Comparison of activity of immobilised and soluble metalloporphyrins by NO release of oximes by chemiluminescence.

abstract：:Syntheses of a new series of biologically potent α-aminophosphonates were accomplished by one-pot Kabachnik-Fields reaction using TiO2-SiO2 as solid supported catalyst under microwave irradiation conditions. The chemical structures of all the newly synthesized compounds were confirmed by analytical and spectral (IR, 1...

journal_title：Archiv der Pharmazie

authors： Chinthaparthi RR,Bhatnagar I,Gangireddy CS,Syama SC,Cirandur SR

更新日期：2013-09-01 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：:A short series of arylhydrazones of 4-[(2-methylimidazo[1,2-a]pyridine-3-yl)azo]benzoic acid hydrazide was synthesized and tested for antimicrobial activity. All of the compounds show antimicrobial activity against Escherichia coli. A few members were also active against Klebsiella pneumoniae, Staphylococcus aureus an...

journal_title：Archiv der Pharmazie

authors： Cesur Z,Büyüktimkin S,Büyüktimkin N,Derbentli S

更新日期：1990-03-01 00:00:00

abstract：:A series of novel N-(4,5-dihydroimidazol-2-yl)-1,3-dihydrobenzimidazole derivatives 2a-d, 3a-d and 4a-p were prepared and their structure was determined by IR and NMR spectroscopic data as well as X-ray analysis of carbonitrile 2a. The compounds were studied as potential inhibitors of the human blood platelet aggregat...

journal_title：Archiv der Pharmazie

authors： Saczewski F,Debowski T,Petrusewicz J,Trzeciak H,Krzystanek E,Krzystanek M,Gdaniec M,Nowakowska E

更新日期：1998-07-01 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：:CXC chemokine receptor-3 (CXCR3) is a G-protein coupled receptor (GPCR) predominantly expressed on activated T lymphocytes that promote Th1 responses. Previously, we described the 3H-quinazolin-4-one containing VUF 5834 (decanoic acid {1-[3-(4-cyano-phenyl)-4-oxo-3,4-dihydro-quinazolin-2-yl]-ethyl}-(2-dimethylamino-et...

journal_title：Archiv der Pharmazie

authors： Storelli S,Verzijl D,Al-Badie J,Elders N,Bosch L,Timmerman H,Smit MJ,De Esch IJ,Leurs R

更新日期：2007-06-01 00:00:00

abstract：:Solid-state Nuclear Magnetic Resonance (NMR) provides a general method to study molecular structure and dynamics in a non-crystalline and insoluble environment. We discuss the latest methodological progress to construct 3D molecular structures from solid-state NMR data obtained under magic-angle-spinning conditions. A...

journal_title：Archiv der Pharmazie

authors： Luca S,Heise H,Lange A,Baldus M

更新日期：2005-06-01 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：:A series of hydantoin prostaglandin analogues, in which the hexamethylene moiety of the acid side chain was replaced by other spacing groups possessing either ether, sulphide and/or olefin functionality, were prepared and evaluated for platelet aggregation inhibiting activity. The 4-thia analogue 13*) proved to be the...

journal_title：Archiv der Pharmazie

authors： Barraclough P,Caldwell AG,Glen RC,Harris CJ,Stepney R,Whittaker N,Whittle BJ

更新日期：1993-02-01 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：:Rapamycin, a potent antifungal antibiotic, was approved as immunosuppressant, and lately its derivatives have been developed into mTOR targeting anticancer drugs. Structure modification was performed at the C-42 position of rapamycin, and a novel series of rapamycin triazole hybrids (4a-d, 5a-e, 8a-e, and 9a-e) was fa...

journal_title：Archiv der Pharmazie

authors： Xie L,Huang J,Chen X,Yu H,Li K,Yang D,Chen X,Ying J,Pan F,Lv Y,Cheng Y

更新日期：2016-06-01 00:00:00

abstract：:In this study, a number of 2,5-disubstituted 1,3,4-thiadiazoles were synthesized using an appropriate synthetic route, and their anticonvulsant activity was determined by the maximal electroshock seizure (MES) test and their neurotoxicity was evaluated by the rotarod test. Additionally, their hypnotic activity was tes...

journal_title：Archiv der Pharmazie

authors： Toolabi M,Khoramjouy M,Aghcheli A,Ayati A,Moghimi S,Firoozpour L,Shahhosseini S,Shojaei R,Asadipour A,Divsalar K,Faizi M,Foroumadi A

更新日期：2020-12-01 00:00:00

abstract：:3-Ethyl 5-methyl 1,4-dihydro-2-[(2-hydroxyethoxy) methyl]-6-methyl-4-(2,3-dichlorophenyl)-3,5-pyridinedicarboxylate (13), a bioisostere of amlodipine, was prepared by the reaction of ethyl 4-(2-hydroxyethoxy)acetoacetate (11) with methyl 2-(2,3-dichlorobenzylidene)acetoacetate (12) and NH4OAc. Compound 13 was elaborat...

