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 and Pseudomonas aeruginosa. The interplanar angle (theta) between the aryl ring and the adjacent azomethine group of some representative compounds was measured by electronic absorption spectroscopy. No structure-activity-relationship between interplanar angle or lipophily and activity was found.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Cesur Z,Büyüktimkin S,Büyüktimkin N,Derbentli Sdoi
10.1002/ardp.19903230304subject
Has Abstractpub_date
1990-03-01 00:00:00pages
141-4issue
3eissn
0365-6233issn
1521-4184journal_volume
323pub_type
杂志文章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
pub_type: 杂志文章
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更新日期:1995-06-01 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
pub_type: 杂志文章
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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
pub_type: 杂志文章
doi:10.1002/ardp.201600313
更新日期:2017-02-01 00:00:00
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journal_title:Archiv der Pharmazie
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更新日期:2020-11-23 00:00:00
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
pub_type: 杂志文章
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更新日期:2013-09-01 00:00:00
abstract::Nine novel acyl thioureas were synthesized. Their identities and purities were confirmed by LC-MS spectra; each structure was elucidated by elemental analysis, IR, 1 Н and 13 C NMR spectra. Applying an in vitro screening of their antifungal potential, three substances (3, 5, and 6) could be selected as showing high ac...
journal_title:Archiv der Pharmazie
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abstract::Herein, we report the synthesis of novel tetrahydro-β-carbolines that induce cell death via the autophagic pathway. Five of the new compounds induced cell death in a panel of patient-derived human metastatic melanoma cells. The autophagic pathway was confirmed using LC3 autophagosome markers; the involvement of ATG7 a...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.201300437
更新日期:2014-06-01 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
pub_type: 杂志文章
doi:10.1002/ardp.19953280304
更新日期:1995-03-01 00:00:00
abstract::The 5-desoxy analogue of BW245C, imidazolidin-2-one 3, has been synthesized by reduction of the N-benzyl hydantoin derivative 6. Compound 3 was found to be approximately equipotent with BW245C as an inhibitor of platelet aggregation and this result indicates that the 5-keto group of BW245C is not essential for platele...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.2503240802
更新日期:1991-08-01 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
pub_type: 杂志文章
doi:10.1002/ardp.19903230802
更新日期:1990-08-01 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
pub_type: 杂志文章
doi:10.1002/ardp.19963290303
更新日期:1996-03-01 00:00:00
abstract::Curcumin, a phenolic compound extracted from Curcuma longa, is commonly used in Asia as a spice and pigment and has several biological functions, particularly antioxidant properties. It has been reported that curcumin exhibits bifunctional antioxidant properties related to its capability to react directly with reactiv...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章,评审
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更新日期:2014-12-01 00:00:00
abstract::An overview of the rhodopsin crystal structure provides a structural basis for understanding the structures and functions of other G-protein coupled receptors (GPCRs). All of the structural details observed to date for rhodopsin will not necessarily carry over to other GPCRs, but major features such as the arrangement...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章,评审
doi:10.1002/ardp.200400995
更新日期:2005-06-01 00:00:00
abstract::A new series of 16 6-chloro-1,1-dioxo-7-{4-[(4-R(1)-phenyl)imino]-4H-3,1-benzoxazin-2-yl}-3-(substituted amino)-1,4,2-benzodithiazines 7-22 was prepared in order to evaluate the cytotoxic activity against six human cancer cell lines. The structures of the new compounds were confirmed by IR, (1)H-, and (13)C-NMR, eleme...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.201000183
更新日期:2011-07-01 00:00:00
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/1521-4184(200109)334:8/9<291::aid-ardp291>
更新日期:2001-09-01 00:00:00
abstract::In an attempt to find a new class of antibacterial agents, we have synthesized thirty new coumarin (2H-benzopyran-2-one) analogues. These derivatives include substituted azetidin-2-ones (beta-lactam) 3a-f, pyrrolidin-2-ones 4a-f, 2H-1,3,4-oxadiazoles 5a-f, and thiazolidin-4-ones 6a-f attached to 4-phenyl-2H-benzopyran...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.200700266
