Dopamine/serotonin receptor ligands, part III [1]: synthesis and biological activities of 7, 7'-alkylene-bis-6, 7, 8, 9, 14, 15-hexahydro-5H-benz[d]indolo[2, 3-g]azecines -- application of the bivalent ligand approach to a novel type of dopamine receptor

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：:36 Novel heterocyclic chalcone derivatives were synthesized and tested for their anti-bacterial activity. Some compounds presented good anti-microbial activities against Gram-positive bacteria (including the multidrug-resistant clinical isolates). This class of compounds presented high potency against Streptococcus mu...

journal_title：Archiv der Pharmazie

authors： Zheng CJ,Jiang SM,Chen ZH,Ye BJ,Piao HR

更新日期：2011-10-01 00:00:00

abstract：:The plant pentacyclic alkaloid camptothecin and its structural analogs were extensively studied. These compounds are interesting due to the antitumor activity associated with their ability to inhibit topoisomerase I in tumor cells. During the last decades of the 20th century, a large number of the silicon-containing c...

journal_title：Archiv der Pharmazie

authors： Lazareva NF,Baryshok VP,Lazarev IM

更新日期：2018-01-01 00:00:00

abstract：:Design, synthesis, and cytotoxic activity of amidine derivatives of melphalan are described and structure-activity relationships are discussed. Evaluation of the cytotoxicity of these compounds employing a MTT assay and inhibition of [(3)H]thymidine incorporation into DNA in both MDA-MB-231 and MCF-7 human breast canc...

journal_title：Archiv der Pharmazie

authors： Bielawska A,Bielawski K,Anchim T

更新日期：2007-05-01 00:00:00

abstract：:Three novel series of quinoline derivatives have been prepared by cyclization of the intermediate 3-(1,3-dioxolan-2-yl)-2-substituted thiocarbamoyl-hydrazinoquinolines with different alpha-halocarbonyl compounds. These series are: 3-(1,3-dioxolan-2-yl)-2-(3-substituted-4-phenylthiazolin-2-y lidene) hydrazinoquinolines...

journal_title：Archiv der Pharmazie

authors： Farghaly AM,Habib NS,Khalil MA,el-Sayed OA,Bistawroos AE

更新日期：1990-04-01 00:00:00

abstract：:A new series of 2-(3-(N-(substituted phenyl)sulfamoyl)ureido)benzothiazoles was synthesized via a one-pot efficient and scalable method, involving the condensation of 2-aminobenzothiazoles derivatives, substituted anilines, and chlorosulfonyl isocyanate. The products were obtained in good yield with a simple workup, a...

journal_title：Archiv der Pharmazie

authors： Cheraiet Z,Meliani S,Nessaib M,Hessainia S,Boukhari A,Djahoudi A,Regainia Z

更新日期：2019-08-01 00:00:00

abstract：:Cathepsin B and plasmin are intra- or extracellular proteases that are overexpressed by several solid tumors. In order to exploit both proteases as molecular targets for tumor-specific cleavage of prodrugs, an albumin-binding formulation of methotrexate was developed that incorporated the peptide sequence D-Ala-Phe-Ly...

journal_title：Archiv der Pharmazie

authors： Warnecke A,Fichtner I,Sass G,Kratz F

更新日期：2007-08-01 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：:We report on the synthesis and biological evaluation of two series of 2,4,5-polysubstituted thiazoles comprising the acid hydrazide functionality and some derived pharmacophores known to contribute to various chemotherapeutic activities. All newly synthesized compounds were subjected to in-vitro antibacterial and anti...

journal_title：Archiv der Pharmazie

authors： Al-Saadi MS,Faidallah HM,Rostom SA

更新日期：2008-07-01 00:00:00

abstract：:Several 5-alkoxy-tetrazolo[1,5-a]quinazoline derivatives have been synthesized by reacting 2,4-dichloroquinazoline with various phenols or aliphatic alcohol and then with sodium azide. The structures of these compounds have been confirmed by IR, MS,( 1)H-NMR, and elementary analysis. Anticonvulsant activities were eva...

journal_title：Archiv der Pharmazie

authors： Wang HJ,Wei CX,Deng XQ,Li FL,Quan ZS

更新日期：2009-11-01 00:00:00

abstract：:2- or 6-(1-Hydroxyiminoalkyl)-5,8-dimethoxy-1,4-naphthoquin-one (DMNQ) and 6-(1-propyloxyimino- alkyl)-DMNQ derivatives were synthesized, and their inhibitory effects on DNA topoisomerase-I (TOPO-I) and antiproliferative activities against L1210 cells were examined. In a comparison, it was found that 6-(1-hydroxyimino...

