Azines and diazines as potential histamine H3-receptor antagonists.

abstract：:A new series of N,N'-(benzene-1,3-diyldi-1,3,4-oxadiazole-5,2-diyl)bis{2-[(5-benzene-1,3-diyl-1,3,4-oxadiazol-2-yl)amino]acetamide}(macrocycle 1), N,N'-(benzene-1,3-diyldi-1,3,4-thiadiazole-5,2-diyl)bis{2-[(5-benzene-1,3-diyl-1,3,4-thiadiazol-2-yl)amino]acetamide} (macrocycle 2) and S,S'-[benzene-1,3-diylbis(4H-1,2,4-...

journal_title：Archiv der Pharmazie

authors： Vinay Kumar B,Naik HS,Girija D,Sharath N,Sudeep HV,Joy Hoskeri H

更新日期：2012-03-01 00:00:00

abstract：:The regio- and stereospecific synthesis of O-methyl-chiro-inositols and O-methyl-scyllo-inositol was achieved, starting from p-benzoquinone. After preparing dimethoxy conduritol-B as a key compound, regiospecific bromination of the alkene moiety of dimethoxy conduritol-B and acid-catalyzed ring opening of dimethoxydia...

journal_title：Archiv der Pharmazie

authors： Aksu K,Akincioglu H,Gulcin I,Kelebekli L

更新日期：2020-09-30 00:00:00

abstract：:Furfurylidenemalononitriles and thienylidenemalononitriles were treated with 1,3-cyclohexanediones to afford 2-amino-4-hetaryl-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile derivatives. The molluscicidal activity of these compounds was investigated. ...

journal_title：Archiv der Pharmazie

authors： Abdelrazek FM,Metz P,Farrag EK

更新日期：2004-09-01 00:00:00

abstract：:The ongoing interest in very efficient systems for the imitation of cytochrome P-450-dependent monooxygenase reactions, consisting of metalloporphyrin and oxygen donor, prompted us to develop a method to compare the catalytic activity of soluble metalloporphyrins with those which have been immobilised on different sil...

journal_title：Archiv der Pharmazie

authors： Lübbe AN,Rickerts B,Duchstein HJ

更新日期：2006-12-01 00:00:00

abstract：:New condensed derivatives of anpirtoline, in which the pyridine ring is replaced with quinoline, quinazoline, 7-chloroquinoline, and 7-chloroquinazoline nuclei, have been synthesized. Their receptor binding profiles (5-HT1A, 5-HT1B) and analgesic activity (hot plate, acetic acid induced writhing) have been studied. Th...

journal_title：Archiv der Pharmazie

authors： Rádl S,Hezky P,Proska J,Krejcí I

更新日期：2000-11-01 00:00:00

abstract：:A screening study was conducted to examine the effect of a series of synthesized pyrazoloquinoline derivatives on the growth of Leishmania donovani promastigotes. Sixteen compounds were tested, ten of which showed an inhibitory effect on the growth of promastigotes. Compound 1 demonstrated potent antileishmanial activ...

journal_title：Archiv der Pharmazie

authors： Al-Qahtani A,Siddiqui YM,Bekhit AA,El-Sayed OA,Aboul-Enein HY,Al-Ahdalb MN

更新日期：2005-10-01 00:00:00

abstract：:6-Amino-5-imino-pyrazolo[4',3':5,6]pyrano[2,3-d]pyrimidine derivative 4 and pyrazolo-[4',3':5,6]pyrano[2,3-d]pyrimidin-5-ylhydrazine derivative 5 were prepared starting from 6-amino-3-methyl-4-(p-nitrophenyl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile 1. The synthesis and structure characterization of 9,11-dihydr...

journal_title：Archiv der Pharmazie

authors： Shamroukh AH,Zaki ME,Morsy EM,Abdel-Motti FM,Abdel-Megeid FM

更新日期：2007-07-01 00:00:00

abstract：:A series of new Mannich bases of N-[(4-arylpiperazin-1-yl)-methyl]-3-(chlorophenyl)-pyrrolidine-2,5-diones 10-23 have been synthesized and evaluated for their anticonvulsant activity in maximum electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure threshold tests. Their neurotoxicity was determined us...

journal_title：Archiv der Pharmazie

authors： Obniska J,Kopytko M,Zagórska A,Chlebek I,Kamiński K

更新日期：2010-06-01 00:00:00

abstract：:Polyketide-derived macrolactones like zearalenone (1), zearalane (2) or curvularin (3) display a wide range of interesting pharmacological activities. Here, we present a short and efficient approach towards this class of natural products by a combination of the Sonogashira and Mitsunobu reactions. The resulting lacton...

