Synthesis of some 1-[(N, N-disubstituted thiocar bamoylthio)acetyl]-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives and investigation of their antibacterial and antifungal activities.

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

authors： Büch HP,Krug R,Knabe J

更新日期：1996-08-01 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：:Several chloro- and iodo-lignanolides have been obtained by direct halogenation of aromatic rings from yatein and 4'-O-demethylyatein. They were assayed as antineoplastics, in order to check the influence in the activity of substitution in both aromatic rings. Although these compounds show a modest antineoplastic acti...

journal_title：Archiv der Pharmazie

authors： Medarde M,Peláez-Lamamié de Clairac R,López JL,Grávalos DG,San Feliciano S

更新日期：1995-09-01 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：:The antioxidant and acetylcholinesterase inhibitory properties of novel symmetric sulfamides derived from phenethylamines were evaluated. Phenethylamines 8-11 were reacted with SO2Cl2 in the presence of Et3N to afford sulfamides in good yields. The synthesized sulfamides were converted to their phenolic derivatives wi...

journal_title：Archiv der Pharmazie

authors： Aksu K,Topal F,Gulcin İ,Tümer F,Göksu S

更新日期：2015-06-01 00:00:00

abstract：:Two new arylnaphthalide lignans, procumphthalide A (1) and 4-O-beta-D-glucopyranosyl-(1"'-->2")-beta-D-apiofuranosyldiphyllin, named procumbenoside B (2), along with cilinaphthalide B (3) and several other known compounds were isolated from the methanolic extracts of Justicia procumbens. By using NMR and other spectra...

journal_title：Archiv der Pharmazie

authors： Weng JR,Ko HH,Yeh TL,Lin HC,Lin CN

更新日期：2004-04-01 00:00:00

abstract：:In an attempt to counteract bacterial pathogenicity, a set of novel imidazolidine-2,4-dione and 2-thioxoimidazolidin-4-one derivatives was synthesized and evaluated as inhibitors of bacterial virulence. The new compounds were characterized and screened for their effects on the expression of virulence factors of Pseudo...

journal_title：Archiv der Pharmazie

authors： Mohamed B,Abdel-Samii ZK,Abdel-Aal EH,Abbas HA,Shaldam MA,Ghanim AM

更新日期：2020-05-01 00:00:00

abstract：:The marine fatty acid (+/-)-2-methoxytetradecanoic acid was synthesized in two steps (71% overall yield) starting from commercially available methyl-2-hydroxy-tetradecanoate. The title compound was antifungal against Candida albicans (ATCC 14053) in RPMI medium and Aspergillus niger (ATCC 16404) and Cryptococcus neofo...

journal_title：Archiv der Pharmazie

authors： Carballeira NM,Ortiz D,Parang K,Sardari S

更新日期：2004-03-01 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 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

authors： Dannhardt G,Bauer A,Nowe U

更新日期：1997-03-01 00:00:00

abstract：:Synthesis of a new series of 1beta-methylcarbapenems with a substituted oxadiazolopyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of the substituent on the oxadiazole ring investigated. In particular, compounds 13...

journal_title：Archiv der Pharmazie

authors： Oh CH,Dong HG,Lee JS,Lee SC,Hong JH,Cho JH

更新日期：2003-12-01 00:00:00

abstract：:In accordance with the significant impetus of the discovery of potent vascular endothelial growth factor receptor 2 (VEGFR-2) inhibitors, herein, we report the design, synthesis, and anticancer evaluation of 12 new N-substituted-4-phenylphthalazin-1-amine derivatives against HepG2, HCT-116, and MCF-7 cells as VEGFR-2 ...

journal_title：Archiv der Pharmazie

authors： El-Adl K,Ibrahim MK,Khedr F,Abulkhair HS,Eissa IH

更新日期：2020-11-16 00:00:00

abstract：:3-Amino-1,4-benzodiazepines as well as chemically related diverse amines were prepared from oxazepam and subsequently screened on the cholecystokinin receptor in a radiolabel binding assay. Oxazepam 2 was activated via its 3-chloro-1,4-benzodiazepine intermediate 3 and was reacted with a large series of aliphatic and ...

journal_title：Archiv der Pharmazie

authors： Offel M,Lattmann P,Singh H,Billington DC,Bunprakob Y,Sattayasai J,Lattmann E

更新日期：2006-04-01 00:00:00

abstract：:New 5-(2-arylethenyl)-1, 2, 4-triazine N-oxide and N, N'-dioxide derivatives were synthesized in order to obtain compounds as selective hypoxic cell cytotoxins. The desired products were obtained when the 5-methyl heterocycle reacted with the corresponding iminium electrophiles. The new compounds were tested for their...

journal_title：Archiv der Pharmazie

authors： Cerecetto H,González M,Risso M,Saenz P,Olea-Azar C,Bruno AM,Azqueta A,De Ceráin AL,Monge A

更新日期：2004-05-01 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

authors： Kahveci B,Yılmaz F,Menteşe E,Ülker S

更新日期：2017-08-01 00:00:00

abstract：:New analogues of nifedipine, in which the 2-nitrophenyl group at position 4 is replaced by a 1-methyl-5-nitro-2-imidazolyl substituent, were synthesized. The symmetrical dialkyl 1, 4-dihydro-2, 6-dimethyl-4-(1-methyl-5-nitro-2-imidazolyl)-3, 5-pyridinedicarboxylates were prepared by a classical Hantzsch condensation. ...

journal_title：Archiv der Pharmazie

authors： Miri R,Javidnia K,Kebriaie-Zadeh A,Niknahad H,Shaygani N,Semnanian S,Shafiee A

