Synthesis and anti-HIV-1 activity of 1-substiuted 6-(3-cyanobenzoyl) and [(3-cyanophenyl)fluoromethyl]-5-ethyl-uracils.

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：: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：:A number of C-3 spirocyclic 2-benzazepine analogs of α-phenyl-N-tert-butyl nitrone (PBN) were synthesized and tested for their activity in protecting rat brain mitochondria and dopaminergic (DA) neurons against 6-hydroxydopamine (6-OHDA), a toxin inducing destruction of the DA nigro-striatal pathway in rodent models o...

journal_title：Archiv der Pharmazie

authors： Soto-Otero R,Méndez-Álvarez E,Sánchez-Iglesias S,Labandeira-García JL,Rodríguez-Pallares J,Zubkov FI,Zaytsev VP,Voskressensky LG,Varlamov AV,de Candia M,Fiorella F,Altomare C

更新日期：2012-08-01 00:00:00

abstract：:The complex of lanthanum (III) was synthesized reacting the respective inorganic salt with 5-aminoorotic acid in amounts equal to the metal:ligand molar ratio of 1:3. The complex was prepared by adding an aqueous solution of lanthanum (III) nitrate to an aqueous solution of the ligand, subsequently raising the pH of t...

journal_title：Archiv der Pharmazie

authors： Kostova I,Rastogi VK,Kiefer W,Kostovski A

更新日期：2006-11-01 00:00:00

abstract：:The aim of this study was to develop a novel nanosize drug candidate for cancer therapy. For this purpose, (S)-methyl 2-[(7-hydroxy-2-oxo-4-phenyl-2H-chromen-8-yl)methyleneamino]-3-(1H-indol-3-yl)propanoate (ND3) was synthesized by the condensation reaction of 8-formyl-7-hydroxy-4-phenylcoumarin with l-tryptophan meth...

journal_title：Archiv der Pharmazie

authors： Budama-Kilinc Y,Kecel-Gunduz S,Ozdemir B,Bicak B,Akman G,Arvas B,Aydogan F,Yolacan C

更新日期：2020-11-01 00:00:00

abstract：:The synthesis of some new analogs of quinolin-4-one and 1,7-naphthyridin-4-one is described. The prepared compounds were tested for their in vitro antitumor and cdc2 kinase or cdc25 phosphatase inhibitory activity. Compound ethyl 7-oxo-2,3-dihydro-7H-pyrido [1,2,3-de][2,3-b]pyrido-1,4-thiazine-6-carboxylate (6b) showe...

journal_title：Archiv der Pharmazie

authors： el-Subbagh HI,Abadi AH,al-Khawad IE,al-Rashood KA

更新日期：1999-01-01 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

abstract：:A synthesis of two new active substances, DOMCl (1-(4-chloromethyl-2, 5-dimethoxyphenyl)-2-propanamine; 2) and DOMOM (1-(2, 5-dimethoxy-4-methoxymethylphenyl)-2-propanamine; 3), was developed. Unexpectedly, the Blanc reaction permitted successful synthesis of 2, 5-dimethoxyphenylpropylamine derivatives having a substi...

journal_title：Archiv der Pharmazie

authors： Harms A,Ulmer E,Kovar KA

更新日期：2003-06-01 00:00:00

abstract：:Fifteen new indazole derivatives have been synthesized. In the Born test, compounds (4f) and (4g) were most active. They inhibited the blood platelet aggregation induced by collagen with an IC(50) = 85 or 90 microM, respectively. After oral administration to rats (60 mg/kg) three of the compounds significantly inhibit...

journal_title：Archiv der Pharmazie

authors： Yildiz AK,Rehse K,Stasch JP,Bischoff E

更新日期：2004-06-01 00:00:00

abstract：:The key step in the synthesis of the pharmacologically interesting 1-phenyltetrahydro-3-benzazepine skeleton is the Michael addition of (2-lithiophenyl)acetaldehyde acetals, which are generated in situ upon treatment of the bromo acetals 5a,b with n-butyllithium, to beta-nitrostyrene (6). The reductive ring closure of...

journal_title：Archiv der Pharmazie

authors： Wünsch B,Nerdinger S,Bauschke G,Höfner G

更新日期：1997-07-01 00:00:00

abstract：:A new class of acetamidomethylsulfonyl bis heterocycles-oxazolyl-1,3,4-oxadiazoles, -thiazolyl-1,3,4-oxadiazoles, and -imidazolyl-1,3,4-oxadiazoles were synthesized from the synthetic intermediates, methyl 2-((4-aryloxazol-2-ylcarbamoyl)methylsulfonyl)acetate, methyl 2-((4-arylthiazol-2-ylcarbamoyl)methylsulfonyl)acet...

