been performed to optimize formulations of orally disintegrating films (ODFs). This study aimed to evaluate sildenafil citrate-loaded ODFs for a controlled release with hydroxypropyl methylcellulose as a film-forming polymer. A factorial design was utilized for optimization with three control factors: ethanol ratio, plasticizer ratio, and the type of plasticizer. Tensile strength, disintegration time, water contact angle, and thickness were chosen as responses...
November 30, 2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28154312/effects-of-m%C3%AE-cd-on-lipoxygenase-induced-ldl-oxidation
#10
Meiying Ao, Yong Chen
Beta-cyclodextrin (β-CD) has been applied as drug/food carriers or potential drugs for treating some diseases. Most recently, some evidence indicated that methyl-β-cyclodextrin (MβCD) and 2-hydroxypropyl-β-cyclodextrin (2-HPβCD), two major derivatives of β-CD, may inhibit atherogenesis, implying that cyclodextrins also can be potential drugs for treating atherosclerosis. It is well known that modification (e.g. oxidation) of low-density lipoprotein (LDL) is one of the most critical steps of atherogenesis...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28154311/synthesis-of-linezolid-metabolites-pnu-142300-and-pnu-142586-toward-the-exploration-of-metabolite-related-events
#11
Kengo Hanaya, Kazuaki Matsumoto, Yuta Yokoyama, Junko Kizu, Mitsuru Shoji, Takeshi Sugai
Linezolid (1) is an oxazolidinone antibiotic that is partially metabolized in vivo via ring cleavage of its morpholine moiety to mainly form two metabolites, PNU-142300 (2) and PNU-142586 (3). It is supposed that accumulation of 2 and 3 in patients with renal insufficiency may cause thrombocytopenia, one of the adverse effects of linezolid. However, the poor availability of 2 and 3 has hindered further investigation of the clinical significance of the accumulation of these metabolites. In this paper, we synthesized metabolites 2 and 3 via a common synthetic intermediate, 4; this will encourage further exploration of events related to these metabolites and lead to improved clinical use of linezolid...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28154310/study-of-schiff-base-derived-with-dioxygenated-rings-and-nitrogen-heterocycle-as-potential-%C3%AE-ketoacyl-acyl-carrier-protein-synthase-iii-fabh-inhibitors
#12
Yang Zhou, Yu-Shun Yang, Xiao-Da Song, Liang Lu, Hai-Liang Zhu
Fatty acid synthesis (FAS) is an essential metabolism during the whole growth and development process of the bacterial. Several key enzymes which involved in this biosynthetic pathway have been considered as useful targets for the development of new antibacterial agents. Among them, β-ketoacyl-acyl carrier protein synthase III (FabH) is the most magnetic target, since it is central to the initiation of fatty acid biosynthesis and is highly conserved of both Gram-positive and Gram-negative bacteria. Following the previous researches, Schiff-based derivatives with dioxygenated rings and N-heterocycle were synthesized in succession, and their biological activities as potential FabH inhibitors were evaluated in this paper...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28154309/design-of-highly-dispersible-plga-microparticles-in-aqueous-fluid-for-the-development-of-long-acting-release-injectables
#13
Atsushi Nakashima, Tomohisa Izumi, Kazutomi Ohya, Keita Kondo, Toshiyuki Niwa
In this study, we developed highly dispersible polylactic glycolic acid (PLGA) copolymer microparticles (MRPs) in aqueous fluid. A solution containing both dissolved aripiprazole as a model drug and PLGA were spray-dried to make MRPs. The resultant MRPs were further co-processed with water-soluble additives and a surfactant to improve their dispersion behavior. The granules containing MRPs and additives, termed granulated microparticles (G-MRPs) were prepared by a newly established drop freeze-drying technique...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28154308/suppression-in-bitterness-intensity-of-bitter-basic-drug-by-chlorogenic-acid
#14
Sayuko Shiraishi, Tamami Haraguchi, Saki Nakamura, Honami Kojima, Ikuo Kawasaki, Miyako Yoshida, Takahiro Uchida
The purpose of the study was to evaluate suppression of the bitterness intensity of bitter basic drugs by chlorogenic acid (CGA) using the artificial taste sensor and human gustatory sensation testing and to investigate the mechanism underlying bitterness suppression using (1)H-NMR. Diphenhydramine hydrocholoride (DPH) was the bitter basic drug used in the study. Quinic acid (QNA) and caffeic acid (CFA) together form CGA. Although all three acids suppressed the bitterness intensity of DPH in a dose-dependent manner as determined by the taste sensor and in gustatory sensation tests, CFA was less effective than either CGA or QNA...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28154307/molecular-interaction-between-intercellular-lipids-in-the-stratum-corneum-and-l-menthol-as-analyzed-by-synchrotron-x-ray-diffraction
#15
Shinya Yoshida, Yasuko Obata, Yoshinori Onuki, Shunichi Utsumi, Noboru Ohta, Hiroshi Takahashi, Kozo Takayama
