Synthesis and antinociceptive activity of orally active opioid peptides: improvement of oral bioavailability by esterification.

abstract：:A series of 5-(4-aryl- or 4-arylcarbonylpiperazin-1-yl)-5-deoxy-1,4: 3,6-dianhydro-L-iditol 2-nitrates was prepared in order to obtain orally active, nitrate-type vasodilators with reduced side effects. Our drug design was based on a small reduction in the lipophilicity compared to that of 5-deoxy-5-[4-(3-phenylthiopr...

journal_title：Chemical & pharmaceutical bulletin

authors： Hayashi H,Ikeda J,Kubo K,Moriyama T,Karasawa A,Suzuki F

更新日期：1993-06-01 00:00:00

abstract：:The constituents of the MeOH extract of Salvia miltiorhiza BUNGE, which showed strong aldose reductase (AR) inhibitory activity, were examined, and two new abietane-type diterpenoids, danshenol A (1) and danshenol B (2), were isolated together with six known ones: dihydrotanshimme I (3), cryptotanshinone (4), tanshino...

journal_title：Chemical & pharmaceutical bulletin

authors： Tezuka Y,Kasimu R,Basnet P,Namba T,Kadota S

更新日期：1997-08-01 00:00:00

abstract：:A series of N-substituted 3,4-diphenyl-1H-pyrrole-2,5-diones (diphenylmaleimides) (IV) were synthesized and tested for cytostatic activity. Compounds IVa--k were prepared from diphenylmaleic anhydride or its dinitro derivative (V or VI) and the corresponding amine. Compounds IVl--n were obtained by reaction of 3-(p-ni...

journal_title：Chemical & pharmaceutical bulletin

authors： Fernández Braña M,Fernández A,Garrido M,López Rodríguez ML,Morcillo MJ,Sanz AM

更新日期：1989-10-01 00:00:00

abstract：:As part of our search for active agents against systemic fungal infections, a new series of triazole compounds with a thiolane ring was synthesized. Their antifungal activities were investigated in vitro and in vivo. Some of these thiolanetriazoles showed promising activity, comparable to that of ketoconazole, against...

journal_title：Chemical & pharmaceutical bulletin

authors： Konosu T,Takeda N,Tajima Y,Yasuda H,Oida S

更新日期：1990-05-01 00:00:00

abstract：: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 target...

journal_title：Chemical & pharmaceutical bulletin

authors： Park H,Yu Y,Kim H,Lee E,Lee H,Jeon R,Kim WY

更新日期：2017-04-01 00:00:00

abstract：:A chemical investigation of Jaspis sp., the marine sponge collected from the South China Sea led to the isolation of six new isomalabaricane-type compounds, jaspolides A-F (1-6). The structures of those compounds were elucidated by extensive spectroscopic methods. The structure-types of 1 to 6 could be classified into...

journal_title：Chemical & pharmaceutical bulletin

authors： Tang S,Pei Y,Fu H,Deng Z,Li J,Proksch P,Lin W

更新日期：2006-01-01 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：:Adipocyte fatty acid binding protein (A-FABP; FABP4), which is predominantly expressed in macrophages and adipose tissue, regulates fatty acid storage and lipolysis, and is also an important mediator of inflammation. Here, we report a synthesis of (14)C-labeled 2-[2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)biphenyl-3-yl...

journal_title：Chemical & pharmaceutical bulletin

authors： Okada T,Hiromura M,Otsuka M,Enomoto S,Miyachi H

更新日期：2012-01-01 00:00:00

abstract：:As part of the search for new topical antiinflammatory agents, various 21-substituted corticosteroids having sulfur-containing moieties were prepared and tested for vasoconstrictive activity in humans. A structure-activity relationship study revealed that substitution of the 21-hydroxy group with a lower alkyl-thio gr...

journal_title：Chemical & pharmaceutical bulletin

authors： Mitsukuchi M,Ikemoto T,Taguchi M,Higuchi S,Abe S,Yasui H,Hatayama K,Sota K

更新日期：1989-07-01 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：:Enantiomerically pure (1S,3S)- and (1S,3R)-1-amino-3-(hydroxymethyl)cyclopentanes have been efficiently synthesized from L-aspartic acid. The title compounds are isosteres of ribose and may be used to construct nucleoside analogs with important antiviral and antineoplastic activities as demonstrated by a concise total...

journal_title：Chemical & pharmaceutical bulletin

authors： Rapoport H,Chen Y,Mohareb RM,Ahn JH,Sim TB,Ho JZ

更新日期：2003-10-01 00:00:00

abstract：:From the seeds of Pharbitis nil (Convolvulaceae), two new oleanene-type triterpene glycosides, pharbitosides A (1) and B (2), together with beta-sitosterol, beta-sitosterol glucoside (daucosterol), caffeic acid, and methyl caffeate were isolated. The structure of pharbitoside A (1) was elucidated to be queretaroic aci...

