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Chemical & Pharmaceutical Bulletin

Tatsuya Hirano, Tomohiko Kinoshita, Daichi Kazamori, Satoshi Inoue, Kouji Nishimura, Asuka Sakurai, Kensuke Ohishi, Yasuhiro Kuramoto, Hirotaka Amano, Akira Yazaki
WFQ-101 with a unique N-1 substituent, 5-amino-4-fluoro-2-(hydroxymethyl)phenyl group, was selected as a lead compound through combination screening based on antimicrobial activity and the efflux index against quinolone-resistant (QR) Pseudomonas aeruginosa (P. aeruginosa). Through structural optimization, we identified WFQ-228 as a novel fluoroquinolone antibiotic candidate. WFQ-228 had potent and superior activity in comparison to levofloxacin (LVX) and ciprofloxacin (CIP) against clinical isolates of P. aeruginosa, Escherichia coli and Acinetobacter baumannii, including QR strains...
January 11, 2018: Chemical & Pharmaceutical Bulletin
Yo Muraki, Midori Yamasaki, Hirohisa Takeuchi, Kimio Tohyama, Noriyasu Sano, Takanori Matsuo
Pulmonary hypertension (PH) is a life-threatening lung disease. Despite the availability of several approved drugs, the development of a new treatment method is needed because of poor prognosis. Tissue selective drug delivery systems can avoid the adverse effects of current therapy and enhance efficacy. We evaluated the possibility of delivering drugs to the lungs of a PH rat model using fluorescence dye-labeled nanosized liposomes. To evaluate the tissue distribution following systemic exposure, fluorescent dye-labeled, 40-180 nm liposomes with and without polyethylene glycol (PEG) were intravenously administered to a monocrotaline-induced PH (MCT) rat model and tissue fluorescence was measured...
January 6, 2018: Chemical & Pharmaceutical Bulletin
Shuoqian Liu, Jorge Freire da Silva Ferreira, Dongming Tian, Yuwei Tang, Liping Liu, Wei Yang, Zhonghua Liu, Na Tian
In order to make full use of artemisinin production waste and thus to reduce the production cost of artemisinin, we developed an efficient and scalable method to isolate high-purity dihydroartemisinic acid from artemisinin production waste by combining anion-exchange resin with silica-gel column chromatography. The adsorption and desorption characteristics of dihydroartemisinic acid on 10 types of anion-exchange resin were investigated, and the results showed that the 717 anion-exchange resin exhibited the highest capacity of adsorption and desorption to dihydroartemisinic acid...
December 28, 2017: Chemical & Pharmaceutical Bulletin
Khaled M Elamin, Yuki Yamashita, Taishi Higashi, Keiichi Motoyama, Hidetoshi Arima
Methyl-β-cyclodextrin (M-β-CyD) exhibits cytotoxic activity, and has the potentials as an antitumor agent. However, a tumor-selectivity of M-β-CyD is low, leading to low antitumor activity and the adverse effects. Meanwhile, hyaluronic acid (HA) is known as a promising tumor targeting ligand, because various cancer cells overexpress CD44, a HA-binding glycoprotein. In the present study, to develop a tumor-selective delivery system for M-β-CyD, we designed a supramolecular complex of M-β-CyD with adamantane-grafted HA (Ad-HA/M-β-CyD) and evaluated it as a tumor-selective antitumor agent...
December 22, 2017: Chemical & Pharmaceutical Bulletin
San-Qing Lin, Zhong-Liu Zhou, Chun-Yan Li
Cyprotuoside C (1) and cyprotuoside D (2), two new cycloartane glycosides were isolated from the ethanol extract of the rhizomes of Cyperus rotundus. Their structures were identified as 24R-9, 10-seco-cycloartan-1 (10), 9 (11)-dien-3β, 7β, 24, 25-tetraol 3-O-β-D-xylopyranosyl-(1→4)-[α-L-arabinopyranosyl-(1→6)]-β-D-glucopyranosyl-25-O-β-D-glucuronide (1) and 9, 10-seco-cycloartan-1 (10), 9 (11), 23 (24)-trien-3β, 7β, 25-triol 3-O-β-D-xylopyranosyl-(1→4)-{α-L-arabinopyranosyl-(1→6)-[ α-L-rhamnopyranosyl-(1→2)-]}-β-D-glucopyranosyl-25-O-β-D-glucuronide (2) by spectroscopic methods...
