Synthesis and antibacterial activity of new 7-piperazinyl-quinolones containing a functionalized 2-(furan-3-yl)ethyl moiety.

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：: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：: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：:The activity of 72 1,4-dihydropyridines as calcium channel antagonists was examined. The simplified molecular input-line entry system (SMILES) was used as representation of the molecular structure of the calcium channel antagonists. Quantitative structure-activity relationships (QSARs) were developed using CORAL softw...

journal_title：Archiv der Pharmazie

authors： Veselinović AM,Milosavljević JB,Toropov AA,Nikolić GM

更新日期：2013-02-01 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：: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：:The histone deacetylase (HDAC) enzyme plays an important role in gene transcription. Inhibitors of histone deacetylases induce cell differentiation and suppress cell proliferation in tumor cells. Hydroxamates with rigid linker have displayed better inhibition profiles than those with linear and flexible aliphatic link...

journal_title：Archiv der Pharmazie

authors： Chakrabarty S,Jasmine,Bhadaliya C,Sinha BN,Mahesh A,Bai H,Blond SY,Jayaprakash V

更新日期：2010-03-01 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：: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：:Novel thiazolyl hydrazonothiazolamines and 1,3,4-thiadiazinyl hydrazonothiazolamines were synthesized by a facile one-pot multicomponent approach by the reaction of 2-amino-4-methyl-5-acetylthiazole, thiosemicarbazide or thiocarbohydrazide and phenacyl bromides or 3-(2-bromoacetyl)-2H-chromen-2-ones in acetic acid wit...

journal_title：Archiv der Pharmazie

authors： Sujatha K,Ommi NB,Mudiraj A,Babu PP,Vedula RR

更新日期：2019-12-01 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：:We describe the synthesis and positive inotropic evaluation of a series of 2-(4-substitutedbenzyl-1,4-diazepan-1-yl)-N-(4,5-dihydro-1-phenyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamides by measuring left atrial stroke volume in preparations of isolated rabbit-heart. Several compounds were developed from, and showed ...

journal_title：Archiv der Pharmazie

authors： Jiang SM,Ye BJ,Liu XK,Zhang TY,Cui X,Piao HR

更新日期：2010-11-01 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：: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：: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：: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：: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 this study, we have explored the prevention of gastric side effects such as gastric lesions and bleeding while maintaining the high analgesic and anti-inflammatory activities by the derivatization of the carboxylate moiety into amides in [5-chloro-6-(2-chloro/fluorobenzoyl)-2-benzoxazolinone-3-yl]acetic acids. We h...

journal_title：Archiv der Pharmazie

authors： Banoglu E,Okçelik B,Kupeli E,Unlü S,Yeşilada E,Amat M,Caturla JF,Sahin MF

更新日期：2003-07-01 00:00:00

abstract：:Phosphono-analogues of glutathione containing the O = P(OR)2 moiety in place of the cysteinyl residue CH2SH 1a-1d were prepared by solution phase peptide synthesis. Benzyl, benzyloxy-carbonyl, and tert-butyl protecting groups were used to mask the individual amino acid functional groups. The formation of peptide bonds...

journal_title：Archiv der Pharmazie

authors： Kunze T

更新日期：1996-11-01 00:00:00

abstract：:Antibiotic-resistant bacteria continue to play an important role in human health and disease. Inventive strategies are necessary to develop new therapeutic leads to challenge drug-resistance problems. From this perception, new quinoline hybrids bearing bioactive pharmacophores were synthesized. The newly synthesized c...

journal_title：Archiv der Pharmazie

authors： Rizk OH,Bekhit MG,Hazzaa AAB,El-Khawass EM,Abdelwahab IA

更新日期：2019-10-01 00:00:00

abstract：:The biotransformation of the positively inotropically active compound N-methyl-N-(2-hydroxy-3-phenoxy-propyl)-11-(2-aminoethyl)-6,11- dihydrodibenz[b,e]-oxepine, neutral fumarate, (Doxaminol, racemic mixture of diastereomeres) in dogs is examined. The metabolits M1-M7 were isolated and their chemical structures identi...

journal_title：Archiv der Pharmazie

authors： Neidlein R,Volland C,Kramer W

更新日期：1990-05-01 00:00:00

abstract：:A series of eperezolid analogs with glycinyl substitutions were prepared and their antibacterial activities were studied against a panel of susceptible and resistant Gram-positive bacteria. The compounds with N-arylacyl or N-heteroarylacyl glycinyl structural units showed good antibacterial activities. The compounds 1...

journal_title：Archiv der Pharmazie

authors： Wang XJ,Wu N,Du GJ,Zhao SQ,Yan M,Gu LQ

更新日期：2009-07-01 00:00:00

abstract：:Various aryl 1-pyrryl sulfones were synthesized and tested as inhibitors of HIV-1. 2-Nitrophenyl-2-ethoxycarbonyl-1-pyrryl sulfone, the most active among test derivatives, was selected as lead compound of the aryl pyrryl sulfone series. The in vitro anti-HIV-1 activity and cytotoxicity of 41 compounds is reported. Som...

journal_title：Archiv der Pharmazie

authors： Artico M,Silvestri R,Stefancich G,Massa S,Pagnozzi E,Musu D,Scintu F,Pinna E,Tinti E,La Colla P

更新日期：1995-03-01 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：:Three series of imidazolidinium ligands (NHC precursors) substituted with 4-vinylbenzyl, 2-methyl-1,4-benzodioxane, and N-propylphthalimide were synthesized. N-Heterocyclic carbene (NHC) precursors were prepared from N-alkylimidazoline and alkyl halides. The novel NHC precursors were characterized by 1 H NMR, 13 C NMR...

journal_title：Archiv der Pharmazie

authors： Aktaş A,Taslimi P,Gülçin İ,Gök Y

更新日期：2017-06-01 00:00:00

abstract：:Poly(vinyl alcohol) was crosslinked with ethylene glycol diglycidyl ether to obtain hydrogel-forming polymers. The polymers were also substituted with oleoyl chloride, providing hydrogels with weak solubility. These new polymeric materials were evaluated for the formulation of sustained drug delivery systems. Vancomyc...

journal_title：Archiv der Pharmazie

authors： Orienti I,Treré R,Luppi B,Bigucci F,Cerchiara T,Zuccari G,Zecchi V

更新日期：2002-03-01 00:00:00

abstract：:A novel approach to the pyridoacridine ring system of the ascididemin-type marine alkaloids is presented. This approach allows for the introduction of the ring A of the alkaloids by using a simple aromatic aldehyde building block. The viability of this approach is demonstrated with the synthesis of AK37, a bioactive d...

journal_title：Archiv der Pharmazie

authors： Raeder S,Bracher F

更新日期：2012-10-01 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：: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：: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