Benzimidazole-1,2,3-triazole hybrid molecules: synthesis and evaluation for antibacterial/antifungal activity.

abstract：:A series of benzamide derivatives possessing potent dopamine D2 , serotonin 5-HT1A , and 5-HT2A receptor properties were synthesized and evaluated as potential antipsychotics. Among them, 5-(4-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)butoxy)-N-cyclopropyl-2-fluorobenzamide (4k) held the best pharmacological profile....

journal_title：Archiv der Pharmazie

authors： Xu M,Guo S,Yang F,Wang Y,Wu C,Jiang X,Zhao Q,Chen W,Tian G,Zhu F,Xie Y,Hu T,Wang Z,He Y,Shen J

更新日期：2019-04-01 00:00:00

abstract：:Patient-derived cell transplantation is an attractive therapy for regenerative medicine. However, this requires effective strategies to reliably differentiate patient cells into clinically useful cell types. Herein, we report the discovery that 5-nitro-5'hydroxy-indirubin-3'oxime (5'-HNIO) is a novel inducer of cell t...

journal_title：Archiv der Pharmazie

authors： Jung DW,Hong YJ,Kim SY,Kim WH,Seo S,Lee JE,Shen H,Kim YC,Williams DR

更新日期：2014-11-01 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：: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：: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：:The photochemical stability of 2, 6, 6-trimethyl-3-carbmethoxy-4-phenyl-5-oxo-1, 4, 5, 6, 7, 8-hexahydroquinoline (HHQ) derivatives with different substituents on the phenyl ring (-Cl, -NO(2), -CF(3), -CH(3), -OCH(3)) has been studied.The process of photodegradation was studied by UV spectrophotometry. The rate of pho...

journal_title：Archiv der Pharmazie

authors： Mielcarek J,Safak C,Simsek R,Matloka A

更新日期：2002-05-01 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：:A series of new Mannich bases of N-[(4-arylpiperazin-1-yl)-methyl]-3-(chlorophenyl)-pyrrolidine-2,5-diones 10-23 have been synthesized and evaluated for their anticonvulsant activity in maximum electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure threshold tests. Their neurotoxicity was determined us...

journal_title：Archiv der Pharmazie

authors： Obniska J,Kopytko M,Zagórska A,Chlebek I,Kamiński K

更新日期：2010-06-01 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：:A series of oximes deriving from 5-arylidene-pyrrolidine-2,3,4-triones and pyridine-2,3,4-triones has been prepared. The presence of the tautomeric nitrosoenol was proven in solutions of alpha-ketooxime 7a. The binding affinity of the new oximes toward the N-methyl-D-aspartate (glycine site) receptor has been measured...

journal_title：Archiv der Pharmazie

authors： Poschenrieder H,Höfner G,Stachel HD

更新日期：1999-09-01 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：: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：:Inhibition of 5-lipoxygenase by anthralin (1) and 41 derivatives is determined: the acids 38 and 39, the lactones 40-42 and 9-anthrone (8) are the most potent inhibitors, the lactone 41 reaching the efficacy of nordihydroguaiaretic acid (NDGA). The results were correlated with the hydrophilic/lipophilic balance of the...

journal_title：Archiv der Pharmazie

authors： Tanzer H,Braun C,Seidel M,Wiegrebe W

更新日期：1991-11-01 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：:Previously, we demonstrated that certain heterocyclic compounds derived from 3-substituted-1,2,4-triazole-5-thiones had promising analgesic/anti-inflammatory activities together with low ulcerogenic properties. Therefore, we sought to design and synthesize new derivatives of triazol-5-thiones-fused heterocycles. In th...

journal_title：Archiv der Pharmazie

authors： Sert-Ozgur S,Tel BC,Somuncuoglu EI,Kazkayasi I,Ertan M,Tozkoparan B

更新日期：2017-07-01 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：:A series of new benzofuran/oxadiazole hybrids (8a-n) was synthesized from 2H-chromene-3-carbonitriles (3a-c) through the multistep synthetic methodology, and these hybrids are known to exhibit anticancer activities. All the compounds were evaluated for their in vitro cytotoxicity against the HCT116 and MIA PaCa2 cell ...

journal_title：Archiv der Pharmazie

authors： Mokenapelli S,Thalari G,Vadiyaala N,Yerrabelli JR,Irlapati VK,Gorityala N,Sagurthi SR,Chitneni PR