November 9, 2017: Chemical & Pharmaceutical Bulletin
Jie Li, Tu-Cai Zheng, Yi Jin, Jian-Guo Xu, Jian-Gang Yu, Yan-Wen Lv
A series of novel quinolone derivatives (8a-j) were synthesized, and their anticancer activities were tested in human cancer cell lines A549, HL-60, and Hela. Compound 8i was found to be 5-times more potent in cell-killing activity for cell lines A549, HL-60, and Hela than the positive control irinotecan or cisplatin, with IC50 of 0.009, 0.008 and 0.010 μM, respectively. The docking study revealed that compound 8i might have strong interactions with the active site of DNA-Topoisomerase I.
November 9, 2017: Chemical & Pharmaceutical Bulletin
Bancha Yingngam, Adelheid H Brantner, Damrongsak Jinarat, Rawiwun Kaewamatawong, Wandee Rungseevijitprapa, Apichart Suksamrarn, Pawinee Piyachaturawat, Ratchanaporn Chokchaisiri
A method for quantification of diarylheptanoids in Curcuma comosa rhizomes and selected pharmaceutical preparations was established by using HPLC-DAD. The chromatographic separation of three diarylheptanoids [(3S)-1-(3,4-dihydroxy-phenyl)-7-phenyl-(6E)-6-hepten-3-ol (1), (3R)-1,7-diphenyl-(4E,6E)-4,6-heptadien-3-ol (2), and (3S)-1,7-diphenyl-(6E)-6-hepten-3-ol (3)] was performed on a Luna C18 analytical column using gradient elution with 0.5% acetic acid in water and acetonitrile with a flow rate of 1 mL/min and a column temperature of 35 °C...
October 26, 2017: Chemical & Pharmaceutical Bulletin
Akira Katsuyama, Kousuke Sato, Fumika Yakushiji, Takanori Matsumaru, Satoshi Ichikawa
A solid-phase synthesis of Park nucleotide as well as lipids I and II analogues, which is applicable to the synthesis of a range of analogues, is described in this work. This technique allows highly functionalized macromolecules to be modularly labeled. Multiple steps are used in a short time (4 d) with a single purification step to synthesize the molecules by solid-phase synthesis.
2018: Chemical & Pharmaceutical Bulletin
Won Se Suh, Oh Kil Kwon, Tae Hyun Lee, Lalita Subedi, Sun Yeou Kim, Kang Ro Lee
Two new secoiridoid glycosides, obtusifolisides A and B (1, 2), together with 7 known secoiridoid glycosides (3-9) were isolated from the twigs of Ligustrum obtusifolium. The chemical structures of new compounds were determined by a spectroscopic data analysis, including one and two dimensional (1D-, 2D)-NMR, High resolution-MS, and experiments involving chemical reactions. The isolated secoiridoid glycosides were evaluated for their anti-inflammatory effects in lipopolysaccharide (LPS)-stimulated BV-2 murine microglia cells...
2018: Chemical & Pharmaceutical Bulletin
Tamami Haraguchi, Takahiro Uchida, Miyako Yoshida, Honami Kojima, Masaaki Habara, Hidekazu Ikezaki
The purpose of this study was to examine the ability of the artificial taste sensor to evaluate the bitterness of drugs by comparing the responses of the taste sensor with documented responses of human TASTE2 receptors (hTAS2Rs). For this purpose 22 bitter compounds, used as ingredients of pharmaceutical medicines in Japan and known ligands of hTAS2Rs, were selected for testing. Their solutions (0.01, 0.03, 0.1 mM) were evaluated by five different taste sensors (AC0, AN0, BT0, C00, AE1). Correlations between physicochemical parameters of the compounds and the responses of the taste sensors and hTAS2Rs were evaluated...
2018: Chemical & Pharmaceutical Bulletin
Thiago Inácio Barros Lopes, Roberta Gomes Coelho, Neli Kika Honda
Several applications have been proposed for tyrosinase inhibitors in the pharmaceutical, food bioprocessing, and environmental industries. However, only a few compounds are known to serve as effective tyrosinase inhibitors. This study evaluated the tyrosinase-related activity of resorcinol (1), orcinol (2) lecanoric acid (3), and derivatives of this acid (4-15). Subjected to alcoholysis, lecanoric acid (3), a depside isolated from the lichen Parmotrema tinctorum, produces orsellinic acid (2,4-dihydroxy-6-methylbenzoic acid) (4) and orsellinates (2,4-dihydroxy-6-methyl benzoates) (5-15)...
