Synthesis and anti-HIV-1 activity of new delavirdine analogues carrying arylpyrrole moieties.

Abstract:

:In our search for novel anti-human immunodeficiency virus (HIV)-1 agents, 14 delavirdine analogues were synthesized and evaluated as potential anti-HIV-1 agents in cell-based assays. Compound 1Aa exhibited potent and selective anti-HIV-1 activity in acutely infected MT4 cells, with effective concentration (EC50) values in the submicromolar range.

authors

Pinna GA,Loriga G,Murineddu G,Grella G,Mura M,Vargiu L,Murgioni C,La Colla P

doi

10.1248/cpb.49.1406

subject

Has Abstract

pub_date

2001-11-01 00:00:00

pages

1406-11

issue

11

eissn

0009-2363

issn

1347-5223

journal_volume

49

pub_type

杂志文章
  • Lobenzarit disodium (CCA) inhibits in vitro immunoglobulin production via direct interaction with B lymphocytes.

    abstract::The regulatory effects of lobenzarit disodium (CCA), a therapeutic agent for treating rheumatoid arthritis (RA), on polyclonal immunoglobulin production by human lymphocytes were investigated in vitro. CCA inhibited the production of immunoglobulin in all the classes examined at a clinically relevant concentration. Mo...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.40.177

    authors: Takeda Y,Urakawa K,Sakamoto A,Nakano T,Sugawara Y,Ohsugi Y,Morita M,Kasahara T

    更新日期:1992-01-01 00:00:00

  • Microbial metabolites of harman alkaloids.

    abstract::Several microorganisms showed the ability to transform the harman alkaloids, harmaline (1), harmalol (2) and harman (5). Harmaline (1) and harmalol (2) were converted by Rhodotorula rubra ATCC 20129 into the tryptamines, 2-acetyl-3-(2-acetamidoethyl)-7-methoxyindole (3) and 2-acetyl-3-(2-acetamidoethyl)-7-hydroxyindol...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.51.646

    authors: Herath W,Mikell JR,Ferreira D,Khan IA

    更新日期:2003-06-01 00:00:00

  • Study of Schiff-Base-Derived with Dioxygenated Rings and Nitrogen Heterocycle as Potential β-Ketoacyl-acyl Carrier Protein Synthase III (FabH) Inhibitors.

    abstract::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 syn...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c16-00772

    authors: Zhou Y,Yang YS,Song XD,Lu L,Zhu HL

    更新日期:2017-01-01 00:00:00

  • 2″,4″-O-diacetylquercitrin, a novel advanced glycation end-product formation and aldose reductase inhibitor from Melastoma sanguineum.

    abstract::A new flavonoid, 2,″4″-O-diacetylquercitrin (1), along with six known flavonoids (2-7) were isolated from the aerial parts of Melastoma sanguineum. The structure of the new flavonoid was established by extensive spectroscopic studies and chemical evidence. The inhibitory effects of isolated compounds (1-7) on advanced...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c12-00877

    authors: Lee IS,Kim IS,Lee YM,Lee Y,Kim JH,Kim JS

    更新日期:2013-01-01 00:00:00

  • Preparation and evaluation of solid dispersion of atorvastatin calcium with Soluplus® by spray drying technique.

    abstract::The aim of the present study was to investigate the effect of Soluplus® on the solubility of atorvastatin calcium and to develop a solid dispersion formulation that can improve the oral bioavailability of atorvastatin calcium. We demonstrated that Soluplus® increases the aqueous solubility of atorvastatin calcium. Sev...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c14-00030

    authors: Ha ES,Baek IH,Cho W,Hwang SJ,Kim MS

    更新日期:2014-01-01 00:00:00

  • Megistoquinones I and II, two quinoline alkaloids with antibacterial activity from the bark of Sarcomelicope megistophylla.

    abstract::Two alkaloids, megistoquinone I (1) and megistoquinone II (2), were isolated from the bark of Sarcomelicope megistophylla. Their structures have been elucidated on the basis of MS and NMR data. Both belong to quinoline alkaloid series and should be considered as oxidation products of a furo[2,3-b]quinoline precursor. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.50.413

    authors: Fokialakis N,Magiatis P,Chinou I,Mitaku S,Tillequin F

    更新日期:2002-03-01 00:00:00

  • Three new limonoids from Cipadessa cinerascens.