journal_title：Chemical & pharmaceutical bulletin

authors： Jung DY,Ha H,Lee HY,Kim C,Lee JH,Bae K,Kim JS,Kang SS

更新日期：2008-02-01 00:00:00

abstract：:Alkylidenemalonates were readily dimerized in the presence of SmI2 to give 2,3-disubstituted 1,1,4,4-butanetetracarboxylates as mixtures of meso and racemic isomers in moderate to good yields. The structure of the less polar isomer of tetraethyl 2,3-diphenyl-1,1,4,4-butanetetracarboxylate was determined by X-ray cryst...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamashita M,Okuyama K,Kawasaki I,Nakamura S,Nagamine R,Tsujita T,Ohta S

更新日期：2000-11-01 00:00:00

abstract：:A new method has been developed for the umpolung α-heteroarylation of ketones via an N-alkoxyenamine. The treatment of ketones with tris(heteroaryl)aluminum reagents in the presence of isoxazolidine gave the corresponding α-heteroarylated ketones in moderate to good yields. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyoshi T,Takeda N,Fukami M,Sato S,Ueda M,Miyata O

更新日期：2014-01-01 00:00:00

abstract：:Solifenacin (Sol), an antimuscarinic agent has been widely used for the treatment of overactive bladder. Transdermal formulations can be administered without water as well as absorbed slowly into the blood over a long period of time. The aim of this study was to develop cream and tape formulations of Sol, and evaluate...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida M,Uchida S,Kashiwagura Y,Tanaka S,Matsui R,Namiki N

更新日期：2019-01-01 00:00:00

abstract：:ZnAB has the combined structure of N,N-bis(2-pyridylmethyl)ethylenediamine as a specific chelater for Zn(2+) and 1,3,5,7-tetramethyl-8-phenyl-boron dipyrromethene as a fluorophore. Complexation of ZnAB with Zn(2+) produces a remarkable enhancement of fluorescence intensity. ZnAB has the advantages of less sensitivity ...

journal_title：Chemical & pharmaceutical bulletin

authors： Koutaka H,Kosuge J,Fukasaku N,Hirano T,Kikuchi K,Urano Y,Kojima H,Nagano T

更新日期：2004-06-01 00:00:00

abstract：:The molecular geometry, acid dissociation constants and partition coefficients of the anilinoquinoline (I), indolo[3,2-c]quinoline (II) and tetrahydroindolo[3,2-d] [1]benzazepine (III) ring systems have been determined using representative compounds: 7-chloro-4-(p-anisidino)quinoline (Ia), 3-chloro-8-methoxy-11H-indol...

journal_title：Chemical & pharmaceutical bulletin

authors： Koh HL,Go ML,Ngiam TL

更新日期：1994-05-01 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：:This study examined the intestinal transport of five harman alkaloids using the Caco-2 cell monolayer as a model of the human intestinal mucosa. Transport parameters, permeability coefficients and percent transports, were calculated and compared under identical conditions with atenolol. Permeability coefficients were ...

journal_title：Chemical & pharmaceutical bulletin

authors： Khan SI,Abourashed EA,Khan IA,Walker LA

更新日期：2004-04-01 00:00:00

abstract：:A rapid, sensitive, and specific analytical method for the determination of 1-hydroxyethylidene-1,1-diphosphonic acid (HEDP) on uncooked foods after treatment with a peracetic acid-based sanitizer (PAS) was developed. The method involves simple sample preparation steps and analysis using ion chromatography (IC) couple...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki I,Kubota H,Ohtsuki T,Tatebe C,Tada A,Yano T,Akiyama H,Sato K

更新日期：2016-01-01 00:00:00

abstract：:Novel cyclic sulfoxides, such as 2-octyl, 2-dodecyl and 2-hexadecyltetrahydrothiophene-1-oxide were prepared by the alkylation of tetrahydrothiophene-1-oxide. Additionally, 2-methyl, 2-ethyl and 2-propyl-5-dodecyltetrahydro-thiophene-1-oxide were conducted by further alkylation. Their enhancing activity on the penetra...

journal_title：Chemical & pharmaceutical bulletin

authors： Aoyagi T,Yamamura M,Matsui K,Nagase Y

更新日期：1992-07-01 00:00:00

abstract：:Mutant activin receptor-like kinase-2 (ALK2) was reported to be closely associated with the pathogenesis of fibrodysplasia ossificans progressiva (FOP) and diffuse intrinsic pontine glioma (DIPG), and therefore presents an attractive target for therapeutic intervention. Through in silico virtual screenings and structu...