journal_title：Archiv der Pharmazie

authors： Song GY,Kim Y,You YJ,Cho H,Kim SH,Sok DE,Ahn BZ

更新日期：2000-04-01 00:00:00

abstract：:Salicylamide amino acid conjugates were prepared utilizing 5-formyl-, 5-dicyanoethenyl-, and 5-nitroethenylsalicylic acid. 5-Substituted salicylanilides were treated with glycine and formaldehyde in a Mannich type reaction affording the corresponding 3-(N-glycino)salicylanilides. The reactions of anilines with pyrans ...

journal_title：Archiv der Pharmazie

authors： Nawwar GA

更新日期：1994-04-01 00:00:00

abstract：:Both 2-nitrooxymethyl-4-phenyl- (2) and 4-nitrooxymethylphenyl-1,4-dihydropyridines (3) represent new combinations of two different vasodilating structures. 2 could not be isolated due to its spontaneous lactonization. Derivatives of 3 were obtained via Hantzsch synthesis using nitrooxymethylated benzaldehydes. The in...

journal_title：Archiv der Pharmazie

authors： Lehmann J,Kahlich R,Meyer zum Gottesberge C,Fricke U

更新日期：1997-08-01 00:00:00

abstract：:Styrylquinazoline derivatives were prepared by Perkin condensation and evaluated for inhibitory activity against HIV-1 integrase. Among them, compound 5c containing a free catechol ring was the most potent (IC(50)=0.8 +/- 1.9 microM)and showed 6-fold more potency than the corresponding styrylquinoline compound (IC(50)...

journal_title：Archiv der Pharmazie

authors： Lee JY,Park JH,Lee SJ,Park H,Lee YS

更新日期：2002-06-01 00:00:00

abstract：:A series of homochiral 7-substituted 1-aminoindans was prepared by means of asymmetric reductive amination from racemic 7-substituted 1-indanones via E-imines and E-imine/enamine mixtures, respectively, and subjected to 5-hydroxytryptamine (5-HT) receptor subtype binding studies. The ee's of the title compounds were d...

journal_title：Archiv der Pharmazie

authors： Landsiedel-Maier D,Frahm AW

更新日期：1998-02-01 00:00:00

abstract：:A novel dimer of 2-(4-pyridylmethyl)-1-indanone (2) was obtained while carrying out aldol condensation of 1-indanone with pyridine-4-carboxaldehyde in potassium hydroxide. The structure of dimer 3 has been established using various spectral techniques and was screened for its ability to inhibit the cytochrome P(450) e...

journal_title：Archiv der Pharmazie

authors： Gupta R,Jindal DP,Jit B,Narang G,Palusczak A,Hartmann RW

更新日期：2004-07-01 00:00:00

abstract：:Several 4-cyano-1,5-diphenylpyrazoles attached to different heterocyclic ring systems at position 3 were synthesized starting from ethyl 4-cyano-1,5-diphenyl-1H-pyrazole-3-carboxylate 1. The newly synthesized compounds were tested in vivo for their anti-estrogenic effects and evaluated in vitro for their cytotoxic pro...

journal_title：Archiv der Pharmazie

authors： Farag AM,Mayhoub AS,Eldebss TM,Amr AG,Ali KA,Abdel-Hafez NA,Abdulla MM

更新日期：2010-07-01 00:00:00

abstract：:In an effort to develop new molecules with improved antihyperlipidemic activity, eight new 2-azetidinone analogs (4a-4h) of ezetimibe were designed through in silico docking experiments with the crystal structure of the Niemann-Pick C1-like 1 protein (NPC1L1). Synthesis and further antihyperlipdemic evaluation of this...

journal_title：Archiv der Pharmazie

authors： Arya N,Dwivedi J,Khedkar VM,Coutinho EC,Jain KS

更新日期：2013-12-01 00:00:00

abstract：:Novel C-5 substituted 6,2'-anhydrouridines 5a-e are synthesized from the hitherto unknown monosubstituted ribofuranosylbarbituric acid derivatives 4a-e. These molecules are high-anti-fixed by a 6,2'-linkage and were assumed to show antiviral and antineoplastic effects. In cell culture test systems, however, none of th...