    abstract::Three new limonoids, cipadesins D--F (1--3), together with 8,15-dihydroxy-13E-labdane, beta-sitosterol and beta-daucosterol, were isolated from the leaves and bark of Cipadessa cinerascens. Their structures were elucidated by spectral evidence. X-Ray crystallographic analysis confirmed the structure of 1. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.55.902

    authors: Yuan XH,Li BG,Xu CX,Zhou M,Qi HY,Zhang GL

    更新日期:2007-06-01 00:00:00

  • New green synthesis and formulations of acyclovir prodrugs.

    abstract::Different green synthesis of alkyl esters of acyclovir (acyclovir prodrugs) is described. Hexanoic, decanoic, dodecanoic and tetradecanoic acyclovir esters were synthesized reacting acyclovir and the respective acid anhydride in dimethyl sulfoxide (DMSO), in solvents from renewable sources and without solvent (T=30 °C...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.59.1089

    authors: de Regil-Hernández R,Martínez-Lagos F,Rodríguez-Bayón A,Sinisterra JV

    更新日期:2011-01-01 00:00:00

  • Synthesis and SAR Study of the Novel Thiadiazole-Imidazole Derivatives as a New Anticancer Agents.

    abstract::In the present study, a novel series of 2-(2-(3-aryl-5-substituted-1,3,4-thiadiazol-2(3H)-ylidene)hydrazinyl)-4,4-diphenyl-1H-imidazol-5(4H)-one derivatives were designed and prepared via the reaction of the most versatile, hitherto unreported 2-(5-oxo-4,4-diphenyl-4,5-dihydro-1H-imidazol-2-yl)-N-phenylhydrazinecarbot...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c16-00344

    authors: Gomha SM,Abdel-Aziz HM,Khalil KD

    更新日期:2016-01-01 00:00:00

  • Stereoselective oxidation at C-4 of flavans by the endophytic fungus Diaporthe sp. isolated from a tea plant.

    abstract::The microbial transformation of five flavans (1-5) by endophytic fungi isolated from the tea plant Camellia sinensis was investigated. It was found that the endophytic filamentous fungus Diaporthe sp. oxidized stereoselectively at C-4 position of (+)-catechin (1) and (-)-epicatechin (2) to give the correspondent 3,4-c...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.53.1565

    authors: Agusta A,Maehara S,Ohashi K,Simanjuntak P,Shibuya H

    更新日期:2005-12-01 00:00:00

  • Cytotoxic activity and DNA-binding properties of isoeuxanthone derivatives.

    abstract::In this study, the interactions of different groups substituted isoeuxanthone derivatives with calf thymus DNA (ct DNA) were investigated by spectrophotometric methods and viscosity measurements. Results indicated that the xanthone derivatives could intercalate into the DNA base pairs by the plane of xanthone ring and...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c13-00789

    authors: Wang HF,Yan H,Gao X,Niu B,Guo R,Wei L,Xu B,Tang N

    更新日期:2014-01-01 00:00:00

  • Progress in Development of Interventions to Prevent Birth Defects in Diabetic Pregnancies.

    abstract::Diabetic embryopathy is a diabetic complication, in which maternal hyperglycemia in early pregnancy causes birth defects in newborn infants. Under maternal diabetic conditions, hyperglycemia disturbs intracellular molecular activities and organelles functions. These include protein misfolding in the endoplasmic reticu...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章,评审

    doi:10.1248/cpb.c18-01013

    authors: Han L,Jiang Z,Zheng X,Qiu J,Hu Y,Li X

    更新日期:2019-01-01 00:00:00

  • Oplopanphesides A-C, three new phenolic glycosides from the root barks of Oplopanax horridus.

    abstract::Three new phenolic glycosides, named oplopanphesides A-C (1-3), have been isolated from the root barks of Oplopanax horridus. Their structures were elucidated by a combination of spectroscopic analyses, including 1D- and 2D-NMR techniques. These phenolic glycosides possess a novel feature in their sugar moieties that ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.59.676

    authors: Huang WH,Zhang QW,Meng LZ,Yuan CS,Wang CZ,Li SP

    更新日期:2011-01-01 00:00:00

  • Synthesis of cis-bicyclo[4.3.0]non-2-ene derivatives. The potent homoisocarbacyclin analogs.

    abstract::Synthesis of homoisocarbacyclin has been achieved efficiently by a general strategy with stereo- and regiochemical control. One of homoisocarbacyclin derivatives, 3-oxa homoisocarbacyclin analog (4), was shown to be potently active in inhibiting gastric ulcer. Another analog, conjugated diene derivative (5), was found...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.37.1647

    authors: Shibasaki M,Takahashi A,Aoki T,Sato H,Narita S

    更新日期:1989-06-01 00:00:00

  • Synthesis and evaluation of novel 2-oxo-1,2-dihydro-3-quinolinecarboxamide derivatives as serotonin 5-HT4 receptor agonists.

