Synthesis and Evaluation of 5-(o-Tolyl)-1H-tetrazole Derivatives as Potent Anticonvulsant Agents.

abstract：:A general procedure for the preparation of 1,2,3-triazole analogs of nucleosides from diethyl 2-azidoethoxymethyl- and 2-azidoethoxyethylphosphonates was elaborated. The application of microwave irradiation shortened the reaction time to 10 min in comparison to ca. 48 h when 1,3-dipolar cycloadditions were performed u...

journal_title：Archiv der Pharmazie

authors： Głowacka IE,Balzarini J,Wróblewski AE

更新日期：2013-04-01 00:00:00

abstract：:A number of 7-piperazinylquinolones carrying a functionalized 2-(furan-3-yl)ethyl moiety attached to the piperazine ring have been synthesized and evaluated as antibacterial agents against a panel of Gram-positive and Gram-negative bacteria. Most of the synthesized compounds exhibited significant antibacterial activit...

journal_title：Archiv der Pharmazie

authors： Foroumadi A,Mohammadhosseini N,Emami S,Letafat B,Faramarzi MA,Samadi N,Shafiee A

更新日期：2007-01-01 00:00:00

abstract：:A series of 6-chloro-3-(4-alkylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones, 7-chloro-3-(4-alkylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones, 6-bromo-3-(4-alkylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones, 6,8-dibromo-3-(4-alkylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones, 6-chloro-3-(4-alkylphenyl)-2H-1,3-ben...

journal_title：Archiv der Pharmazie

authors： Waisser K,Matyk J,Kunes J,Dolezal R,Kaustová J,Dahse HM

更新日期：2008-12-01 00:00:00

abstract：:The stereoisomers of amidinomycin 7 and their intermediates 1-6, which are produced from homochiral 3-oxocyclopentanecarboxylic acids by asymmetric synthesis, are tested for their antimicrobial effects by agar diffusion test and by Bouillon serial dilution assay. Their antibiotic activities against Bacillus subtilis, ...

journal_title：Archiv der Pharmazie

authors： Sung SY,Kist M,Frahm AW

更新日期：1997-01-01 00:00:00

abstract：:A new series of 1,4-disubstituted phthalazinylpiperazine derivatives 7a-f, 12a-f and 20a-f were designed and synthesized in order to develop potent and selective antitumor agents. The target compounds were screened for their cytotoxic activities against A549, HT-29 and MDA-MB-231 cancer cell lines in vitro. Among them...

journal_title：Archiv der Pharmazie

authors： Liu Y,Zhang S,Li Y,Wang J,Song Y,Gong P

更新日期：2012-04-01 00:00:00

abstract：:Several chloro- and iodo-lignanolides have been obtained by direct halogenation of aromatic rings from yatein and 4'-O-demethylyatein. They were assayed as antineoplastics, in order to check the influence in the activity of substitution in both aromatic rings. Although these compounds show a modest antineoplastic acti...

journal_title：Archiv der Pharmazie

authors： Medarde M,Peláez-Lamamié de Clairac R,López JL,Grávalos DG,San Feliciano S

更新日期：1995-09-01 00:00:00

abstract：:A new series of 16 6-chloro-1,1-dioxo-7-{4-[(4-R(1)-phenyl)imino]-4H-3,1-benzoxazin-2-yl}-3-(substituted amino)-1,4,2-benzodithiazines 7-22 was prepared in order to evaluate the cytotoxic activity against six human cancer cell lines. The structures of the new compounds were confirmed by IR, (1)H-, and (13)C-NMR, eleme...

journal_title：Archiv der Pharmazie

authors： Pomarnacka E,Kornicka A,Kuchnio A,Heinrichs M,Grünert R,Gdaniec M,Bednarski PJ

