Synthesis and biological evaluation of some 2,4,5-trisubstituted thiazole derivatives as potential antimicrobial and anticancer agents.

abstract：:Furfurylidenemalononitriles and thienylidenemalononitriles were treated with 1,3-cyclohexanediones to afford 2-amino-4-hetaryl-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile derivatives. The molluscicidal activity of these compounds was investigated. ...

journal_title：Archiv der Pharmazie

authors： Abdelrazek FM,Metz P,Farrag EK

更新日期：2004-09-01 00:00:00

abstract：:The synthesis and biological evaluation of oximes of 2-aryl-6-methoxy-3,4-dihydronaphthalene (7a, 7b, 14a, 14b) as nonsteroidal inhibitors of 17 alpha-hydroxylase-C17,20-lyase (P450 17, CYP 17) is described. The target compounds were synthesized and identified by 1H NMR and MS. The preparation of the key intermediates...

journal_title：Archiv der Pharmazie

authors： Zhuang Y,Hartmann RW

更新日期：1998-01-01 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：: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

authors： Farghaly TA,Mahmoud HK

更新日期：2013-05-01 00:00:00

abstract：:(2S,3R)-3,7-Diamino-2-hydroxy-heptanoyl-Leu-Pro-OH [(2S,3R)-DAHHA-Leu-Pro-OH, 4], analogue of the N-terminal tripeptide of probestin, has been synthesized, and tested as inhibitor of AP-B, Leu-AP, AP-M, and enkephalin-degrading APs, and as analgesic. In order to establish structure-activity relationships the dipeptide...

journal_title：Archiv der Pharmazie

authors： Herranz R,Vinuesa S,Pérez C,García-López MT,De Ceballos ML,Murillo FM,del Río J

更新日期：1992-08-01 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：: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：: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：: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

authors： Miller MC 3rd,Bastow KF,Stineman CN,Vance JR,Song SC,West DX,Hall IH

更新日期：1998-04-01 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：: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 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：: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：:The newly synthesized analogs of NAN-190 containing m-Cl and m-CF(3) substituents in the arylpiperazine moiety and their conformationally restricted counterparts showed a very high 5-HT(1A )receptor affinity. In the LLR test, the flexible compounds 4a and 5a displayed features of a partial agonist and agonist, respect...

journal_title：Archiv der Pharmazie

authors： Paluchowska MH,Bugno R,Charakchieva-Minol S,Bojarski AJ,Tatarczyńska E,Chojnacka-Wójcik E

更新日期：2006-09-01 00:00:00

abstract：:Schistosoma mansoni histone deacetylase 8 (SmHDAC8) has been recently identified as a new potential target for the treatment of schistosomiasis. A series of newly designed and synthesized alkoxyamide-based and hydrazide-based HDAC inhibitors were tested for inhibitory activity against SmHDAC8 and human HDACs 1, 6, and...

journal_title：Archiv der Pharmazie

authors： Stenzel K,Chakrabarti A,Melesina J,Hansen FK,Lancelot J,Herkenhöhner S,Lungerich B,Marek M,Romier C,Pierce RJ,Sippl W,Jung M,Kurz T

更新日期：2017-08-01 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：: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

authors： Pomarnacka E,Kornicka A,Kuchnio A,Heinrichs M,Grünert R,Gdaniec M,Bednarski PJ

更新日期：2011-07-01 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

authors： Trujillo J,Granados-Castro LF,Zazueta C,Andérica-Romero AC,Chirino YI,Pedraza-Chaverrí J

更新日期：2014-12-01 00:00:00

abstract：:In this study, we have explored the prevention of gastric side effects such as gastric lesions and bleeding while maintaining the high analgesic and anti-inflammatory activities by the derivatization of the carboxylate moiety into amides in [5-chloro-6-(2-chloro/fluorobenzoyl)-2-benzoxazolinone-3-yl]acetic acids. We h...

journal_title：Archiv der Pharmazie

authors： Banoglu E,Okçelik B,Kupeli E,Unlü S,Yeşilada E,Amat M,Caturla JF,Sahin MF