    abstract::A series of N-azabicycloalkyl-1-alkyl-2-oxo-1,2-dihydro-3-quinolinecarboxamides were synthesized and tested for serotonin 5-HT4 receptor-stimulating effects in the regulation of electrically-evoked contraction in guinea pig muscle. Among them, N-azabicycloalkyl-1-isopropyl-2-oxo-1,2-dihydro-3-quinolinecarboxamide (8c,...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.48.2003

    authors: Suzuki M,Ohuchi Y,Asanuma H,Kaneko T,Yokomori S,Ito C,Isobe Y,Muramatsu M

    更新日期:2000-12-01 00:00:00

  • Light irradiation is a factor in the bactericidal activity of silver-loaded zeolite.

    abstract::Silver loaded zeolite (Ag-Z) was previously found to have effective bactericidal activity against Escherichia coli. To understand the mechanisms of bactericidal activity of Ag-Z, role of light irradiation was focused and investigated in this study. In this study, we focused on light irradiation. Antibacterial assay an...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.56.692

    authors: Inoue Y,Kogure M,Matsumoto K,Hamashima H,Tsukada M,Endo K,Tanaka T

    更新日期:2008-05-01 00:00:00

  • CTRP12 Ameliorated Lipopolysaccharide-Induced Cardiomyocyte Injury.

    abstract::C1q/tumor necrosis factor (TNF)-related protein 12 (CTRP12) is a secretory protein that participates in the regulation of glucose and lipid metabolism in obesity and diabetes. Its role in cardiovascular disease, particularly sepsis-induced cardiac injury, is unclear. Here, we stimulated cardiomyocytes with lipopolysac...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c19-00646

    authors: Zhou MQ,Jin E,Wu J,Ren F,Yang YZ,Duan DD

    更新日期:2020-01-01 00:00:00

  • Oleanene-type triterpene glycosides from puerariae radix. IV. Six new saponins from Pueraria lobata.

    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

    pub_type: 杂志文章

    doi:10.1248/cpb.45.362

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

    更新日期:1997-02-01 00:00:00

  • Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. V. Thienopyridazinone derivatives.

    abstract::Synthesis and pharmacological evaluation of novel thienopyridazinones and related compounds are described. A thiophene ring was found to be able to replace the benzene ring of a phthalazinone without loss of biological activities. This observation supports our hypothesis that the benzene ring plays an important role i...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.43.236

    authors: Yamaguchi M,Maruyama N,Koga T,Kamei K,Akima M,Kuroki T,Hamana M,Ohi N

    更新日期:1995-02-01 00:00:00

  • Relationship between effects of phenolic compounds on the generation of free radicals from lactoperoxidase-catalyzed oxidation of NAD(P)H or GSH and their DPPH scavenging ability.

    abstract::The influence of various phenolic compounds on the lactoperoxidase (LPO)/hydrogen peroxide (H2O2)-catalyzed oxidation of biochemical reductants such as reduced beta-nicotinamide adenine dinucleotide (NADH), reduced beta-nicotinamide adenine dinucleotide phosphate (NADPH) or reduced glutathione (GSH) was investigated b...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.49.299

    authors: Ueda J,Tsuchiya Y,Ozawa T

    更新日期:2001-03-01 00:00:00

  • Synthesis and testosterone 5 alpha-reductase-inhibitory activity of 4-aza-5 alpha-androstane-17-carboxamide compound with an aromatic moiety in the C-17 carbamoyl group.

    abstract::A series of 4-aza-5 alpha-androstane compounds with one or two aromatic moieties in the carbamoyl group at the C-17 position were synthesized and their inhibitory activities for rat and human prostatic testosterone 5 alpha-reductase were tested in vitro. Compounds with one aromatic moiety in the carbamoyl group showed...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.44.115

    authors: Kurata H,Ishibashi K,Saito S,Hamada T,Horikoshi H,Furukawa Y,Kojima K

    更新日期:1996-01-01 00:00:00

  • Phenylpropanoids from Umbilicus pendulinus.

    abstract::Phytochemical investigation of the leaves of Umbilicus pendulinus afforded in addition to 2-O-caffeoyl malate, isoquercitrin and Z-venusol, the new isomer E-venusol. Special NMR experiments were carried out to elucidate the configuration of the two latter compounds. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.48.1768

    authors: Viornery L,Saliba C,Daskiewicz JB,Bayet C,Comte G,Fenet B,Gutierrez G,Barron D