更新日期：2011-07-01 00:00:00

abstract：:Non-steroidal anti-inflammatory drugs (NSAIDs), which are widely used for the treatment of rheumatic arthritis, pain, and many different types of inflammatory disorders, cause serious gastrointestinal (GI) side effects. The free carboxylic acid group existing on their chemical structure is correlated with GI toxicity ...

journal_title：Archiv der Pharmazie

authors： Koksal M,Ozkan-Dagliyan I,Ozyazici T,Kadioglu B,Sipahi H,Bozkurt A,Bilge SS

更新日期：2017-09-01 00:00:00

abstract：:A range of 11 derivatives of flavone-8-acetic acid (FAA) in which the structure has been substantially altered in different ways have been prepared and their anti-tumour activity evaluated in vitro against a panel of human and murine tumour cell lines and in vivo against MAC 15A. The generally poor activity observed s...

journal_title：Archiv der Pharmazie

authors： Aitken RA,Bibby MC,Cooper PA,Double JA,Laws AL,Ritchie RB,Wilson DW

更新日期：2000-06-01 00:00:00

abstract：:Alzheimer's disease (AD) is the most common type of dementia and related to the degeneration of hippocampal cholinergic neurons, which dramatically affects cognitive ability. Acetylcholinesterase (AChE) inhibitors are employed as drugs for AD therapy. Three series of sulfonylhydrazone compounds were designed, and thei...

journal_title：Archiv der Pharmazie

authors： Fernandes TB,Cunha MR,Sakata RP,Candido TM,Baby AR,Tavares MT,Barbosa EG,Almeida WP,Parise-Filho R

更新日期：2017-11-01 00:00:00

abstract：:A new series of pyrazole, phenylpyrazole, and pyrazoline analogs of diarylpentanoids (excluding compounds 3a, 4a, 5a, and 5b) was pan-assay interference compounds-filtered and synthesized via the reaction of diarylpentanoids with hydrazine monohydrate and phenylhydrazine. Each analog was evaluated for its anti-inflamm...

journal_title：Archiv der Pharmazie

authors： Mohd Faudzi SM,Leong SW,Auwal FA,Abas F,Wai LK,Ahmad S,Tham CL,Shaari K,Lajis NH,Yamin BM

更新日期：2021-01-01 00:00:00

abstract：:Although a few experimental approaches to isolated limb perfusion (ILP) are described in the literature, none of these animal models mimics the clinical perfusion techniques adequately to improve the technique of ILP on the basis of valid preclinical data. Therefore, we developed an ILP setup in rats allowing online m...

journal_title：Archiv der Pharmazie

authors： Gürtler U,Fuchs P,Stangelmayer A,Bernhardt G,Buschauer A,Spruss T

更新日期：2004-12-01 00:00:00

abstract：:Synthesis of 2-chloro-1,1-dimethylethyl and 2-chloro-2,2-dimethylethyl analogues of ifosfamide was performed via aziridine intermediate. In vitro metabolic activation showed that both compounds are metabolised at a rate similar to the parent drug. However, their anticancer activity against L1210 leukaemia in mice was ...

journal_title：Archiv der Pharmazie

authors： Misiura K,Kardacka K,Kusnierczyk H

更新日期：2001-09-01 00:00:00

abstract：:Marine organisms play an important role in natural product-based drug research due to accumulation of structurally unique and bioactive metabolites. The exploration of marine-derived compounds may significantly extend the scientific knowledge of potential scaffolds for antibiotic drug discovery. Development of novel a...

journal_title：Archiv der Pharmazie

authors： Daletos G,Ancheeva E,Chaidir C,Kalscheuer R,Proksch P

更新日期：2016-10-01 00:00:00

abstract：:A series of new positive inotropic agents was synthesized with the aim of combining the pharmacophores of the imidazolone-type phosphodiesterase (PDE) inhibitor enoximone and guanidine-type histamine H2 receptor agonists such as arpromidine. All compounds are para-substituted 4-benzoyl-5-alkyl-2-imidazolones. H2 agoni...