journal_title：Archiv der Pharmazie

authors： Krauss J,Unterreitmeier D,Neudert C,Bracher F

更新日期：2005-12-01 00:00:00

abstract：:The 5-desoxy analogue of BW245C, imidazolidin-2-one 3, has been synthesized by reduction of the N-benzyl hydantoin derivative 6. Compound 3 was found to be approximately equipotent with BW245C as an inhibitor of platelet aggregation and this result indicates that the 5-keto group of BW245C is not essential for platele...

journal_title：Archiv der Pharmazie

authors： Barraclough P,Jackson WP,Harris CJ

更新日期：1991-08-01 00:00:00

abstract：:Alzheimer's disease (AD) is a neurodegenerative disorder characterized by dementia, memory impairment, cognitive dysfunction, and speech impairment. The utility of cholinergic replacement by acetylcholinesterase (AChE) inhibitors in AD treatment has been well documented so far. Recently, studies have also evidenced th...

journal_title：Archiv der Pharmazie

authors： Kalaycı M,Türkeş C,Arslan M,Demir Y,Beydemir Ş

更新日期：2020-11-06 00:00:00

abstract：:The present work describes the synthesis and antifungal evaluation of new 5-arylidene-(Z)-2-dimethylamino-1,3-thiazol-4-ones 4a-f, obtained by the reaction of aromatic aldehydes 1 and rhodanine 2 followed by treatment with DMF. All compounds were tested against a panel of yeasts, hialohyphomycetes, and dermatophytes u...

journal_title：Archiv der Pharmazie

authors： Insuasty B,Gutiérrez A,Quiroga J,Abonia R,Nogueras M,Cobo J,Svetaz L,Raimondi M,Zacchino S

更新日期：2010-01-01 00:00:00

abstract：:The synthesis of a novel library of purine derivatives bearing various bicyclic and polycylic substituents at the N-9 position is described. The series includes norbornanes, bicyclo[2.2.2]octanes, and bicyclo[3.2.1]octanes attached at the bridgehead position as well as bicyclo[3.1.1]heptanes, tetrahydro-1-naphthalenes...

journal_title：Archiv der Pharmazie

authors： Dejmek M,Sála M,Plačková P,Hřebabecký H,Mascarell Borredà L,Neyts J,Dračínský M,Procházková E,Jansa P,Leyssen P,Mertlíková-Kaiserová H,Nencka R

更新日期：2014-07-01 00:00:00

abstract：:A series of 5-alkyl-5-phenylbarbituric acid analogues were shown to be potent hypolipidemic agents in rats and mice at 20 mg/kg/day. This dose is lower than that required for hypolipidemic activity for clofibrate and nicotinic acid derivatives in rodents and man. These new derivatives reduced both serum cholesterol an...

journal_title：Archiv der Pharmazie

authors： Hall IH,Patrick MA,Maguire JH

更新日期：1990-09-01 00:00:00

abstract：:The combined effects of amino acid antagonists with proven or potential inhibitory activities on aminoacyl-tRNA synthetases were investigated on the murine leukemic cell line P388 D1. As the best result a summation of the antiproliferative effects was observed. Combinations with established cytostatic agents like plat...

journal_title：Archiv der Pharmazie

authors： Laske R,Schönenberger H,Holler E

更新日期：1991-03-01 00:00:00

abstract：:To identify new agents for the treatment of American cutaneous leishmaniasis, a series of eight 1,4-bis(substituted benzalhydrazino)phthalazines was evaluated against Leishmania braziliensis and Leishmania mexicana parasites. These compounds represent a disubstituted version of the 1-chloro-4-(monoaryl/heteroarylhydra...

journal_title：Archiv der Pharmazie

authors： Romero AH,Rodríguez N,Oviedo H,Lopez SE

更新日期：2019-06-01 00:00:00

abstract：:Novel sulfur-containing glutethimide derivatives, substituted with either thiol or methylsulfide groups in the ortho/para positions of the aromatic ring, were synthesized and tested for both human placental aromatase and bovine adrenocortical desmolase inhibitory activities. The synthesis was achieved by the chlorosul...

journal_title：Archiv der Pharmazie

authors： Bednarski PJ,Hartmann RW

更新日期：1993-07-01 00:00:00

abstract：:A series of hydantoin prostaglandin analogues, in which the hexamethylene moiety of the acid side chain was replaced by other spacing groups possessing either ether, sulphide and/or olefin functionality, were prepared and evaluated for platelet aggregation inhibiting activity. The 4-thia analogue 13*) proved to be the...

journal_title：Archiv der Pharmazie

authors： Barraclough P,Caldwell AG,Glen RC,Harris CJ,Stepney R,Whittaker N,Whittle BJ

更新日期：1993-02-01 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：:Reaction of K2PtCl4 with the substituted 2-aminomethylpyridines 9, 14, and 22 affords the corresponding dichloroplatinum(II) complexes 3-5. Compounds 3 and 22 show remarkable relative binding affinities for the estrogen receptor. Towards the hormone-independent P388-tumor of the CD2F1-mouse the platinum(II) complexes ...

