Design, synthesis and biological evaluation of some 2-azetidinone derivatives as potential antihyperlipidemic agents.

abstract：:A number of novel pyridazinomorphinans have been synthesized by the inverse electron demand Diels-Alder reaction of various 3,6-disubstituted 1,2,4,5-tetrazines with enamines derived from dihydrocodeinone and with codeinone. Reduction of some of the pyridazinomorphinans did not furnish the expected pyrroloepoxymorphin...

journal_title：Archiv der Pharmazie

authors： Klindert T,Stroetmann I,Seitz G,Höfner G,Wanner KT,Frenzen G,Eckhoff B

更新日期：1997-06-01 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：: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 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：:In an attempt to counteract bacterial pathogenicity, a set of novel imidazolidine-2,4-dione and 2-thioxoimidazolidin-4-one derivatives was synthesized and evaluated as inhibitors of bacterial virulence. The new compounds were characterized and screened for their effects on the expression of virulence factors of Pseudo...

journal_title：Archiv der Pharmazie

authors： Mohamed B,Abdel-Samii ZK,Abdel-Aal EH,Abbas HA,Shaldam MA,Ghanim AM

更新日期：2020-05-01 00:00:00

abstract：:A series of novel 2,4-disubstituted 7-methyl-1,1,3-trioxo-2,4-dihydro-pyrazolo[4,5-e] [1,2,4]thiadiazines (PTDs) was synthesized, structurally confirmed by spectral analysis, and evaluated for their anti-HIV activities by inhibition of HIV-induced cytopathogenicity in MT-4 cell culture. The results showed that some co...

journal_title：Archiv der Pharmazie

authors： Liu XY,Yan RZ,Wang Y,Zhan P,De Clercq E,Pannecouque C,Witvrouw M,Molina MT,Vega S

更新日期：2008-04-01 00:00:00

abstract：:2-Acetyl-(6-picolyl)-4N-substituted thiosemicarbazones and their copper(II) complexes were shown to be potent antineoplastic and cytotoxic agents against murine and human cultured cells. Numerous derivatives were as active against solid tumor growth as clinically useful agents. The agents inhibited L1210 DNA and RNA s...

journal_title：Archiv der Pharmazie

authors： Miller MC 3rd,Bastow KF,Stineman CN,Vance JR,Song SC,West DX,Hall IH

更新日期：1998-04-01 00:00:00

abstract：:A series of 7, 7'-alkylene-bridged dimers(7a-e) of the benz [d]indolo[3, 2-f]azecine derivative LE300 was synthesized. Affinity and functional activity at dopamine D(1) and D(2) receptors were estimated by radioligand binding and a functional Ca(2+) assay. All the new bivalent ligands showed significant binding affini...

journal_title：Archiv der Pharmazie

authors： Abadi AH,Lankow S,Hoefgen B,Decker M,Kassack MU,Lehmann J

更新日期：2002-08-01 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：:[4-(Adamantane-1-carboxamido)-3-oxo-1-thia-4-azaspiro[4.4]nonan-2-yl]acetic acid (4a) and [4-(adamantane-1-carboxamido)-8-nonsubstituted/substituted-3-oxo-1-thia-4-azas-piro[4.5]decane-2-yl]acetic acid (4b-g) derivatives were synthesized; their structures were verified by elemental analysis, infrared spectroscopy, 1 H...

journal_title：Archiv der Pharmazie

authors： Turk-Erbul B,Karaman EF,Duran GN,Ozbil M,Ozden S,Goktas F

更新日期：2021-01-06 00:00:00

abstract：:Schistosoma mansoni histone deacetylase 8 (SmHDAC8) has been recently identified as a new potential target for the treatment of schistosomiasis. A series of newly designed and synthesized alkoxyamide-based and hydrazide-based HDAC inhibitors were tested for inhibitory activity against SmHDAC8 and human HDACs 1, 6, and...