journal_title：Archiv der Pharmazie

authors： Glass D,Buschauer A,Tenor H,Bartel S,Will-Shahab L,Krause EG

更新日期：1995-10-01 00:00:00

abstract：:The diffusion of a series of non steroidal antiinflammatory drugs through a silicone rubber membrane has been studied from suspensions both of the free and beta-cyclodextrin complexes forms at different pH values of the medium. Higher diffusion rates of the complexed forms as compared with the free ones and a rate-lim...

journal_title：Archiv der Pharmazie

authors： Orienti I,Cavallari C,Zecchi V,Fini A

更新日期：1989-04-01 00:00:00

abstract：:New condensed derivatives of anpirtoline, in which the pyridine ring is replaced with quinoline, isoquinoline, quinazoline, and phthalazine nuclei, have been synthesized. Their receptor binding profiles (5-HT1A, 5-HT1B) and analgesic activity (hot plate, acetic acid induced writhing) have been studied. The analgesic a...

journal_title：Archiv der Pharmazie

authors： Rádl S,Kovárová L,Hezky P,Vosátka V,Königová O,Proska J,Krejcí I

更新日期：1999-06-01 00:00:00

abstract：:3-Amino-1,4-benzodiazepines as well as chemically related diverse amines were prepared from oxazepam and subsequently screened on the cholecystokinin receptor in a radiolabel binding assay. Oxazepam 2 was activated via its 3-chloro-1,4-benzodiazepine intermediate 3 and was reacted with a large series of aliphatic and ...

journal_title：Archiv der Pharmazie

authors： Offel M,Lattmann P,Singh H,Billington DC,Bunprakob Y,Sattayasai J,Lattmann E

更新日期：2006-04-01 00:00:00

abstract：:Sixteen new 1-(2-methoxyphenyl)-4-(1-phenethylpiperidin-4-yl)piperazines and 1-(2-methoxyphenyl)-4-[(1-phenethylpiperidin-4-yl)methyl]piperazines were synthesized to be used as probes for mapping the dopamine D2 receptor (D2 DAR) arylpiperazine binding site. All compounds were evaluated for their affinity toward D2 DA...

journal_title：Archiv der Pharmazie

authors： Penjišević JZ,Šukalović VV,Andrić DB,Roglić GM,Šoškić V,Kostić-Rajačić SV

更新日期：2016-08-01 00:00:00

abstract：:Biphalin [(Tyr-D-Ala-Gly-Phe-NH-)2 ] is an octapeptide with mixed μ/δ opioid activity. Its structure is based on two identical enkephalin-like portions linked "tail-to-tail" by a hydrazine bridge. This study presents the synthesis and in vitro and in vivo bioassays of two biphalin analogs that do not present the toxic...

journal_title：Archiv der Pharmazie

authors： Costante R,Pinnen F,Stefanucci A,Mollica A

更新日期：2014-05-01 00:00:00

abstract：:The synthesis and the pharmacological properties of some new prazosin analogues are described. ...

journal_title：Archiv der Pharmazie

authors： Rampa A,Valenti P,Da Re P,Carrara M,Zampiron S,Cima L,Giusti P

更新日期：1989-06-01 00:00:00

abstract：:Series of N-(4-substitutedphenyl)-4-(1-methyl (or 1,2-dimethyl)-4-oxo-1,2-dihydroquinazolin-3(4H)-yl)-alkanamides (5a-j) and 4-chloro-N'-((1-methyl (or 1,2-dimethyl)-4-oxo-1,2-dihydroquinazolin-3(4H)-yl)-alkaloyl)benzohydrazides (6a-f) were designed based on the previously reported essential structural features for an...