    更新日期:2000-11-01 00:00:00

  • Three New Polyphenolic Acids from the Leaves of Eucalyptus citriodora with Antivirus Activity.

    abstract::Six polyphenolic acids (1-6), including the three new compounds citriodolic acids A, B, and C (1-3), were isolated from the leaves of Eucalyptus citriodora. Their structures were elucidated by spectroscopic methods including one dimensional (1D)- and 2D-NMR, high-resolution electrospray ionization (HR-ESI)-MS, and cir...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c16-00362

    authors: Lin SQ,Zhou ZL,Yin WQ

    更新日期:2016-11-01 00:00:00

  • Pharmacokinetics in chimpanzees of recombinant human tissue-type plasminogen activator produced in mouse C127 and Chinese hamster ovary cells.

    abstract::Pharmacokinetics of recombinant tissue-type plasminogen activator (rt-PA) produced in mouse C127 cells (t-PA(C127] and Chinese hamster ovary cells (t-PA(CHO] was investigated in chimpanzees. rt-PA was administered via a constant rate i.v. infusion for 60 min, and t-PA concentration and activity in plasma were measured...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.38.517

    authors: Tanigawara Y,Hori R,Okumura K,Tsuji J,Shimizu N,Noma S,Suzuki J,Livingston DJ,Richards SM,Keyes LD

    更新日期:1990-02-01 00:00:00

  • Saponin and sapogenol. L. On the constituents of the roots of Glycyrrhiza uralensis Fischer from Xinjiang, China. Chemical structures of licorice-saponin L3 and isoliquiritin apioside.

    abstract::From the air-dried roots of Glycyrrhiza uralensis Fischer collected in Xinjiang province, China ("Shinkyo-Kanzo" in Japanese), a new oleanene-type triterpene oligoglycoside named licorice-saponin L3 and a new chalcone oligoglycoside named isoliquiritin apioside were isolated together with glycyrrhizin, 18 alpha-glycyr...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.41.1567

    authors: Kitagawa I,Hori K,Uchida E,Chen WZ,Yoshikawa M,Ren J

    更新日期:1993-09-01 00:00:00

  • Isolation and identification of anti-tumor-promoting principles from the fresh-water cyanobacterium Phormidium tenue.

    abstract::Bioassay-directed fractionation of the extract of the cyanobacterium P. tenue led to the isolation of the three classes of glycolipids, viz., monogalactosyl diacylglycerol (MGDG), digalactosyl diacylglycerol (DGDG), and sulfoquinovosyl diacylglycerol (SQDG) as anti-tumor-promoters. In comparing the anti-tumor-promotin...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.41.1664

    authors: Shirahashi H,Murakami N,Watanabe M,Nagatsu A,Sakakibara J,Tokuda H,Nishino H,Iwashima A

    更新日期:1993-09-01 00:00:00

  • Syntheses and Biological Evaluation of Novel Hydroxamic Acid Derivatives Containing Purine Moiety as Histone Deacetylase Inhibitors.

    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

    pub_type: 杂志文章

    doi:10.1248/cpb.c17-00997

    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

  • Cytotoxic cardenolides from woods of Euonymus alata.

    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

    pub_type: 杂志文章

    doi:10.1248/cpb.44.615

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

    更新日期:1996-03-01 00:00:00

  • New iridoids from Gelsemium species.

    abstract::Four new iridoids structurally related to gelsemide (5) were isolated from two Loganiaceous plants, Gelsemium elegans and G. rankinii. Among them, GEIR-1 (1) has a novel tetracyclic caged structure. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.56.870

    authors: Kogure N,Ishii N,Kobayashi H,Kitajima M,Wongseripipatana S,Takayama H

    更新日期:2008-06-01 00:00:00

  • Naturally occurring 5-lipoxygenase inhibitor. II. Structures and syntheses of ardisianones A and B, and maesanin, alkenyl-1,4-benzoquinones from the rhizome of Ardisia japonica.

    abstract::New alkenyl-1,4-benzoquinones, ardisianones A (1) and B (2), and the known maesanin (3) as 5-lipoxygenase inhibitors have been isolated from the rhizome of Ardisia japonica. Their structures have been elucidated as 2-methoxy-6-[(Z)-10'-pentadecenyl]-1,4-benzoquinone and 5-hydroxy-2-methoxy-6-[(Z)-8'-tridecenyl]-1,4-be...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.41.561

    authors: Fukuyama Y,Kiriyama Y,Okino J,Kodama M,Iwaki H,Hosozawa S,Matsui K

    更新日期:1993-03-01 00:00:00