journal_title：Archiv der Pharmazie

authors： Stenzel K,Chakrabarti A,Melesina J,Hansen FK,Lancelot J,Herkenhöhner S,Lungerich B,Marek M,Romier C,Pierce RJ,Sippl W,Jung M,Kurz T

更新日期：2017-08-01 00:00:00

abstract：:Structural studies of hydroxy-aluminum phosphates with antacid application are performed. The antacid properties of the products depend on their chemical composition and way of preparation. Scanning electron microscope, X-ray- and IR-spectroscopy have evidenced the formation of a one-phase product. The IR-spectra indi...

journal_title：Archiv der Pharmazie

authors： Misheva E

更新日期：1990-08-01 00:00:00

abstract：:Novel 6,11-dioxo-6,11-dihydro-benzo[f]pyrido[1,2-a]indole-12-carboxamide derivatives and the corresponding 7,10-dihydroxy analogues were designed in accordance with Moore's and Pindur's theory and synthesized based on the structural similarity with known antitumour agents such as ellipticine, daunorubicin, mitoxantron...

journal_title：Archiv der Pharmazie

authors： Defant A,Guella G,Mancini I

更新日期：2007-03-01 00:00:00

abstract：:We report in this work the synthesis, cytotoxicity, and antimicrobial activity of ([1,2,4]triazolo[1,5-c]quinazolin-2-ylthio)carboxylic acid amides 4-7 in connection with our previous research in the preparation of triazoloquinazoline derivatives. Due to simplicity, general availability of starting materials, and high...

journal_title：Archiv der Pharmazie

authors： Antipenko LN,Karpenko AV,Kovalenko SI,Katsev AM,Komarovska-Porokhnyavets EZ,Novikov VP

更新日期：2009-11-01 00:00:00

abstract：:A series of oximes deriving from 5-arylidene-pyrrolidine-2,3,4-triones and pyridine-2,3,4-triones has been prepared. The presence of the tautomeric nitrosoenol was proven in solutions of alpha-ketooxime 7a. The binding affinity of the new oximes toward the N-methyl-D-aspartate (glycine site) receptor has been measured...

journal_title：Archiv der Pharmazie

authors： Poschenrieder H,Höfner G,Stachel HD

更新日期：1999-09-01 00:00:00

abstract：:Rapamycin is an mTOR allosteric inhibitor with multiple functions such as immunosuppressive, anticancer, and lifespan prolonging activities. Its C-43 semi-synthetic derivatives temsirolimus and everolimus have been used as mTOR targeting anticancer drugs in the clinic. Following our previous research on antitumor rapa...

journal_title：Archiv der Pharmazie

authors： Huang Q,Xie L,Chen X,Yu H,Lv Y,Huang X,Ying J,Zheng C,Cheng Y,Huang J

更新日期：2018-11-01 00:00:00

abstract：:The syntheses, conformational studies, and investigations on the estrogen receptor binding of [R/S-1-(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]platinum(II) complexes (1-PtL2, 2L = leaving groups) are described. A Strecker synthesis using the 2,6-dichloro-4-methoxybenzaldehyde, NaCN, and NH4Cl afforded the cyanoami...

journal_title：Archiv der Pharmazie

authors： Gust R,Lubczyk V,Schmidt K,Shihada U

更新日期：2001-03-01 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：:N-Methoxyquinolinium salts 3 are prepared as potential cardiotonic agents by alkylation of the corresponding N-oxides 2 synthesized by two different methods. 1. Oxidation of some quinoline derivatives 1 using 30% H2O2 or 3-chloroperbenzoic acid. 2. Nitration of the quinoline-N-oxides 2a, 2c, and 2m. Preparation of 2h ...

journal_title：Archiv der Pharmazie

authors： Bünz C,Heber D,Ravens U

更新日期：1993-04-01 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：:In an attempt to find a new class of antibacterial agents, we have synthesized thirty new coumarin (2H-benzopyran-2-one) analogues. These derivatives include substituted azetidin-2-ones (beta-lactam) 3a-f, pyrrolidin-2-ones 4a-f, 2H-1,3,4-oxadiazoles 5a-f, and thiazolidin-4-ones 6a-f attached to 4-phenyl-2H-benzopyran...