journal_title：Archiv der Pharmazie

authors： Mahaboob Basha N,Lavanya G,Padmaja A,Padmavathi V

更新日期：2013-07-01 00:00:00

abstract：:Series of N-(4-substitutedphenyl)-4-(1-methyl (or 1,2-dimethyl)-4-oxo-1,2-dihydroquinazolin-3(4H)-yl)-alkanamides (5a-j) and 4-chloro-N'-((1-methyl (or 1,2-dimethyl)-4-oxo-1,2-dihydroquinazolin-3(4H)-yl)-alkaloyl)benzohydrazides (6a-f) were designed based on the previously reported essential structural features for an...

journal_title：Archiv der Pharmazie

authors： Noureldin NA,Kothayer H,Lashine EM,Baraka MM,El-Eraky W,Awdan SA

更新日期：2017-02-01 00:00:00

abstract：:A novel series of N-(2-(piperazin-1-yl)phenyl)aryl carboxamide derivatives were simply synthesized by Ugi-multicomponent reaction as β-secretase (BACE1) inhibitors. The BACE1 inhibitory activity of the synthesized compounds was examined using a Forester resonance energy transfer (FRET)-based assay. Among the tested co...

journal_title：Archiv der Pharmazie

authors： Edraki N,Firuzi O,Fatahi Y,Mahdavi M,Asadi M,Emami S,Divsalar K,Miri R,Iraji A,Khoshneviszadeh M,Firoozpour L,Shafiee A,Foroumadi A

更新日期：2015-05-01 00:00:00

abstract：:Permeability glycoprotein (P-gp) is involved in the pathology of various diseases including cancer and epilepsy, mainly through the translocation of some medicines across the cell membrane. Here, we employed image-based quantitative structure-activity relationship (QSAR) models to predict the P-gp inhibitory activity ...

journal_title：Archiv der Pharmazie

authors： Shayanfar S,Shayanfar A,Ghandadi M

更新日期：2016-02-01 00:00:00

abstract：:In the present study, a novel series of polyfunctionalized imidazopyrimidines 6a-u and 9a-d were efficiently constructed by a domino reaction between 2-imino-6-substituted-2,3-dihydropyrimidin-4(1H)-ones 4a-d or 8a-c and 2-bromoacetophenones 5a-i under mild basic conditions. The synthesized series were screened for th...

journal_title：Archiv der Pharmazie

authors： Abdel-Mohsen HT,Abood A,Flanagan KJ,Meindl A,Senge MO,El Diwani HI

更新日期：2020-03-01 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 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：: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：: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：:The synthesis and the pharmacological properties of some new prazosin analogues are described. ...

journal_title：Archiv der Pharmazie

authors： Rampa A,Valenti P,Da Re P,Carrara M,Zampiron S,Cima L,Giusti P

更新日期：1989-06-01 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

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：:Prevention of the formation of advanced glycation end-products (AGEs) is a reliable approach to achieve control over hyperglycemia and the associated pathogenesis of diabetic vascular complications. In these terms, new synthetic approaches to 6-nitroazolo[1,5-a]pyrimidines have been developed on the basis of the promi...

journal_title：Archiv der Pharmazie

authors： Spasov AA,Babkov DA,Sysoeva VA,Litvinov RA,Shamshina DD,Ulomsky EN,Savateev KV,Fedotov VV,Slepukhin PA,Chupakhin ON,Charushin VN,Rusinov VL

更新日期：2017-12-01 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：: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：: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：: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：:Two new arylnaphthalide lignans, procumphthalide A (1) and 4-O-beta-D-glucopyranosyl-(1"'-->2")-beta-D-apiofuranosyldiphyllin, named procumbenoside B (2), along with cilinaphthalide B (3) and several other known compounds were isolated from the methanolic extracts of Justicia procumbens. By using NMR and other spectra...

journal_title：Archiv der Pharmazie

authors： Weng JR,Ko HH,Yeh TL,Lin HC,Lin CN

更新日期：2004-04-01 00:00:00

abstract：:In this study, some novel cyanine dyes, 1, 3, and 5-15, were synthesized by a one-pot step reaction of pyridinium salts 2 and/or 4 with benzenaminium salt 1. N-{[1-Chloro-3,4-dihydronaphthalen-2-yl)methylene]benzenaminium} chloride 1 was obtained by the reaction of α-tetralone with Vilsmeier-Haack reagent, followed by...

journal_title：Archiv der Pharmazie

authors： Fadda AA,Tawfik EH,Abdel-Motaal M,Selim YA

更新日期：2020-11-10 00:00:00

abstract：:A new series of 4-hydroxycoumarin derivatives 3a-d was synthesized by the reaction of 3-bromo-4-hydroxy coumarin 1 with various heteroaldehydes 2a-d in good yields. The synthesized compounds were characterized on the basis of their elemental and spectral (IR, (1)H-NMR and mass spectrometry) analysis. All target compou...

journal_title：Archiv der Pharmazie

authors： Siddiqui ZN,N MM,Ahmad A,Khan AU

更新日期：2011-06-01 00:00:00