journal_title：Archiv der Pharmazie

authors： Folkers G,Junginger G,Müller CE,Schloz U,Eger K

更新日期：1989-02-01 00:00:00

abstract：:The synthesis of two series of derivatives containing the quinazolinone-4 moiety is described. 3-Amino-2(1H)-thioxo-4(3H)-quinazolinone (1) was subjected to reactions with halogenoketones and halogenoaldehydes, leading to the production of the corresponding ketones, aldehydes, Schiff bases, and 6-oxo-1,4,5-thiadiazin[...

journal_title：Archiv der Pharmazie

authors： Nawrocka W,Zimecki M

更新日期：1997-12-01 00:00:00

abstract：:In search of structure-activity relationships among histamine H3-receptor antagonists the imidazole ring of known H3-receptor antagonists was replaced by different heteroaromatic ring systems. Thus, azines and diazines with ether (6-13) and carbamate (15-24) moieties as functional groups were synthesized. The obtained...

journal_title：Archiv der Pharmazie

authors： Kieć-Kononowicz K,Ligneau X,Stark H,Schwartz JC,Schunack W

更新日期：1995-05-01 00:00:00

abstract：:Rationally designed Mycobacterium tuberculosis (Mtb) inhibitors were synthesized under Buchwald conditions using Pd2 (dba)3 /xantphos and the compounds were investigated for their biological activity against the Mtb standard strain H37Rv and two other clinically isolated multidrug-resistant strains with different drug...

journal_title：Archiv der Pharmazie

authors： Gangarapu NR,Ranganatham A,Reddy EK,Yellappa S,Chandrasekhar KB

更新日期：2020-07-01 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：:The design, synthesis, and investigation of antitumor and anti-lipase activities of some coumarin-triazole hybrid molecules are reported. The synthesis of these hybrid molecules was performed under microwave irradiation and conventional heating procedures. The newly synthesized hybrid molecules were investigated as in...

journal_title：Archiv der Pharmazie

authors： Kahveci B,Yılmaz F,Menteşe E,Ülker S

更新日期：2017-08-01 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：:Fourteen new 1-[(N, N-disubstituted thiocarbamoylthio)acetyl]-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives (7a-n) were synthesised by reacting 1-(chloroacetyl)-3-(2-thienyl)-5-aryl-2-pyrazolines (5a-g) and appropriate sodium salts of N, N-disubstituted dithiocarbamoic acids (6a, b). The structures of the synthesised ...

journal_title：Archiv der Pharmazie

authors： Turan-Zitouni G,Ozdemir A,Güven K

更新日期：2005-03-01 00:00:00

abstract：:The active form of vitamin D3 , calcitriol, is a potent antiproliferative compound. However, when effective antitumor doses of calcitriol are used, hypercalcemic effects are observed, thus blocking its therapeutic application. To overcome this problem, structural analogues have been designed with the aim of retaining ...

journal_title：Archiv der Pharmazie

authors： Obiol DJ,Martínez A,Ferronato MJ,Quevedo MA,Grioli SM,Alonso EN,Gómez G,Fall Y,Facchinetti MM,Curino AC

更新日期：2019-05-01 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：:New analogues of nifedipine, in which the 2-nitrophenyl group at position 4 is replaced by a 1-methyl-5-nitro-2-imidazolyl substituent, were synthesized. The symmetrical dialkyl 1, 4-dihydro-2, 6-dimethyl-4-(1-methyl-5-nitro-2-imidazolyl)-3, 5-pyridinedicarboxylates were prepared by a classical Hantzsch condensation. ...

journal_title：Archiv der Pharmazie

authors： Miri R,Javidnia K,Kebriaie-Zadeh A,Niknahad H,Shaygani N,Semnanian S,Shafiee A

更新日期：2003-09-01 00:00:00

abstract：:New phosphoramide mustards (6-8) have been prepared from the antibiotics 2 and 3, and from 5. The mixture of cyclophosphamides could be separated by preparative layer and column chromatography. The assignments of configuration to the isomeric phosphoramidates was based on the magnetic anisotropy of the P = O bond. The...

journal_title：Archiv der Pharmazie

authors： Csorvási A,Kövér KE,Menyhárt MM,Sztaricskai F,Dobrynin YV,Nikolaeva TG

更新日期：1998-09-01 00:00:00