Structure-activity relationship of orally potent tripeptide-based HIV protease inhibitors containing hydroxymethylcarbonyl isostere.

abstract：:A new heptapeptide GAGPHGG (OC1) was isolated from Carapax trionycis which was a traditional Chinese medicine (TCM) used for treatment of hepatic diseases. The structure of OC1 was characterized by MS, NMR techniques, together with amino acid sequence analysis. The hepatoprotective activity of OC1 was evaluated in viv...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang P,Zhang Y,An Y,Xu K,Xu X,Fu C,Lin J,Xu S,Li Q,Lei H

更新日期：2013-01-01 00:00:00

abstract：:A new stilbene, 4-[(2"E)-7"-hydroxy-3",7"-dimethyloct-2"-enyl]-2',3,4',5-tetrahydroxy-trans-stilbene (1), and the known compound chlorophorin (2) were isolated from the heartwood of Chlorophora excelsa. Both 1 and 2 showed tyrosinase inhibitory activity with IC(50) values of 96 and 1.3 microM, respectively. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Shimizu K,Yasutake S,Kondo R

更新日期：2003-03-01 00:00:00

abstract：:Analogs related to 1 alpha,25-dihydroxy-2 beta-(3-hydroxypropoxy)vitamin D3 (ED-71) (4), oxa-type and carba-type analogs of vitamin D3 bearing substituents at the 2 beta-position of 1 alpha,25-dihydroxyvitamin D3 (1), were synthesized from the alpha-epoxides (6 and 13). Three analogs, ED-71 (4) and two carba-type anal...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono Y,Watanabe H,Shiraishi A,Takeda S,Higuchi Y,Sato K,Tsugawa N,Okano T,Kobayashi T,Kubodera N

更新日期：1997-10-01 00:00:00

abstract：:Using CPG support linked with 5-deazaflavin, the 5-deazaflavin modified oligodeoxynucleotides at 3'-end(ODN-dF1) were synthesized. The thermal stability of the duplex of ODN-dF1 with its complement was higher than that of oligonucleotide linked to 5-deazaflavin at 5'-end internucleotide linkage. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakamura Y,Akiyama T,Bessho K,Yoneda F

更新日期：1993-07-01 00:00:00

abstract：:The novel hydroxamates containing purine scaffold were designed, synthesized and screened for their biological activities as histone deacetylase (HDAC) inhibitors. Some of them exhibited excellent acti-HDACs activities and antiproliferative activities, the most promising compound was 7m'. Western blot analysis indicat...

journal_title：Chemical & pharmaceutical bulletin

authors： Xu Z,Yang Y,Mai X,Liu B,Xiong Y,Feng L,Liao Y,Zhang Y,Wang H,Ouyang L,Liu S

更新日期：2018-01-01 00:00:00

abstract：:Clotrimazole (CT)-containing proliposomes were prepared by penetrating an ethanol solution of CT and Egg phosphatidylcholine (PC) into microporous sorbitol particles, followed by vacuum evaporation of the solvent. As a result, CT proliposomes with free-flowing flowability were obtained. On contact with water, the prol...

journal_title：Chemical & pharmaceutical bulletin

authors： Ning MY,Guo YZ,Pan HZ,Yu HM,Gu ZW

更新日期：2005-06-01 00:00:00

abstract：:Caragana tibetica KOM. (Fabaceae) is a medicinal plant that has been traditionally used in western part of China. In the course of our screening study on antioxidant activity of medicinal plants, the 70% acetone extract of the stems of C. tibetica was found to have a potent superoxide anion scavenging activity. Tibeti...

journal_title：Chemical & pharmaceutical bulletin

authors： Xiang T,Uno T,Ogino F,Ai C,Duo J,Sankawa U

更新日期：2005-09-01 00:00:00

abstract：:Gadolinium-diethylenetriaminepentaacetic acid (Gd-DTPA), a paramagnetic contrast agent for use in magnetic resonance imaging (MRI) was bound to stearylamine and incorporated into the liposomal membranes (Gd-DTPA liposomes). In addition, the Gd-DTPA liposomes were coated with mannan (cholesterol-aminoethylcarbamylmethy...

