Novel 3,6-disubstituted 7H-1,2,4-triazolo[3,4-b][1,3,4]thiadiazines: synthesis, characterization, and evaluation of analgesic/anti-inflammatory, antioxidant activities.

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 diffusion of a series of non steroidal antiinflammatory drugs through a silicone rubber membrane has been studied from suspensions both of the free and beta-cyclodextrin complexes forms at different pH values of the medium. Higher diffusion rates of the complexed forms as compared with the free ones and a rate-lim...

journal_title：Archiv der Pharmazie

authors： Orienti I,Cavallari C,Zecchi V,Fini A

更新日期：1989-04-01 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：:A set of 40 derivatives of 3-hydroxypicolinic acid and 2-sulfanylbenzoic acid, isosteric to salicylanilides was synthesized. The compounds were evaluated for in vitro activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium, Candida albicans, Candida tropicalis, Candida krusei, Candi...

journal_title：Archiv der Pharmazie

authors： Waisser K,Pesina M,Holý P,Pour M,Bures O,Kunes J,Klimesová V,Buchta V,Kubanová P,Kaustová J

更新日期：2003-08-01 00:00:00

abstract：:The chemical reactivity of cytotoxic 5-indolone derivatives is examined in order to get ideas about their behaviour in biological systems. Dienone-phenol-rearrangement preserving the indole ring system could not be achieved, aromatization of 1b gives the phenol derivative 3 alpha. In diluted NaOH ester hydrolysis occu...

journal_title：Archiv der Pharmazie

authors： Eger K,Frey M

更新日期：1992-09-01 00:00:00

abstract：:A range of novel pyridine-2,4,6-tricarbohydrazide thiourea compounds (4a-i) were synthesized in good to excellent yields (63-92%). The enzyme inhibitory potentials of these compounds were investigated against α- and β-glucosidases because these enzymes play a crucial role in treating type-2 diabetes mellitus (T2DM). A...

journal_title：Archiv der Pharmazie

authors： Rehman TU,Riaz S,Khan IU,Ashraf M,Bajda M,Gawalska A,Yar M

更新日期：2018-01-01 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

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：: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 active form of vitamin D3, 1α,25(OH)2D3, plays a major role in maintaining calcium/phosphate homeostasis. In addition, it is a potent antiproliferative and pro-differentiating agent. Unfortunately, it usually causes hypercalcemia in vivo when effective antitumour doses are used. It has therefore been found necessa...

journal_title：Archiv der Pharmazie

authors： Ferronato MJ,Salomón DG,Fermento ME,Gandini NA,López Romero A,Rivadulla ML,Pérez-García X,Gómez G,Pérez M,Fall Y,Facchinetti MM,Curino AC

更新日期：2015-05-01 00:00:00

abstract：:Salicylamide amino acid conjugates were prepared utilizing 5-formyl-, 5-dicyanoethenyl-, and 5-nitroethenylsalicylic acid. 5-Substituted salicylanilides were treated with glycine and formaldehyde in a Mannich type reaction affording the corresponding 3-(N-glycino)salicylanilides. The reactions of anilines with pyrans ...

journal_title：Archiv der Pharmazie

authors： Nawwar GA

更新日期：1994-04-01 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 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：:Novel betulin derivatives were prepared and tested for their antitumor activity. Starting from 3-O-acetyl- or 3-O-methyl-betulinic aldehyde, the synthesis of C-28 ethynyl derivatives was performed; their subsequent transformation with several 1,3-dipolarophiles afforded pyrazoles and 1,2,3-triazoles. Their screening f...

journal_title：Archiv der Pharmazie

authors： Csuk R,Barthel A,Sczepek R,Siewert B,Schwarz S

更新日期：2011-01-01 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：:Three novel series of quinoline derivatives have been prepared by cyclization of the intermediate 3-(1,3-dioxolan-2-yl)-2-substituted thiocarbamoyl-hydrazinoquinolines with different alpha-halocarbonyl compounds. These series are: 3-(1,3-dioxolan-2-yl)-2-(3-substituted-4-phenylthiazolin-2-y lidene) hydrazinoquinolines...

journal_title：Archiv der Pharmazie

authors： Farghaly AM,Habib NS,Khalil MA,el-Sayed OA,Bistawroos AE

更新日期：1990-04-01 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：:Fourteen new 1-[(N, N-disubstituted thiocarbamoylthio)acetyl]-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives (7a-n) were synthesised by reacting 1-(chloroacetyl)-3-(2-thienyl)-5-aryl-2-pyrazolines (5a-g) and appropriate sodium salts of N, N-disubstituted dithiocarbamoic acids (6a, b). The structures of the synthesised ...

journal_title：Archiv der Pharmazie

authors： Turan-Zitouni G,Ozdemir A,Güven K

更新日期：2005-03-01 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

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：:A series of potent HIV-protease inhibitors has been prepared. Several of the newly synthesized compounds showed high plasma even after oral administration to animals. Based on the overall biological profile, CGP 61755 was chosen for further preclinical evaluation. For this compound, a 10 step synthesis potentially sui...

journal_title：Archiv der Pharmazie

authors： Capraro HG,Bold G,Fässler A,Cozens R,Klimkait T,Lazdins J,Mestan J,Poncioni B,Rösel JL,Stover D,Lang M

更新日期：1996-06-01 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：:New resveratrol (trans-3,4',5-trihydroxystilbene) analogs were synthesized and screened for their in vitro cancer chemopreventive potential using various bioassays relevant for the prevention of carcinogenesis in humans: two assays to detect modulators of carcinogen metabolism (Cyp1A inhibition; determination of NAD(P...

journal_title：Archiv der Pharmazie

authors： Orsini F,Verotta L,Klimo K,Gerhäuser C

更新日期：2016-06-01 00:00:00

abstract：:Starting from the commercially available 6-methyl-2-pyridylamine (1) the pyrido[3,2-e][1,4]diazepine 14a was synthesized in 12 steps with 7% total yield. 14a, the N-methyl derivative 14b, the thiolactam 15a, the amidine 16, and the 1,2,4-triazole 17 were tested for anti-HIV-1-activity. None of the compounds tested pos...

journal_title：Archiv der Pharmazie

authors： Görlitzer K,Wilpert C,Rübsamen-Waigmann H,Suhartono H,Wang L,Immelmann A

更新日期：1995-03-01 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：:A series of dialkyl, dicycloalkyl, and diaryl ester analogues of nifedipine, in which the ortho-nitro phenyl group at position 4 is replaced by the 4-(5)-chloro-2-ethyl-5-(4)-imidazolyl substituent, were synthesized and evaluated as calcium channel antagonists using the high K+ contraction of guinea pig ileal longitud...

journal_title：Archiv der Pharmazie

authors： Davood A,Mansouri N,Rerza Dehpour A,Shafaroudi H,Alipour E,Shafiee A

更新日期：2006-06-01 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：: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：: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 objective of this work was to develop a liver-specific antihepato carcinoma agent. A series of 5-fluorouracil / cholic acid conjugates (5-FU-cholic acid conjugates) were prepared and tested for their chemical characteristics and bio-distribution properties. The in-vitro stability trial showed 5-FU-cholic acid conj...

journal_title：Archiv der Pharmazie

authors： Qian S,Wu JB,Wu XC,Li J,Wu Y

更新日期：2009-09-01 00:00:00