journal_title：Archiv der Pharmazie

authors： Noureldin NA,Kothayer H,Lashine EM,Baraka MM,El-Eraky W,Awdan SA

更新日期：2017-02-01 00:00:00

abstract：:Ten pyrazole derivatives were synthesized and evaluated for their ability to inhibit the replication of influenza virions. All the compounds were synthesized in good-to-excellent yield, and the structures were ascertained with the help of (1) H NMR, (13) C NMR, mass, and elemental analysis. Among the tested series, co...

journal_title：Archiv der Pharmazie

authors： Meng FJ,Sun T,Dong WZ,Li MH,Tuo ZZ

更新日期：2016-03-01 00:00:00

abstract：:A rapid and efficient one-pot condensation reaction of long-chain alkyl and alkenyl acid hydrazides and nitriles was carried out to afford 3,5-disubstituted-1H-1,2,4-triazoles. The compounds 5a-o were screened for in-vitro antibacterial activity against the representative panel of two Gram-positive and two Gram-negati...

journal_title：Archiv der Pharmazie

authors： Sharma S,Gangal S,Rauf A,Zahin M

更新日期：2008-11-01 00:00:00

abstract：:3-Ethyl 5-methyl 1,4-dihydro-2-[(2-hydroxyethoxy) methyl]-6-methyl-4-(2,3-dichlorophenyl)-3,5-pyridinedicarboxylate (13), a bioisostere of amlodipine, was prepared by the reaction of ethyl 4-(2-hydroxyethoxy)acetoacetate (11) with methyl 2-(2,3-dichlorobenzylidene)acetoacetate (12) and NH4OAc. Compound 13 was elaborat...

journal_title：Archiv der Pharmazie

authors： Yiu SH,Knaus EE

更新日期：1999-10-01 00:00:00

abstract：:Albumin binding for the enantiomers of four closely related N-methyl-5-phenyl-5-alkyl-barbiturates 1-4 was investigated for three different mammalian species by means of equilibrium dialysis. Lipid solubility (n-heptane/phosphate buffer distribution coefficient) increased stepwise by a factor of 56 from 1 to 4. Bovine...

journal_title：Archiv der Pharmazie

authors： Büch HP,Krug R,Knabe J

更新日期：1996-08-01 00:00:00

abstract：:Although a large number of pharmaceutical therapies are available to treat cardiovascular diseases like heart failure, in many medical conditions treatment is still not optimal and, therefore, the need for innovative, safe and efficacious drugs is still very high in this indication. Biomarkers are an important tool in...

journal_title：Archiv der Pharmazie

authors： Kramer F,Dinh W

更新日期：2016-06-01 00:00:00

abstract：:Solid-state Nuclear Magnetic Resonance (NMR) provides a general method to study molecular structure and dynamics in a non-crystalline and insoluble environment. We discuss the latest methodological progress to construct 3D molecular structures from solid-state NMR data obtained under magic-angle-spinning conditions. A...

journal_title：Archiv der Pharmazie

authors： Luca S,Heise H,Lange A,Baldus M

更新日期：2005-06-01 00:00:00

abstract：:Cycloaddition reactions of the nitrilimines 4-6 with N-arylmaleimides 7 and acrylamide (11) yield the pyrrolopyrazole derivatives 8-10 and 2-pyrazolines 12, respectively, in excellent yield. The regioselectivity and biological activities of some of the new compounds were investigated. ...

journal_title：Archiv der Pharmazie

authors： Ead HA,Hassaneen HM,Abdallah MA,Mousa HA

更新日期：1991-01-01 00:00:00

abstract：:The precise definition of the structural requirements for effective topoisomerase II poisoning by drug molecules is still an elusive issue. In the attempt to better define a pharmacophoric pattern, we prepared several conjugates combining the chemical features of two well-known topoisomerase II poisons, amsacrine and ...

journal_title：Archiv der Pharmazie

authors： Zagotto G,Gianoncelli A,Sissi C,Marzano C,Gandin V,Pasquale R,Capranico G,Ribaudo G,Palumbo M

更新日期：2014-10-01 00:00:00