更新日期：2003-07-01 00:00:00

abstract：:Ten pyrazole derivatives were synthesized and evaluated for their ability to inhibit the replication of influenza virions. All the compounds were synthesized in good-to-excellent yield, and the structures were ascertained with the help of (1) H NMR, (13) C NMR, mass, and elemental analysis. Among the tested series, co...

journal_title：Archiv der Pharmazie

authors： Meng FJ,Sun T,Dong WZ,Li MH,Tuo ZZ

更新日期：2016-03-01 00:00:00

abstract：:Novel C-5 substituted 6,2'-anhydrouridines 5a-e are synthesized from the hitherto unknown monosubstituted ribofuranosylbarbituric acid derivatives 4a-e. These molecules are high-anti-fixed by a 6,2'-linkage and were assumed to show antiviral and antineoplastic effects. In cell culture test systems, however, none of th...

journal_title：Archiv der Pharmazie

authors： Folkers G,Junginger G,Müller CE,Schloz U,Eger K

更新日期：1989-02-01 00:00:00

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 derivati...

journal_title：Archiv der Pharmazie

authors： el-Feky SA,Abd el-Samii ZK

更新日期：1991-06-01 00:00:00

abstract：:A series of novel 2,4-disubstituted 7-methyl-1,1,3-trioxo-2,4-dihydro-pyrazolo[4,5-e] [1,2,4]thiadiazines (PTDs) was synthesized, structurally confirmed by spectral analysis, and evaluated for their anti-HIV activities by inhibition of HIV-induced cytopathogenicity in MT-4 cell culture. The results showed that some co...

journal_title：Archiv der Pharmazie

authors： Liu XY,Yan RZ,Wang Y,Zhan P,De Clercq E,Pannecouque C,Witvrouw M,Molina MT,Vega S

更新日期：2008-04-01 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

authors： Iqbal N,Knaus EE

更新日期：1996-01-01 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：: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

authors： Berger ML,Schödl C,Noe CR

更新日期：1996-03-01 00:00:00

abstract：:MXT-M-3,2 breast cancer implanted into female B6D2F1 mice accelerates the growth of an identical second tumor. This process is accompanied by a significant increase of the granulocyte and monocyte numbers in the blood and of the granulocyte and macrophage numbers in the spleen. A significant positive correlation of st...

journal_title：Archiv der Pharmazie

authors： Schlemmer R,Spruss T,Bernhardt G,Schönenberger H

更新日期：2000-12-01 00:00:00

abstract：:The influence of RE 1492 on the storage of red blood cells (RBCs) was investigated. RE 1492 (c > or = 50 mumol/L) induces the formation of cup cells and hence delays the appearance of echinocytes and crenated spheres in the blood. A concentration of 50 mumol/L RE 1492 drops hemolysis by 50%. At this concentration afte...

journal_title：Archiv der Pharmazie

authors： Rehse K,Müller S

更新日期：1995-04-01 00:00:00

abstract：:The histone deacetylase (HDAC) enzyme plays an important role in gene transcription. Inhibitors of histone deacetylases induce cell differentiation and suppress cell proliferation in tumor cells. Hydroxamates with rigid linker have displayed better inhibition profiles than those with linear and flexible aliphatic link...

journal_title：Archiv der Pharmazie

authors： Chakrabarty S,Jasmine,Bhadaliya C,Sinha BN,Mahesh A,Bai H,Blond SY,Jayaprakash V

更新日期：2010-03-01 00:00:00

abstract：:Some new N-[6-indazolyl]arylsulfonamides and N-[alkoxy-6-indazolyl]arylsulfonamides were prepared by the reduction of 2-alkyl-6-nitroindazoles with SnCl2 in different alcohols, followed by coupling the corresponding amine with arylsulfonyl chlorides in pyridine. The newly synthesized compounds were evaluated for their...

journal_title：Archiv der Pharmazie

authors： Abbassi N,Rakib el M,Chicha H,Bouissane L,Hannioui A,Aiello C,Gangemi R,Castagnola P,Rosano C,Viale M

更新日期：2014-06-01 00:00:00