更新日期：2003-09-01 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：:Starting from substituted 9-chloroacridines, a series of quinacrine and spacered dimeric acridine compounds was prepared. Their ability to interrupt the protein association of prion- and Alzheimer-specific proteins and Ab peptides was explored using a fast screening system based on FACS analysis. The bis-acridines dis...

journal_title：Archiv der Pharmazie

authors： Csuk R,Barthel A,Raschke C,Kluge R,Ströhl D,Trieschmann L,Böhm G

更新日期：2009-12-01 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：:Synthesis of some new derivatives of 2-aryl-4-oxo-1-(4-quinazolyl)quinazolines is described. Methyl N-(4-quinazolyl)anthranilate was allowed to react with phenyl iso(thio)cyanate to give 3-phenyl-1-(4-quinazolyl)-1, 2, 3, 4-tetrahydro-2, 4-dioxo- and 4-oxo-2-thioxoquinazolines (3a and 3b respectively) Alternatively, a...

journal_title：Archiv der Pharmazie

authors： Gineinah MM,El-Sherbeny MA,Nasr MN,Maarouf AR

更新日期：2002-01-01 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：:2- or 6-(1-Hydroxyiminoalkyl)-5,8-dimethoxy-1,4-naphthoquin-one (DMNQ) and 6-(1-propyloxyimino- alkyl)-DMNQ derivatives were synthesized, and their inhibitory effects on DNA topoisomerase-I (TOPO-I) and antiproliferative activities against L1210 cells were examined. In a comparison, it was found that 6-(1-hydroxyimino...

journal_title：Archiv der Pharmazie

authors： Song GY,Kim Y,You YJ,Cho H,Kim SH,Sok DE,Ahn BZ

更新日期：2000-04-01 00:00:00

abstract：:The key step in the synthesis of the pharmacologically interesting 1-phenyltetrahydro-3-benzazepine skeleton is the Michael addition of (2-lithiophenyl)acetaldehyde acetals, which are generated in situ upon treatment of the bromo acetals 5a,b with n-butyllithium, to beta-nitrostyrene (6). The reductive ring closure of...

journal_title：Archiv der Pharmazie

authors： Wünsch B,Nerdinger S,Bauschke G,Höfner G

更新日期：1997-07-01 00:00:00

abstract：:As per structural requirement essential for anticonvulsant activity, a series of new 6-(2-amino-substituted phenyl)-4-(substituted phenyl)-1,2,4-triazine-3,5-dione derivatives were designed and synthesized. All the synthesized title derivatives were assessed for in vivo anticonvulsant screening by the two most employe...

journal_title：Archiv der Pharmazie

authors： Khan AA,Siddiqui N,Akhtar MJ,Ali Z,Yar MS

更新日期：2016-04-01 00:00:00

abstract：:Cycloaddition reactions of the nitrilimines 4-6 with N-arylmaleimides 7 and acrylamide (11) yield the pyrrolopyrazole derivatives 8-10 and 2-pyrazolines 12, respectively, in excellent yield. The regioselectivity and biological activities of some of the new compounds were investigated. ...

journal_title：Archiv der Pharmazie

authors： Ead HA,Hassaneen HM,Abdallah MA,Mousa HA

更新日期：1991-01-01 00:00:00

abstract：:Phosphono-analogues of glutathione containing the O = P(OR)2 moiety in place of the cysteinyl residue CH2SH 1a-1d were prepared by solution phase peptide synthesis. Benzyl, benzyloxy-carbonyl, and tert-butyl protecting groups were used to mask the individual amino acid functional groups. The formation of peptide bonds...

journal_title：Archiv der Pharmazie

authors： Kunze T

更新日期：1996-11-01 00:00:00

abstract：:Schiff base transition metal complexes are an important class of compounds with great potential for therapeutic interventions. However, data on antileukemic and antilymphoma effects of these complexes are limited. The activity of N,N'-bis(salicylidene)-1,2-phenylenediamine (salophene, 1), its iron(II/III) and manganes...

journal_title：Archiv der Pharmazie

authors： Hille A,Wolf T,Schumacher P,Ott I,Gust R,Kircher B

更新日期：2011-04-01 00:00:00

abstract：:Reaction of K2PtCl4 with the substituted 2-aminomethylpyridines 9, 14, and 22 affords the corresponding dichloroplatinum(II) complexes 3-5. Compounds 3 and 22 show remarkable relative binding affinities for the estrogen receptor. Towards the hormone-independent P388-tumor of the CD2F1-mouse the platinum(II) complexes ...

journal_title：Archiv der Pharmazie

authors： Brunner H,Nerl G,von Angerer E,Knebel N

更新日期：1991-10-01 00:00:00

abstract：:In this study, some novel cyanine dyes, 1, 3, and 5-15, were synthesized by a one-pot step reaction of pyridinium salts 2 and/or 4 with benzenaminium salt 1. N-{[1-Chloro-3,4-dihydronaphthalen-2-yl)methylene]benzenaminium} chloride 1 was obtained by the reaction of α-tetralone with Vilsmeier-Haack reagent, followed by...

journal_title：Archiv der Pharmazie

authors： Fadda AA,Tawfik EH,Abdel-Motaal M,Selim YA

更新日期：2020-11-10 00:00:00

abstract：:Pyrrolo[3,4-c]-beta-carbolinedione dimers 5-14 were synthesized from furo[3,4-c]-beta-carbolinediones and diamines by solvent-free TaCl5/silica catalyzed reaction under microwave irradiation. The inhibitory property of these target compounds, the starting materials 2, 31, 32, and the N-alkylated pyrrolo[3,4-c]-beta-ca...

journal_title：Archiv der Pharmazie

authors： Mahboobi S,Eluwa S,Kumar S,Koller M,Störl K

更新日期：1999-07-01 00:00:00