journal_title：Chemical & pharmaceutical bulletin

authors： Kunimasa J,Inui K,Hori R,Kawamura Y,Endo K

更新日期：1992-09-01 00:00:00

abstract：:Italian canned tomatoes contain the tomato glycosides esculeosides B-1 (1, 0.0052%) and B-2 (2, 0.0068%) without esculeoside A. Herein, the structure of esculeoside B-1 (1) is characterized to be 3-O-β-lycotetraosyl (5S,22R,23S,25S)-22,26-epimino-16β,23-epoxy-3β,23,27-trihydroxycholestane 27-O-β-D-glucopyranoside. We ...

journal_title：Chemical & pharmaceutical bulletin

authors： Manabe H,Fujiwara Y,Ikeda T,Ono M,Murakami K,Zhou JR,Yokomizo K,Nohara T

更新日期：2013-01-01 00:00:00

abstract：:This report describes the synthesis and antiviral effects of (6'R)-6'-C-ethynyl, -ethenyl, and -ethyl derivatives of neplanocin A (7a, 8a, and 9a, respectively) and the corresponding 6'S-diastereomers (7b, 8b, and 9b, respectively), as examples of 6'-C-substituted analogues of neplanocin A. Grignard reaction of the 6'...

journal_title：Chemical & pharmaceutical bulletin

authors： Shuto S,Obara T,Saito Y,Yamashita K,Tanaka M,Sasaki T,Andrei G,Snoeck R,Neyts J,Padalko E,Balzarini J,De Clercq E,Matsuda A

更新日期：1997-07-01 00:00:00

abstract：:Three new oleanane-type saponins, giganteosides L (1), M (2) and N (3) along with eight known ones were isolated from the roots of Cephalaria gigantea. Their structures were established as 3-O-[beta-D-galactopyranosyl-(1-->2)-beta-D-glucuronopyranosyl]-28-O-[beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl]-oleanol...

journal_title：Chemical & pharmaceutical bulletin

authors： Tabatadze N,Elias R,Faure R,Gerkens P,De Pauw-Gillet MC,Kemertelidze E,Chea A,Ollivier E

更新日期：2007-01-01 00:00:00

abstract：:Asymmetric total synthesis of benzene analogues of galbonolide, a 14-membered antifungal macrolide, possessing a benzene ring instead of a conjugated diene structure, was achieved starting from chiral 1-aryl-1-propanol obtained by enzyme-catalyzed kinetic resolution with high enantioselectivity. Representatively, a me...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakoh H,Sakuraba S,Sugimoto Y,Imamura H,Jona H,Yamada K,Bamba-Nagano R,Hashizume T,Morishima H

更新日期：2004-01-01 00:00:00

abstract：:A vaginal suppository containing ulinastatin (UTI) was developed as a hospital pharmacy product from UTI injection solution and Witepsol® S-55. After mixing at 50°C for 0-8 h, UTI suppositories were prepared, which had good UTI content uniformity. Because 2% surfactant was contained in S-55, the UTI injection solution...

journal_title：Chemical & pharmaceutical bulletin

authors： Kishino T,Inoue Y,Inoue K,Saito K,Kondo M,Otsuka K,Terukina T,Hattori Y,Otsuka M

更新日期：2018-01-01 00:00:00

abstract：:The purpose of this research is to investigate the applicability of terahertz (THz) reflectance spectroscopy for quantification of drug substance in tablets, so as to demonstrate the feasibility for applying this technique to tableting process monitoring. In order to acquire a suitable absorbance spectrum for this pur...

journal_title：Chemical & pharmaceutical bulletin

authors： Hisazumi J,Watanabe T,Suzuki T,Wakiyama N,Terada K

更新日期：2012-01-01 00:00:00

abstract：:A new cardenolide diglycoside (1) was isolated from Nerium oleander together with ten known cardenolide diglycosides 2-11. The structure of compound 1 was established on the basis of their spectroscopic data. The in vitro anti-inflammatory activity of compounds 1-11 was examined on the basis of inhibitory activity aga...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhao M,Bai L,Toki A,Hasegawa R,Sakai J,Hasegawa T,Ogura H,Kataoka T,Bai Y,Ando M,Hirose K,Ando M

