Abstract:
:Diverse biological activities have been found in compounds having a quinazolinone ring system. A large number of 4(3H)-quinazolinones, in particular those possessing 2-alkyl-3-aryl, 2,3-dialkyl, and 2-alkyl-3-amino substitution, have been evaluated for pharmacological activity. On the other hand, thiazolidone derivatives are reported to have anesthetic, anticonvulsant, and hypnotic activity.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
el-Feky SA,Abd el-Samii ZKdoi
10.1002/ardp.19913240613subject
Has Abstractpub_date
1991-06-01 00:00:00pages
381-3issue
6eissn
0365-6233issn
1521-4184journal_volume
324pub_type
杂志文章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
pub_type: 杂志文章
doi:10.1002/ardp.200400917
更新日期:2004-12-01 00:00:00
abstract::1-Acetylcarbazoles are readily converted to 3-desazacanthin-4-ones upon treatment with Bredereck's reagent, but in contrast to canthin-4-ones, these do not undergo ring transformation reactions with guanidine. Only after N-protection (methyl or 2-(trimethylsilyl)ethoxymethyl group), 2-desaza analogues of the alkaloid ...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.201400328
更新日期:2015-02-01 00:00:00
abstract::Rapamycin is an mTOR allosteric inhibitor with multiple functions such as immunosuppressive, anticancer, and lifespan prolonging activities. Its C-43 semi-synthetic derivatives temsirolimus and everolimus have been used as mTOR targeting anticancer drugs in the clinic. Following our previous research on antitumor rapa...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.201800123
更新日期:2018-11-01 00:00:00
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.201500342
更新日期:2016-03-01 00:00:00
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/1521-4184(200012)333:12<404::aid-ardp404>3
更新日期:2000-12-01 00:00:00
abstract::The aim of our study was to investigate structure activity relationship following the replacement of the 6-phenyl substituent at the 6,7-diaryl-2,3-dihydropyrrolizine template by various heteroaromatic residues. In this context we developed a new, efficient, and highly sensitive test method for the screening of dual c...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.19973300908
更新日期:1997-10-01 00:00:00
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.200700007
更新日期:2007-07-01 00:00:00
abstract::A series of 1H,3H-thiazolo[3,4-a]benzimidazoles were synthesized and tested for their in vitro antitumour activity against 60 human tumour cell lines. Some derivatives exhibited both tumour growth inhibition activity and cellular selectivity. In particular, compound 8c, the most active of the series, was very active t...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/1521-4184(200106)334:6<203::aid-ardp203>3.
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abstract::1-deoxy-D-xylulose-5-phosphate reductoisomerase (Dxr) represents an essential enzyme of the mevalonate-independent pathway of the isoprenoid biosynthesis. Using fosmidomycin as a specific inhibitor of Dxr, this enzyme was previously validated as target for the treatment of malaria and bacterial infections. The replace...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.200700149
更新日期:2007-09-01 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
pub_type: 杂志文章
doi:10.1002/ardp.200400935
更新日期:2005-03-01 00:00:00
abstract::We describe the synthesis and positive inotropic evaluation of a series of 2-(4-substitutedbenzyl-1,4-diazepan-1-yl)-N-(4,5-dihydro-1-phenyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamides by measuring left atrial stroke volume in preparations of isolated rabbit-heart. Several compounds were developed from, and showed ...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.201000032
更新日期:2010-11-01 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
pub_type: 杂志文章
doi:10.1002/ardp.19903230304
更新日期:1990-03-01 00:00:00
abstract::The pyrrolidino enaminones, with the carboxylic acid chain fixed at the nitrogen, inhibit cyclooxygenase more potently or selectively than 5-lipoxygenase. According to the structure-activity relationships discussed the potency depends significantly on the chain length of the carboxylic acid, the substitution pattern o...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.19973300307
更新日期:1997-03-01 00:00:00
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/(sici)1521-4184(200002)333:2/3<63::aid-ard
更新日期:2000-03-01 00:00:00
abstract::Three ketomethylene pseudodideptide analogues [(S)Lys psi(COCH2)(R and S)Phe (14 or 15 and 15 or 14) and (S)Lys psi(COCH2)(xi Trp (19)] of natural arphamenine A [(S)Arg psi(COCH2(R,S)Phe (1)] were easily prepared by a route involving two successive main reactions: a malonic ester alkylation with Z-protected lysine iod...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.19923250103