journal_title：Archiv der Pharmazie

authors： Hassan GS,Farag NA,Hegazy GH,Arafa RK

更新日期：2008-11-01 00:00:00

abstract：:Previously, we demonstrated that certain heterocyclic compounds derived from 3-substituted-1,2,4-triazole-5-thiones had promising analgesic/anti-inflammatory activities together with low ulcerogenic properties. Therefore, we sought to design and synthesize new derivatives of triazol-5-thiones-fused heterocycles. In th...

journal_title：Archiv der Pharmazie

authors： Sert-Ozgur S,Tel BC,Somuncuoglu EI,Kazkayasi I,Ertan M,Tozkoparan B

更新日期：2017-07-01 00:00:00

abstract：:Some 2-arylpyrazolo[1,5-c][1,3]benzoxazin-5-ones 1 and 5- oxopyrazolo[1,5-c][1,3]benzoxazin-2-carboxylates 2 were prepared and biologically evaluated for their binding at benzodiazepine receptor (BZR) in rat cortical membranes. Structure-activity relationship studies suggest that, although proton donor d and proton ac...

journal_title：Archiv der Pharmazie

authors： Varano F,Catarzi D,Colotta V,Cecchi L,Filacchioni G,Galli A,Costagli C

更新日期：1996-12-01 00:00:00

abstract：:Schiff base transition metal complexes are an important class of compounds with great potential for therapeutic interventions. However, data on antileukemic and antilymphoma effects of these complexes are limited. The activity of N,N'-bis(salicylidene)-1,2-phenylenediamine (salophene, 1), its iron(II/III) and manganes...

journal_title：Archiv der Pharmazie

authors： Hille A,Wolf T,Schumacher P,Ott I,Gust R,Kircher B

更新日期：2011-04-01 00:00:00

abstract：:Michael-type reaction of compounds of type 9 were studied. Addition reactions with acrolein and methyl vinyl ketone, respectively, lead--depending on the conditions--to pyridoindoles of type 16 and 14 and/or to tetrahydrocarbazoles of type 17 and 15. With Triton B compounds 15 undergo retro-Michael-type elimination of...

journal_title：Archiv der Pharmazie

authors： Mahboobi S,Burgemeister T,Kastner F

更新日期：1995-01-01 00:00:00

abstract：:A series of 5-amino-3-methylisoxazole-4-carboxylic acid amides has been prepared by condensation of 5-amino-3-methylisoxazole-4-carboxylic acid with ethyl chloroformate. The resulting mixed anhydride undergoes condensation with appropriate phenylamides to form the corresponding amides 6-16. The compounds obtained were...

journal_title：Archiv der Pharmazie

authors： Ryng S,Zimecki M,Sonnenberg Z,Mokrosz MJ

更新日期：1999-05-01 00:00:00

abstract：:6-(1-Acyloxyalkyl)-5,8-dimethoxy-1,4-naphthoquinone (DMNQ; 5,8-dimethoxy-1,4-naphthoquinone) derivatives were synthesized and examined for their inhibitory effect on DNA topoisomerase-I (Topo I) and their antiproliferative activity against L1210 cells. The Topo-I inhibitory effect of 6-(1-hydroxyalkyl)-DMNQ derivative...

journal_title：Archiv der Pharmazie

authors： Kim Y,You YJ,Ahn BZ

更新日期：2001-10-01 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：: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 derivatives of 1H-benzimidazole-2-carboxylic acid (BICA, 2a) were tested in vitro in comparison to 1H-indole-2-carboxylic acid (ICA, 1e) for their ability to displace [3H]glycine from rat hippocampal membranes. Compound 2a was 8 times more potent than 1e (Ki 5.3 microM, as compared to 42 microM). However, intr...

journal_title：Archiv der Pharmazie

authors： Berger ML,Schödl C,Noe CR

更新日期：1996-03-01 00:00:00