2018: Chemical & Pharmaceutical Bulletin
Nanami Murakami, Misaki Yoshida, Tatsuhiko Yoshino, Shigeki Matsunaga
Cp*Co(III)-catalyzed (Cp*=pentamethylcyclopentadienyl) C-H bond functionalization of 6-arylpurines using gem-difluoroalkenes and allyl fluorides is described. The reaction with gem-difluoroalkenes afforded monofluoroalkenes with high (Z)-selectivity, while the reaction with allyl fluorides led to C-H allylation in moderate (Z)-selectivity. Both reactions proceeded using a user-friendly single-component catalyst [Cp*Co(CH3CN)3](SbF6)2 in fluorinated alcohol solvents without any additives. Robustness was also demonstrated by a preparative-scale reaction under air...
2018: Chemical & Pharmaceutical Bulletin
Kaori Sakurai
Cell surface glycolipids are implicated in the formation of lipid rafts and membrane microdomains, where they interact with protein receptors to mediate a variety of cellular processes such as cell-cell recognition, cell adhesion, and membrane signaling. Studies of glycolipid function at the local membrane structures have not been straightforward to date, because the locally clustered structures are labile and their protein binding affinities tend to be weak. While specific glycolipid-binding proteins have been employed as molecular probes for detecting lipid rafts, small peptides may be more suitable for probing glycolipids at the cell surface due to their small size as well as their ease of synthetic preparation and functionalization...
2018: Chemical & Pharmaceutical Bulletin
Kentaro Takai, Takeshi Enomoto
Among the muscarinic acetylcholine receptor (mAChR) subtypes, the M4 receptor has been investigated as a promising drug target for the treatment of schizophrenia. These investigations have been based on findings from M4-deficient mice studies as well as on the results of a clinical trial that used xanomeline, an M1/M4 mAChRs-preferring agonist. Both orthosteric agonists and positive allosteric modulators of M4 mAChR have been reported as promising ligands that not only have antipsychotic effects, but can also improve cognitive impairment and motor dysfunction...
2018: Chemical & Pharmaceutical Bulletin
Takayuki Irie, Masaaki Sawa
The majority of kinase inhibitors have been developed as ATP competitors to interact with a hinge region in ATP binding sites of kinases. 7-Azaindole has been found as an excellent hinge binding motif by making two hydrogen bonds with the kinase hinge region. Vemurafenib, a B-RAF kinase (serine-threonine kinase [STK]) inhibitor approved by the U.S. Food and Drug Administration (FDA) for the treatment of melanoma, was created from this simple 7-azaindole fragment by successful use of structure-based drug design techniques...
2018: Chemical & Pharmaceutical Bulletin
Yoshinari Sawama, Kwihwan Park, Tsuyoshi Yamada, Hironao Sajiki
Deuterium-labeled compounds are widely utilized in various scientific fields. We summarize the recent advances in the direct deuteration of sugar, saturated fatty acid, and arene derivatives using heterogeneous platinum group metal on carbon catalysts by our research group. Hydrogen gas is a key catalyst-activator to facilitate the present H-D exchange reactions. In this review, the direct activation method of catalysts using in situ-generated hydrogen based on the dehydrogenation of alcohols is introduced...
2018: Chemical & Pharmaceutical Bulletin
Takaaki Sumiyoshi
No abstract text is available yet for this article.
2018: Chemical & Pharmaceutical Bulletin
(no author information available yet)
No abstract text is available yet for this article.
2018: Chemical & Pharmaceutical Bulletin
Satoru Tamura, Keigo Sato, Tomikazu Kawano
A versatile N-alkylation was performed using sodium triacetoxyborohydride and carboxylic acid as an alkyl source. The combination of these reagents furnished products different from those given previously by a similar reaction. Moreover, the mild conditions of our method allowed some functional groups to remain through the reaction, whereas they would react and be converted into other moieties in the similar reductive N-alkylation reported previously. Herein, we provide a new procedure for the preparation of various compounds containing nitrogen atoms...
2018: Chemical & Pharmaceutical Bulletin
Hideyuki Konishi
The use of toxic gas surrogates in organic reactions instead of the gas itself contributes to enhancing the safety, practicality, and efficiency of the reactions involved. Our efforts toward the creation of toxic gas surrogates and the development of a series of catalytic reactions using these surrogates are described. Improvements in substrate scope during the hydroesterification of alkenes using formates facilitated by the Ru-imidazole catalyst system provided the opportunity to discover that phenyl formate is a useful carbon monoxide (CO) surrogate for the generation of CO and phenol under weakly basic conditions...
2018: Chemical & Pharmaceutical Bulletin
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