更新日期:1992-01-01 00:00:00
abstract::New series of perimidine derivatives and fused perimidines were derived from the reaction of ketene aminals 1 and 2 with diazotized anilines or hydrazonoyl chlorides. In addition, 8,10-disubstituted-[1,2,4]triazolo[4,3-a]perimidines (20a-m) were prepared through the reaction of perimidine-2-thione (15) with hydrazonoy...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.201200486
更新日期:2013-05-01 00:00:00
abstract::2-Acetyl-(6-picolyl)-4N-substituted thiosemicarbazones and their copper(II) complexes were shown to be potent antineoplastic and cytotoxic agents against murine and human cultured cells. Numerous derivatives were as active against solid tumor growth as clinically useful agents. The agents inhibited L1210 DNA and RNA s...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/(sici)1521-4184(199804)331:4<121::aid-ardp
更新日期:1998-04-01 00:00:00
abstract::We report in this work the synthesis, cytotoxicity, and antimicrobial activity of ([1,2,4]triazolo[1,5-c]quinazolin-2-ylthio)carboxylic acid amides 4-7 in connection with our previous research in the preparation of triazoloquinazoline derivatives. Due to simplicity, general availability of starting materials, and high...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.200900077
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
pub_type: 杂志文章
doi:10.1002/ardp.201200421
更新日期:2013-04-01 00:00:00
abstract::Viral gastroenteritis is a serious viral infection which affects a large number of individuals around the world, most of them being children. The infection may occur due to different viruses, for example, coxsackievirus, adenovirus, and rotavirus. There is no available cure for such infections, and the treatment mainl...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.201400387
更新日期:2015-03-01 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
更新日期:2018-05-01 00:00:00
abstract::A novel series of hybrid molecules 4a-i and 5a-i were prepared by condensation of 4-(trimethylsilylethynyl)benzaldehyde 1 with substituted o-phenylenediamines. These in turn were reacted with 2-(azidomethoxy)ethyl acetate in a Cu alkyne-azide cycloaddition (CuAAC) to generate the 1,2,3-triazole pharmacophore under mic...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.201400142
更新日期:2014-10-01 00:00:00
abstract::Paullones 3 and 4 with aminoalkyl side chains in 2- or 3-position were synthesized as derivatives of kenpaullone 1. Both 3 and 4 showed the characteristic CDK1-inhibitory activity of the paullones and a modest antiproliferative activity on cultured human tumor cell lines. Hence, 3 and 4 appear to be suitable tools for...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/1521-4184(200209)335:7<311::AID-ARDP311>3.
更新日期:2002-07-01 00:00:00
abstract::In continuation of our effort aimed towards the development of novel aldose reductase inhibitors, several phenylacetic acids bearing an alkoxy substituent in position 3 or 4, respectively, were prepared and screened. The latter represent formal ring opening products of the cyclohexylmethyloxyphenylacetic acids IIa and...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.200600054
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.200900065
更新日期:2009-12-01 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
pub_type: 杂志文章
doi:10.1002/ardp.201300262
更新日期:2013-12-01 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
pub_type: 杂志文章
doi:10.1002/ardp.202000137
更新日期:2020-11-01 00:00:00
abstract::6-(1-Acyloxyalkyl)-5,8-dimethoxy-1,4-naphthoquinone (DMNQ; 5,8-dimethoxy-1,4-naphthoquinone) derivatives were synthesized and examined for their inhibitory effect on DNA topoisomerase-I (Topo I) and their antiproliferative activity against L1210 cells. The Topo-I inhibitory effect of 6-(1-hydroxyalkyl)-DMNQ derivative...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/1521-4184(200110)334:10<318::aid-ardp318>3
更新日期:2001-10-01 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
pub_type: 杂志文章
doi:10.1002/ardp.201600369
更新日期:2017-08-01 00:00:00
abstract::A number of phenylamides of 5-benzamidopyrazole-4-carboxylic acid were prepared in 50-80% yields from 1-phenyl (or methyl)-6-phenylpyrazolo[3,4-d]1,3-oxazin-4(1H)-ones and aniline derivatives. All the compounds were tested for their analgesic and antiinflammatory activities, as well as for their ulcerogenic potential ...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/1521-4184(200105)334:5<153::aid-ardp153>3.
更新日期:2001-05-01 00:00:00