更新日期：2020-06-01 00:00:00

abstract：:The shock-induced serine protease HtrA1 is a potential regulator of human placenta development during pregnancy. The protein contains a functional PDZ domain that has been solved in complex with a phage display-derived heptapeptide: Asp-6 Ser-5 Arg-4 Ile-3 Trp-2 Trp-1 Val0 . In this study, a rationally designed haloge...

journal_title：Archiv der Pharmazie

authors： Dou SF,Liu H,Cao TM,Wen QL,Li J,Shao QC

更新日期：2016-04-01 00:00:00

abstract：:A new series of N,N'-(benzene-1,3-diyldi-1,3,4-oxadiazole-5,2-diyl)bis{2-[(5-benzene-1,3-diyl-1,3,4-oxadiazol-2-yl)amino]acetamide}(macrocycle 1), N,N'-(benzene-1,3-diyldi-1,3,4-thiadiazole-5,2-diyl)bis{2-[(5-benzene-1,3-diyl-1,3,4-thiadiazol-2-yl)amino]acetamide} (macrocycle 2) and S,S'-[benzene-1,3-diylbis(4H-1,2,4-...

journal_title：Archiv der Pharmazie

authors： Vinay Kumar B,Naik HS,Girija D,Sharath N,Sudeep HV,Joy Hoskeri H

更新日期：2012-03-01 00:00:00

abstract：:Michael-type reaction of compounds of type 9 were studied. Addition reactions with acrolein and methyl vinyl ketone, respectively, lead--depending on the conditions--to pyridoindoles of type 16 and 14 and/or to tetrahydrocarbazoles of type 17 and 15. With Triton B compounds 15 undergo retro-Michael-type elimination of...

journal_title：Archiv der Pharmazie

authors： Mahboobi S,Burgemeister T,Kastner F

更新日期：1995-01-01 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：: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：: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：:A general procedure for the preparation of 1,2,3-triazole analogs of nucleosides from diethyl 2-azidoethoxymethyl- and 2-azidoethoxyethylphosphonates was elaborated. The application of microwave irradiation shortened the reaction time to 10 min in comparison to ca. 48 h when 1,3-dipolar cycloadditions were performed u...

journal_title：Archiv der Pharmazie

authors： Głowacka IE,Balzarini J,Wróblewski AE

更新日期：2013-04-01 00:00:00

abstract：:This paper reports the synthesis of the new compound 1-[2-acetoxy-3-(4-phenyl-1-piperazinyl)propyl]pyrrolidin-2-one (Ac-MG-1). Preliminary pharmacological assessment revealed that Ac-MG-1 possesses anti-arrhythmic activity and a local anesthetic effect. The crystal structure of Ac-MG-1 was determined by X-ray diffract...

journal_title：Archiv der Pharmazie

authors： Malawska B,Filipek B,Stadnicka K,Ciechanowicz-Rutkowska M

更新日期：1995-06-01 00:00:00

abstract：:A series of 3,4-bis-chalcone-N-arylpyrazoles 3a-k was prepared from diacetyl pyrazoles 2a-e. The reaction of 2d and 2e with hydrazine hydrate gave pyrazolo[3,4-d]pyridazine derivatives 4a-b. Furthermore, the reaction of 2a-e with thiosemicarbazide afforded pyrazolo[3,4-d]pyridazine thiocyanate salts 5a-e. The synthesi...

journal_title：Archiv der Pharmazie

authors： El-Sabbagh OI,Mostafa S,Abdel-Aziz HA,Ibrahim HS,Elaasser MM

更新日期：2013-09-01 00:00:00

abstract：:The synthesis of 4-Methoxyphenyl-[5-methyl-6-(2-(4-morpholinyl)-ethyl)-6H-thieno[2,3- b]pyrrol-4-yl)phenylmethanone (1), a thiophene analogue of the analgesic Pravadoline B, is described. Starting with the acetylprotected thienylhydrazine 2b compound 7 was obtained in a Fischer-analogue cyclication in two steps. Use o...

journal_title：Archiv der Pharmazie

authors： Binder D,Schnait H,Rovenszky F,Enzenhofer R,Stroissnig H

更新日期：1991-04-01 00:00:00

abstract：:New condensed derivatives of anpirtoline, in which the pyridine ring is replaced with quinoline, quinazoline, 7-chloroquinoline, and 7-chloroquinazoline nuclei, have been synthesized. Their receptor binding profiles (5-HT1A, 5-HT1B) and analgesic activity (hot plate, acetic acid induced writhing) have been studied. Th...

journal_title：Archiv der Pharmazie

authors： Rádl S,Hezky P,Proska J,Krejcí I

更新日期：2000-11-01 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

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