journal_title：Archiv der Pharmazie

authors： Brunner H,Nerl G,von Angerer E,Knebel N

更新日期：1991-10-01 00:00:00

abstract：:The synthesis of tacrine-thiadiazolidinone hybrids is described. These compounds are designed as dual acetylcholinesterase inhibitors binding simultaneously to the peripheral and catalytic sites of the enzyme. All tested compounds exhibit significant AChE inhibitory activity. Competition assays using propidium as refe...

journal_title：Archiv der Pharmazie

authors： Dorronsoro I,Alonso D,Castro A,del Monte M,García-Palomero E,Martínez A

更新日期：2005-01-01 00:00:00

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 series of potent HIV-protease inhibitors has been prepared. Several of the newly synthesized compounds showed high plasma even after oral administration to animals. Based on the overall biological profile, CGP 61755 was chosen for further preclinical evaluation. For this compound, a 10 step synthesis potentially sui...

journal_title：Archiv der Pharmazie

authors： Capraro HG,Bold G,Fässler A,Cozens R,Klimkait T,Lazdins J,Mestan J,Poncioni B,Rösel JL,Stover D,Lang M

更新日期：1996-06-01 00:00:00

abstract：:Numerous novel N,N-disubstituted 5-alkyliden- or 5-aralkyliden-3-aminorhodanines 2 have been prepared by condensation of carbonyl compounds with 1. The effectiveness of some derivatives in an "akanthose test" with hairless mice was shown. ...

journal_title：Archiv der Pharmazie

authors： Hanefeld W,Helfrich V,Jalili MA,Schlitzer M

更新日期：1993-06-01 00:00:00

abstract：:New, non-imidazole histamine H3 receptor antagonists were prepared and in vitro tested as H3 receptor antagonists measured as the electrically evoked contraction of the guinea-pig jejunum. The 2-(1-piperidinyl)- and 2-(1-pyrrolidinyl)benzothiazoles show no or very poor activity; 2-[1-(4-amino)piperidinyl]- and 2-(1,2-...

journal_title：Archiv der Pharmazie

authors： Walczyński K,Guryn R,Zuiderveld OP,Timmerman H

更新日期：1999-11-01 00:00:00

abstract：:Pyrrolo[3,4-c]-beta-carbolinedione dimers 5-14 were synthesized from furo[3,4-c]-beta-carbolinediones and diamines by solvent-free TaCl5/silica catalyzed reaction under microwave irradiation. The inhibitory property of these target compounds, the starting materials 2, 31, 32, and the N-alkylated pyrrolo[3,4-c]-beta-ca...

journal_title：Archiv der Pharmazie

authors： Mahboobi S,Eluwa S,Kumar S,Koller M,Störl K

更新日期：1999-07-01 00:00:00

abstract：:A set of 40 derivatives of 3-hydroxypicolinic acid and 2-sulfanylbenzoic acid, isosteric to salicylanilides was synthesized. The compounds were evaluated for in vitro activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium, Candida albicans, Candida tropicalis, Candida krusei, Candi...

journal_title：Archiv der Pharmazie

authors： Waisser K,Pesina M,Holý P,Pour M,Bures O,Kunes J,Klimesová V,Buchta V,Kubanová P,Kaustová J

更新日期：2003-08-01 00:00:00

abstract：:The synthesis and preliminary assays as hypocholesterolemic agents of five N-diphenylmethylpiperazines are described. The evaluations were carried out in hypercholesterolemic mice and two of these compounds were more effective than bezafibrate in the test employed. The di-p-chlorosubstituted compounds showed higher ac...

journal_title：Archiv der Pharmazie

authors： Alivert A,Canals F,Bonet JJ,Gómez-Parra V,Sánchez-Alonso F

更新日期：1991-09-01 00:00:00

abstract：:The 2-(2-Bromophenyl)-acetaldehyde acetals 8 are treated with n-BuLi and the aldehydes 7 and 11 to form the hydroxyacetales 9 and 12, respectively. 9 is cyclized under acidic conditions to the epoxybenzoxocine 2; analogously 12 yields the epoxydibenzoxocine 14. ...

journal_title：Archiv der Pharmazie

authors： Wünsch B

更新日期：1990-11-01 00:00:00

abstract：:Copper and zinc have been found to contribute to the burden of amyloid-β (Aβ) aggregations in neurodegenerative Alzheimer's disease (AD). Dysregulation of these metals leads to the generation of reactive oxygen species (ROS) and eventually results in oxidative damage and accumulation of the Aβ peptide, which are the k...

journal_title：Archiv der Pharmazie

authors： Fu CL,Hsu LS,Liao YF,Hu MK

更新日期：2016-05-01 00:00:00