journal_title：Archiv der Pharmazie

authors： Yiu SH,Knaus EE

更新日期：1999-10-01 00:00:00

abstract：:6-Amino-5-imino-pyrazolo[4',3':5,6]pyrano[2,3-d]pyrimidine derivative 4 and pyrazolo-[4',3':5,6]pyrano[2,3-d]pyrimidin-5-ylhydrazine derivative 5 were prepared starting from 6-amino-3-methyl-4-(p-nitrophenyl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile 1. The synthesis and structure characterization of 9,11-dihydr...

journal_title：Archiv der Pharmazie

authors： Shamroukh AH,Zaki ME,Morsy EM,Abdel-Motti FM,Abdel-Megeid FM

更新日期：2007-07-01 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：: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：: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：:The new chemical entities febuxostat and topiroxostat have been approved by the US Food and Drug Administration, opening new avenues for exploiting different heterocycles other than purines as xanthine oxidase (XO) inhibitors. A different series of substituted 2-benzamido-4-methylthiazole-5-carboxylic acid derivatives...

journal_title：Archiv der Pharmazie

authors： Ali MR,Kumar S,Afzal O,Shalmali N,Ali W,Sharma M,Bawa S

更新日期：2017-02-01 00:00:00

abstract：:A 3D pharmacophore model predicting anticonvulsant activity was obtained for a series of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives recently disclosed as a new class of noncompetitive AMPA receptor antagonists. The training set included 17 compounds with varying potency against audiogenic seizures in DBA...

journal_title：Archiv der Pharmazie

authors： De Luca L,Gitto R,Barreca ML,Caruso R,Quartarone S,Citraro R,De Sarro G,Chimirri A

更新日期：2006-07-01 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：:The 5-HT1A and 5-HT2 receptor affinity of a set of 44 N-alkylated 1-aryl-piperazines and their analogs has been analyzed: the n-hexyl derivatives were the most potent and the most selective 5-HT1A ligands of all the investigated N-alkyl homologues. The alkyl chain may stabilize the 5-HT1A receptor-ligand complex by hy...

journal_title：Archiv der Pharmazie

authors： Mokrosz JL,Mokrosz MJ,Charakchieva-Minol S,Paluchowska MH,Bojarski AJ,Duszyńska B

更新日期：1995-02-01 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：: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：:Based upon molecular modeling, the pharmacophore of potential inhibitors of p38 MAPK (mitogen-activated protein kinases) is discussed and the predictive binding affinities are calculated. Syntheses of original diarylimidazo[2,1-a]phthalazines obtained by Suzuki coupling are described. ...

journal_title：Archiv der Pharmazie

authors： Mavel S,Thery I,Gueiffier A

更新日期：2002-01-01 00:00:00

abstract：:This review emphasizes the relationship of breast cancer, estrogen receptor and ligands, especially the centrality of the estrogen receptor, which mediates on one hand the hormone-induced gene transcription and on the other hand the anti-estrogen action against breast cancer. The characterization of the estrogen recep...

journal_title：Archiv der Pharmazie

authors： Bai Z,Gust R

更新日期：2009-03-01 00:00:00

abstract：:A series of 1-¿omega-(4-aryl-1-piperazinyl)alkyl]indolin-2(1H)-one derivatives 2-14 was synthesized in order to obtain ligands with a dual 5-HT1A/5-HT2A activity. The majority of those compounds (2-5, 7, 10-13) exhibited a high 5-HT1A (Ki = 2-44 nM) and/or 5-HT2A affinity (Ki = 51 and 39 for 5 and 7, respectively). In...

journal_title：Archiv der Pharmazie

authors： Mokrosz MJ,Duszyńska B,Misztal S,Kłodzińska A,Tatarczyńska E,Chojnacka-Wójcik E,Dziedzicka-Wasylewska M

更新日期：1998-10-01 00:00:00

abstract：:A series of 4-amino-7,8-dimethoxy-5H-pyrimido[5,4-b]indole derivatives has been synthesized. These compounds resemble carbazeram and other pyridazino compounds with activity in the cardiovascular system. Some of these new compounds possess inotropic activity (Table 2), with a complementary effect on the inhibition of ...

journal_title：Archiv der Pharmazie

authors： Monge A,Martínez-Crespo FJ,Villanueva MA,Font M,Santiago E,Martínez de Irujo JJ,Alberdi E,López-Unzu MJ,Cenarruzabeitia E,Castiella E

更新日期：1993-11-01 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：:The synthesis and odour properties of the new santalol analogue, methyl-beta-santalol, are described. The additional methyl group adjacent to the hydroxyl function of the standard molecule, beta-santalol, deprives the new compound of the sandalwood note. The synthesis and the odour evaluation of this compound supports...

journal_title：Archiv der Pharmazie

authors： Buchbauer G,Zechmeister-Machhart F,Weiss-Greiler P,Wolschann P

更新日期：1997-04-01 00:00:00

abstract：:Polyketide-derived macrolactones like zearalenone (1), zearalane (2) or curvularin (3) display a wide range of interesting pharmacological activities. Here, we present a short and efficient approach towards this class of natural products by a combination of the Sonogashira and Mitsunobu reactions. The resulting lacton...

journal_title：Archiv der Pharmazie

authors： Krauss J,Unterreitmeier D,Neudert C,Bracher F

更新日期：2005-12-01 00:00:00