更新日期:2008-11-01 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
pub_type: 杂志文章
doi:10.1002/ardp.19963290105
更新日期:1996-01-01 00:00:00
abstract::With the purpose of expanding the structural variety of chemical compounds available as pharmacological tools for the treatment of Alzheimer's disease, we synthesized and evaluated a novel series of indole-benzoxazinones (Family I) and benzoxazine-arylpiperazine derivatives (Family II) for potential human acetylcholin...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.201800024
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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
pub_type: 杂志文章
doi:10.1002/ardp.201300262
更新日期:2013-12-01 00:00:00
abstract::Several 2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-benzimidazole-5-carboxamidine analogues were synthesized for their antibacterial and antifungal activities against S. aureus, Methicillin-resistant S. aureus (MRSA), C. albicans, and C. krusei. MIC values of the targeted compounds 43-58 are comparabl...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.200500168
更新日期:2006-02-01 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
pub_type: 杂志文章
doi:10.1002/ardp.201600022
更新日期:2016-06-01 00:00:00
abstract::Novel 6,11-dioxo-6,11-dihydro-benzo[f]pyrido[1,2-a]indole-12-carboxamide derivatives and the corresponding 7,10-dihydroxy analogues were designed in accordance with Moore's and Pindur's theory and synthesized based on the structural similarity with known antitumour agents such as ellipticine, daunorubicin, mitoxantron...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.200600160
更新日期:2007-03-01 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
pub_type: 杂志文章
doi:10.1002/ardp.19963290805
更新日期:1996-08-01 00:00:00
abstract::The synthesis of a novel library of purine derivatives bearing various bicyclic and polycylic substituents at the N-9 position is described. The series includes norbornanes, bicyclo[2.2.2]octanes, and bicyclo[3.2.1]octanes attached at the bridgehead position as well as bicyclo[3.1.1]heptanes, tetrahydro-1-naphthalenes...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.201300431
更新日期:2014-07-01 00:00:00
abstract::In this study, the synthesis of a new series of 3,6-disubstituted-7H-1,2,4-triazolo[3,4-b][1,3,4]thiadiazine 1a-4c compounds derived from 4-amino-3-substituted-1,2,4-triazole-5-thiones 1-4 is described. All of the synthesized compounds were screened for their possible analgesic / anti-inflammatory, antioxidant activit...
journal_title:Archiv der Pharmazie
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更新日期:2009-05-01 00:00:00
abstract::Poly(vinyl alcohol) was crosslinked with ethylene glycol diglycidyl ether to obtain hydrogel-forming polymers. The polymers were also substituted with oleoyl chloride, providing hydrogels with weak solubility. These new polymeric materials were evaluated for the formulation of sustained drug delivery systems. Vancomyc...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/1521-4184(200203)335:2/3<89::AID-ARDP89>3.
更新日期:2002-03-01 00:00:00
abstract::We report on the synthesis and biological evaluation of two series of 2,4,5-polysubstituted thiazoles comprising the acid hydrazide functionality and some derived pharmacophores known to contribute to various chemotherapeutic activities. All newly synthesized compounds were subjected to in-vitro antibacterial and anti...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.200800026
更新日期:2008-07-01 00:00:00
abstract::A series of homochiral 7-substituted 1-aminoindans was prepared by means of asymmetric reductive amination from racemic 7-substituted 1-indanones via E-imines and E-imine/enamine mixtures, respectively, and subjected to 5-hydroxytryptamine (5-HT) receptor subtype binding studies. The ee's of the title compounds were d...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/(sici)1521-4184(199802)331:2<59::aid-ardp5
更新日期:1998-02-01 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
pub_type: 杂志文章
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更新日期:2009-11-01 00:00:00
abstract::New, non-imidazole histamine H3 receptor antagonists were prepared and in vitro tested as H3 receptor antagonists measured as the electrically evoked contraction of the guinea-pig jejunum. The 2-(1-piperidinyl)- and 2-(1-pyrrolidinyl)benzothiazoles show no or very poor activity; 2-[1-(4-amino)piperidinyl]- and 2-(1,2-...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/(sici)1521-4184(199911)332:11<389::aid-ard
更新日期:1999-11-01 00:00:00