Benzimidazole-type glycine antagonists: the role of the ring nitrogen atoms.

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

abstract：:A group of racemic 3-[2-nitrooxyethyl (1,3-dinitrooxy-2-propyl or 4-nitrophenylethyl)] 5-isopropyl 1,4-dihydro-2,6-dimethyl-4-[2- trifluoromethylphenyl (2-nitrophenyl or 3-nitrophenyl)]-3,5-pyridinedicarboxylates 13-15 were prepared using the Hantzsch reaction that involved the condensation of 2-nitrooxyethyl 9a, 1,3-...

journal_title：Archiv der Pharmazie

authors： Iqbal N,Knaus EE

更新日期：1996-01-01 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：:The pyrrolidino enaminones, with the carboxylic acid chain fixed at the nitrogen, inhibit cyclooxygenase more potently or selectively than 5-lipoxygenase. According to the structure-activity relationships discussed the potency depends significantly on the chain length of the carboxylic acid, the substitution pattern o...

journal_title：Archiv der Pharmazie

authors： Dannhardt G,Bauer A,Nowe U

更新日期：1997-03-01 00:00:00

abstract：:Platensimycin is a natural product isolated from various strains of Streptomyces platensis which exhibits antimicrobial activity against Gram positive bacteria, including vancomycin- and linezolide-resistant species. Analogues of platensimycin were synthesized from 3-aminobenzoic acid or other aniline derivatives and ...

journal_title：Archiv der Pharmazie

authors： Krauss J,Knorr V,Manhardt V,Scheffels S,Bracher F

更新日期：2008-06-01 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：: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：:The oncoprotein cytotoxic associated gene A (CagA) of Helicobacter pylori plays a pivotal role in the development of gastric cancer, so it has been an important target for anti-H. pylori drugs. Conventional drugs are currently being implemented against H. pylori. The inhibitory role of plant metabolites like curcumin ...

journal_title：Archiv der Pharmazie

authors： Srivastava AK,Tewari M,Shukla HS,Roy BK

更新日期：2015-08-01 00:00:00

abstract：:Two series of amino-1,4-benzoquinones (AQ1-18) based on the structural analogs of plastoquinones were synthesized and the structure-activity relationship against chronic myelogenous leukemia activity was examined. All of the synthesized compounds were tested for their cytotoxic effects on different leukemic cell lines...

journal_title：Archiv der Pharmazie

authors： Ciftci HI,Bayrak N,Yıldırım H,Yıldız M,Radwan MO,Otsuka M,Fujita M,Tuyun AF

更新日期：2019-12-01 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：:New series of perimidine derivatives and fused perimidines were derived from the reaction of ketene aminals 1 and 2 with diazotized anilines or hydrazonoyl chlorides. In addition, 8,10-disubstituted-[1,2,4]triazolo[4,3-a]perimidines (20a-m) were prepared through the reaction of perimidine-2-thione (15) with hydrazonoy...

journal_title：Archiv der Pharmazie

authors： Farghaly TA,Mahmoud HK

更新日期：2013-05-01 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：:1-Substiuted 6-(3-cyanobenzoyl) and [(3-cyanophenyl)fluoromethyl]-5-ethyl-uracils were synthesized and evaluated in cell-based assays against HIV-1 wild-type and its clinically relevant non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant mutants. Some of the synthesized compounds showed activity against H...

journal_title：Archiv der Pharmazie

authors： Loksha YM,Pedersen EB,Loddo R,La Colla P

更新日期：2009-09-01 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：:The antioxidant and acetylcholinesterase inhibitory properties of novel symmetric sulfamides derived from phenethylamines were evaluated. Phenethylamines 8-11 were reacted with SO2Cl2 in the presence of Et3N to afford sulfamides in good yields. The synthesized sulfamides were converted to their phenolic derivatives wi...

journal_title：Archiv der Pharmazie

authors： Aksu K,Topal F,Gulcin İ,Tümer F,Göksu S

更新日期：2015-06-01 00:00:00

abstract：:Enantiomerically pure 1, 2-diamino-1-(4-fluorophenyl)propanes were synthesized by stereospecific and stereoselective procedures by use of the (1R, 2S)- and (1S, 2R)-2-amino-1-(4-fluorophenyl)propanols (12a) as intermediates. The enantiomeric purity was determined by (1)H NMR spectroscopy after conversion of the propan...

journal_title：Archiv der Pharmazie

authors： Dufrasne F,Gelbcke M,Schnurr B,Gust R

更新日期：2002-05-01 00:00:00

abstract：:Isatin and azole moieties, which have the ability to form various noncovalent interactions with different therapeutic targets, are common pharmacophores in drug development. Isatin and azole derivatives possess promising in vitro and in vivo anticancer activity, and many of them, such as semaxanib, sunitinib, and carb...

journal_title：Archiv der Pharmazie

authors： Hou Y,Shang C,Wang H,Yun J

更新日期：2020-01-01 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：: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：:We describe a method to determine the affinity constant values between Ketoprofen and beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin in semisolid vehicles. The method is based on the diffusion of the drug, released from semisolid vehicles, through a lipidic non porous membrane. The affinity constants of Ketopro...

journal_title：Archiv der Pharmazie

authors： Orienti I,Zecchi V,Bertasi V,Fini A

更新日期：1991-12-01 00:00:00

abstract：:The butadiene derivatives 10a-c react with the oxa-bicyclooctanone 9 to give the cyclohexene annulated oxatropanes 11a-c. The acetoxyderivatives 11b and 11c can be transformed into the cyclohexadiene or benzene derivatives 13 and 12, respectively. 11a reacts with HN3 to afford the tricyclic oxazepanone 14 which can be...

journal_title：Archiv der Pharmazie

authors： Eiden F,Kainz A,Gebhard R

更新日期：1992-02-01 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：: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：: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 newly synthesized analogs of NAN-190 containing m-Cl and m-CF(3) substituents in the arylpiperazine moiety and their conformationally restricted counterparts showed a very high 5-HT(1A )receptor affinity. In the LLR test, the flexible compounds 4a and 5a displayed features of a partial agonist and agonist, respect...

journal_title：Archiv der Pharmazie

authors： Paluchowska MH,Bugno R,Charakchieva-Minol S,Bojarski AJ,Tatarczyńska E,Chojnacka-Wójcik E

更新日期：2006-09-01 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：: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：: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：:Despite cellular complexity, a limited number of small molecules act as intracellular second messengers. Protein kinase A (PKA) is the main transducer of the information carried by cyclic adenosine monophosphate (cAMP). Recently, cellular imaging has achieved major technical advancements, although the search for more ...

journal_title：Archiv der Pharmazie

authors： Ribaudo G,Zagotto G,Ongaro A,Ricci A,Caretta A,Mucignat-Caretta C

更新日期：2020-04-01 00:00:00

abstract：:The effect of triterpenes and flavonoids on the activity of several hyaluronic acid-splitting enzymes was investigated. Studies showed that the inhibitory effect of the triterpenes glycyrrhizin and glycyrrhetinic acid is dependent on the source of hyaluronate lyase. Hyaluronate lyase from Streptococcus agalactiae (Hya...

journal_title：Archiv der Pharmazie

authors： Hertel W,Peschel G,Ozegowski JH,Müller PJ

更新日期：2006-06-01 00:00:00