更新日期：2011-01-01 00:00:00

abstract：:The anti-anginal drug Ranolazine, a partial fatty acid oxidation (pFOX) inhibitor, is thought to modulate the metabolism during myocardial ischemia by activating pyruvate dehydrogenase activity to promote glucose oxidation. Ranolazine and its five principal metabolites: CVT-2512, CVT-2513, CVT-2514, CVT-2738 and CVT-4...

journal_title：Chemical & pharmaceutical bulletin

authors： Yao Z,Gong S,Guan T,Li Y,Wu X,Sun H

更新日期：2009-11-01 00:00:00

abstract：:A new resveratrol dimer and a new C-glucosyl resveratrol were isolated from stem wood of Hopea utilis along with nine stilbenoid derivatives comprising bergenin and (+)-lyoniresinol. The structures have been elucidated on the basis of the spectroscopic evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka T,Ito T,Ido Y,Nakaya K,Iinuma M,Chelladurai V

更新日期：2001-06-01 00:00:00

abstract：:A new series of 3-(5-3-methyl-5-[(3-methyl-7-5-[2-(aryl)-4-oxo-1,3-thiazolan-3-yl]-1,3,4-thiadiazol-2-ylbenzo[b]furan-5-yl)methyl]benzo[b]furan-7-yl-1,3,4-thiadiazol-2-yl)-2-(aryl)-1,3-thiazolan-4-one 5a-j has been synthesized by the reaction of N2-[(E)-1-(4-methylphenyl)methylidene]-5-(3-methyl-5-[3-methyl-7-(5-[(E)-...

journal_title：Chemical & pharmaceutical bulletin

authors： Reddy CS,Rao DC,Yakub V,Nagaraj A

更新日期：2010-06-01 00:00:00

abstract：:From Puerariae Radix, the root of Pueraria lobata (Leguminosae), six new oleanene-type triterpene glycosides, called kudzusaponins A1 (1), A2 (2), Ar (3), SA4 (5), and SB1 (6) were isolated together with kudzusaponin A3 (7), soyasaponins SA3 (8), and I (9). The structures of 1-6 were determined to be 3-O-alpha-L-rhamn...

journal_title：Chemical & pharmaceutical bulletin

authors： Arao T,Kinjo J,Nohara T,Isobe R

更新日期：1997-02-01 00:00:00

abstract：:The aim of this study was to search for a novel choline acetyltransferase (ChAT) activator from plants traditionally grown in Korea. An ethanol extract from Chaenomeles sinensis Koehne showed the highest ChAT-activating effect in vitro in an assay that used human neuroblastoma cells and [(14)C]acetyl-CoA. The active c...

journal_title：Chemical & pharmaceutical bulletin

authors： Kwon YK,Choi SJ,Kim CR,Kim JK,Kim HK,Choi JH,Song SW,Kim CJ,Park GG,Park CS,Shin DH

更新日期：2015-01-01 00:00:00

abstract：:Based on the result of X-ray crystallographic analysis of our peroxisome proliferator-activated receptor alpha and delta (PPARalpha/delta) co-agonist complexed with human PPAR ligand binding domain (LBD), we designed and synthesized an optically active fluorescent PPARalpha/delta co-agonist, which has a pyrene unit in...

journal_title：Chemical & pharmaceutical bulletin

authors： Araya Y,Kasuga J,Toyota K,Hirakawa Y,Oyama T,Makishima M,Morikawa K,Hashimoto Y,Miyachi H

更新日期：2008-09-01 00:00:00

abstract：:We have engineered a novel, non-viral, multifunctional gene vector (STR-CH(2)R(4)H(2)C) that contained stearoyl (STR) and a block peptide consisting of Cys (C), His (H), and Arg (R). STR-CH(2)R(4)H(2)C can form a stable nano-complex with plasmid DNA (pDNA) based on electronic interactions and disulfide cross linkages....