l-Menthol increases drug partitioning on the surface of skin, diffusion of drugs in the skin, and lipid fluidity in the stratum corneum and alters the rigidly arranged lipid structure of intercellular lipids. However, l-menthol is a solid at room temperature, and it is difficult to determine the effects of l-menthol alone. In this study, we vaporized l-menthol in order to avoid the effects of solvents. The vaporized l-menthol was applied to the stratum corneum or lipid models comprising composed of ceramides (CER) [EOS], the longest lipid acyl chain of the ceramides in the stratum corneum lipids that is associated with the barrier function of the skin; CER [NS], the shorter lipid acyl chain of the ceramides, and the most components in the stratum corneum of the intercellular lipids that is associated with water retention in the intercellular lipid structure of the stratum corneum; cholesterol; and palmitic acid...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28154306/taste-masking-effect-of-chlorogenic-acid-cga-on-bitter-drugs-evaluated-by-taste-sensor-and-surface-plasmon-resonance-on-the-basis-of-cga-drug-interactions
#16
Sayuko Shiraishi, Tamami Haraguchi, Saki Nakamura, Dahong Li, Honami Kojima, Miyako Yoshida, Takahiro Uchida
The purpose of this study was to evaluate the taste-masking effects of chlorogenic acid (CGA) on bitter drugs using taste sensor measurements and surface plasmon resonance (SPR) analysis of CGA-drug interactions. Six different bitter drugs were used: amlodipine besylate (AMD), diphenhydramine hydrochloride (DPH), donepezil hydrochloride (DNP), rebamipide (RBM), diclofenac sodium (DCF) and etodolac (ETD). Taste sensor outputs were significantly inhibited by the addition of CGA to all drugs. The inhibition ratio of the taste sensor output decreased in the following order DPH>DNP>AMD≈DCF≈RBM≈ETD...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049920/lignan-diesters-of-canangafruticoside-a-from-the-leaves-of-cananga-odorata-var-odorata
#17
Haruka Katsui, Sachiko Sugimoto, Katsuyoshi Matsunami, Hideaki Otsuka, Sorasak Lhieochaiphant
From the leaves of Cananga odorata var. odorata, three relatively large molecules, namely two aryl naphthalene lignan diesters of canangafruticoside A and one cyclobutane lignan diester of canangafruticoside A, were isolated along with four known compounds. The structures of the new compounds were elucidated based on spectroscopic evidence.
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049919/utility-of-pyrazolylchalcone-synthon-to-synthesize-azolopyrimidines-under-grindstone-technology
#18
Maher Abd El-Aziz El-Hashash, Sobhi Mohamed Gomha, Elham Ezz El-Arab
A series of pyrazolyl-triazolo[1,5-a]pyrimidines, pyrazolyl-tetrazolo[1,5-a]pyrimidines, pyrazolyl-benzo[4,5]imidazo[1,2-a]pyrimidines and bis-azolopyrimidines were prepared by reaction of pyrazolyl-chalcones or its bis-pyrazolyl-chalcones with the appropriate heterocyclic amines as aminotriazole, aminotetrazole, 2-aminobenzimidazole and 4,6-dimethyl-1H-pyrazolo[3,4-b]pyridin-3-amine by grinding method. The newly synthesized compounds have been characterized on the basis of elemental analysis and spectral data (IR, (1)H- and (13)C-NMR, Mass)...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049918/trialkylamine-derivatives-containing-a-triazole-moiety-as-promising-ergosterol-biosynthesis-inhibitor-design-synthesis-and-antifungal-activity
#19
Guoqing Sui, Wen Zhang, Kun Zhou, Yulin Li, Bingyu Zhang, Dan Xu, Yong Zou, Wenming Zhou
As a part of our continuing research on amine derivative antifungal agents, 19 novel target compounds containing 1,2,4-triazole and tertiary amine moieties were designed and synthesized, and their in vitro antifungal activities against six phytopathogenic fungi (Magnaporthe grisea, Alternaria solani, Fusarium solani, Curvularia lunata, A. alternata, F. graminearum) were assayed. All target compounds were elucidated by means of (1)H-NMR, (13)C-NMR, high resolution (HR)-MS, and IR analysis. The results showed that most of the derivatives exhibited obvious activity against each of the fungi at 50 µg/mL...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049917/synthesis-docking-study-and-kinase-inhibitory-activity-of-a-number-of-new-substituted-pyrazolo-3-4-c-pyridines
#20
Meropi Sklepari, Nikolaos Lougiakis, Athanasios Papastathopoulos, Nicole Pouli, Panagiotis Marakos, Vassilios Myrianthopoulos, Thomas Robert, Stéphane Bach, Emmanuel Mikros, Sandrine Ruchaud
A series of new pyrazolo[3,4-c]pyridines bearing various 1, 3, 5 or 1, 3, 7 pattern substitutions, were designed and synthesized. Some of them showed interesting inhibitory activity mainly against glycogen synthase kinase 3 (GSK3)α/β as well as against cdc2-like kinases 1 (CLK1) and dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), with good selectivity and remarkable structure-activity relationships (SARs), without being cytotoxic. Molecular simulations in correlation with biological data revealed the importance of the existence of N1-H as well as the absence of a bulky 7-substituent...
2017: Chemical & Pharmaceutical Bulletin
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