journal_title：Chemical & pharmaceutical bulletin

authors： Sekimata K,Sato T,Sakai N,Watanabe H,Mishima-Tsumagari C,Taguri T,Matsumoto T,Fujii Y,Handa N,Honma T,Tanaka A,Shirouzu M,Yokoyama S,Miyazono K,Hashizume Y,Koyama H

更新日期：2019-01-01 00:00:00

abstract：:Indoloquinoline alkaloid cryptolepine and pyridocarbazole alkaloid ellipticine are of great interest because in vitro and in vivo studies revealed their good cytotoxic properties. In order to obtain some biologically active analogs of these compounds, we developed a synthesis based on the photocyclization of tertiary ...

journal_title：Chemical & pharmaceutical bulletin

authors： Aragon PJ,Yapi AD,Pinguet F,Chezal JM,Teulade JC,Blache Y

更新日期：2007-09-01 00:00:00

abstract：:Four new bicyclic hexapeptides, named as RA-XI, -XII, XIII and -XIV were isolated from Rubia cordifolia and showed potent antitumor activities against P-388. The structures were elucidated from spectroscopic and chemical evidences. RA-XII, XIII and -XIV were proved to be unique bicyclic hexapeptidic glucosides. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Morita H,Yamamiya T,Takeya K,Itokawa H

更新日期：1992-05-01 00:00:00

abstract：:N-(2-Dimethylaminoethyl)carboxamide (1a-d), 2-dimethylaminoethyl alkyl ether (2a, b), and 2-dimethylaminoethyl 2-hydroxy-2-phenethyl ether (3a-c) and its amino and methylene analogues (3d, 4) have been screened for antiamnestic and antihypoxic activities in mice. A clear reversing effect on electroconvulsive shock-ind...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono S,Yamafuji T,Chaki H,Todo Y,Maekawa M,Kitamura K,Tai M,Narita H

更新日期：1995-09-01 00:00:00

abstract：:The percutaneous (p.c.) absorption of clonazepam (CZP), an antiepileptic drug, was investigated in rabbits. CZP was efficiently absorbed from a gel ointment (0.5% CZP, 1g, 9 cm2) with Azone and therapeutic plasma concentrations were maintained for 27 h. The bioavailability of CZP from the gel ointment was 47.2 +/- 3.1...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogiso T,Ito Y,Iwaki M,Yamamoto Y

更新日期：1989-02-01 00:00:00

abstract：:Epidermal cells from newborn rat skin were cultured on type IV collagen-coated Millipore filter, and the transport of low density lipoprotein (LDL) labeled with Rhodamine B isothiocyanate (RB-LDL) through the cultured cell layer was examined. The transport of RB-LDL was dependent on temperature and biological energy. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohkura K,Terada H

更新日期：1991-02-01 00:00:00

abstract：:The methanolic extracts from the wood and bark of Cotylelobium melanoxylon were found to inhibit plasma glucose elevation after sucrose loading in rats and triglyceride elevation after olive oil loading in mice. A new stilbene dimer, melanoxylin A, together with the known stilbene dimers [(+)-ampelopsin F, (+)-isoampe...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuda H,Asao Y,Nakamura S,Hamao M,Sugimoto S,Hongo M,Pongpiriyadacha Y,Yoshikawa M

更新日期：2009-05-01 00:00:00

abstract：:A major lysosomal membrane glycoprotein (LGP107) which has an apparent molecular weight (Mr) of 107 kilodaltons (kDa) was purified from rat liver by a simple method with a yield of 1 mg/87 g wet weight of liver. The purification procedures include; preparation of tritosomal membranes of triton-filled lysosomes (tritos...

journal_title：Chemical & pharmaceutical bulletin

authors： Akasaki K,Yamaguchi Y,Ohta M,Matsuura F,Furuno K,Tsuji H

更新日期：1990-10-01 00:00:00

abstract：:Anti-tauro 1 beta-hydroxycholic acid antisera were prepared by immunizing rabbits with N-(1 beta,3 alpha, 7 alpha, 12 alpha-tetrahydroxy-5 beta-cholan-24-oyl)-2- aminopropionic acid-bovine serum albumin (BSA) conjugate. The antisera raised had high affinity (1.25-1.46 x 10(9) M-1) and specificity for conjugated 1 beta...

journal_title：Chemical & pharmaceutical bulletin

authors： Ikegawa S,Murai T,Yoshimura T,Tohma M

更新日期：1992-07-01 00:00:00