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka K,Kanazawa T,Ogawa T,Suda Y,Takashima Y,Fukuda T,Okada H

更新日期：2011-01-01 00:00:00

abstract：:Three new quinovic acid glycosides, named gongganosides A (1), B (2), and C (3), were isolated from the bark of Bhesa paniculata (Celastraceae), an Indonesian medicinal plant collected in Sumatra Island. The chemical structures have been elucidated on the basis of chemical and physicochemical evidence as quinovic acid...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohashi K,Kojima H,Tanikawa T,Okumura Y,Kawazoe K,Tatara N,Shibuya H,Kitagawa I

更新日期：1994-08-01 00:00:00

abstract：:The title compound, PNU-97018 [systemic name: 2-butyl-3,6,7,8,9,11-hexahydro-6,9-dimethyl-3-([2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl)-6,9-ethano-4H-imidazo[4,5-d]-pyridazino[1,2-a]pyridazin-4-one] is a newly developed angiotensin II receptor antagonist. The compound and its methanolate and ethanolate were ch...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishii H,Yamaguchi K,Seki H,Sakamoto S,Tozuka Y,Oguchi T,Yamamoto K

更新日期：2002-08-01 00:00:00

abstract：:A rapid tandem mass spectrometric (MS-MS) method for the quantification of Oxcarbazepine (OXB) in human plasma using imipramine as an internal standard (IS) has been developed and validated. Chromatographic separation was achieved isocratically on a C18 reversed-phase column within 3.0 min, using a mobile phase of ace...

journal_title：Chemical & pharmaceutical bulletin

authors： Srinubabu G,Ratnam BV,Rao AA,Rao MN

更新日期：2008-01-01 00:00:00

abstract：:Three cytotoxic cardenolides, acovenosigenin A 3-O-alpha-L-ramnopyranoside (1), euonymoside A (2) and euonymusoside A (3), were isolated from the woods of Euonymus alata (Celastraceae). The chemical structure of a new cardenolide, euonymusoside A (3) has been elucidated on the basis of extensive spectral analysis and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitanaka S,Takido M,Mizoue K,Nakaike S

更新日期：1996-03-01 00:00:00

abstract：:The synthesis of three series of curcumin analogues with mono-carbonyl is described. Their in vitro anti-bacterial activities against seven Gram-positive and Gram-negative bacteria were tested and the effect of substituents on the aryl ring and the space structure of the linking strain were discussed. It was observed ...

journal_title：Chemical & pharmaceutical bulletin

authors： Liang G,Yang S,Jiang L,Zhao Y,Shao L,Xiao J,Ye F,Li Y,Li X

更新日期：2008-02-01 00:00:00

abstract：:Even though β-lapachone is a promising compound with antitumor, antiinflammatory, antineoplastic, and wound-healing effects, there are still issues concerning its chemical stability and degradation mechanisms. The objective of this study was to obtain degradation profiles of β-lapachone and evaluate its chemical stabi...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim KH,Park SH,Adhikary P,Cho JH,Kang NG,Jeong SH

更新日期：2016-01-01 00:00:00

abstract：:Atranorin, lichexanthone, and the (+)-usnic, diffractaic, divaricatic, perlatolic, psoromic, protocetraric, and norstictic acids isolated from the lichens Parmotrema dilatatum (VAIN.) HALE, Usnea subcavata MOTYKA, Usnea sp., Ramalina sp., Cladina confusa (SANT.) FOLMM. & AHTI, Dirinaria aspera HÄSÄNEN, and Parmotrema ...

journal_title：Chemical & pharmaceutical bulletin

authors： Brandão LF,Alcantara GB,Matos Mde F,Bogo D,Freitas Ddos S,Oyama NM,Honda NK

更新日期：2013-01-01 00:00:00

abstract：:Four vitamin D3 analogues (7a, 7b, 7c and 7d) bearing a hydroxyalkoxy group at the 2 beta-position were synthesized from the alpha-epoxide (5). The C-3 analogue (7b) showed the highest potency for elevating plasma calcium levels in rats. Furthermore, the 25-hydroxylated C-3 analogue (ED-71) (3), prepared from the 25-h...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyamoto K,Murayama E,Ochi K,Watanabe H,Kubodera N

更新日期：1993-06-01 00:00:00