Synthesis and evaluation of sulfur-containing glutethimide derivatives for aromatase and desmolase inhibitory activity.

abstract：:Marine organisms play an important role in natural product-based drug research due to accumulation of structurally unique and bioactive metabolites. The exploration of marine-derived compounds may significantly extend the scientific knowledge of potential scaffolds for antibiotic drug discovery. Development of novel a...

journal_title：Archiv der Pharmazie

authors： Daletos G,Ancheeva E,Chaidir C,Kalscheuer R,Proksch P

更新日期：2016-10-01 00:00:00

abstract：:CXC chemokine receptor-3 (CXCR3) is a G-protein coupled receptor (GPCR) predominantly expressed on activated T lymphocytes that promote Th1 responses. Previously, we described the 3H-quinazolin-4-one containing VUF 5834 (decanoic acid {1-[3-(4-cyano-phenyl)-4-oxo-3,4-dihydro-quinazolin-2-yl]-ethyl}-(2-dimethylamino-et...

journal_title：Archiv der Pharmazie

authors： Storelli S,Verzijl D,Al-Badie J,Elders N,Bosch L,Timmerman H,Smit MJ,De Esch IJ,Leurs R

更新日期：2007-06-01 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 preparation and detailed composition of an oil newly extracted from pure soy germ (not less than 96 % hypocotyle) are presented. Experiments in vivo showed that soybean-germ oil (SGO) possesses a remarkable protective activity against UVB-induced skin inflammation, exceeding that of tocopherol acetate by a factor ...

journal_title：Archiv der Pharmazie

authors： Bonina F,Puglia C,Avogadro M,Baranelli E,Cravotto G

更新日期：2005-12-01 00:00:00

abstract：:The active form of vitamin D3 , calcitriol, is a potent antiproliferative compound. However, when effective antitumor doses of calcitriol are used, hypercalcemic effects are observed, thus blocking its therapeutic application. To overcome this problem, structural analogues have been designed with the aim of retaining ...

journal_title：Archiv der Pharmazie

authors： Obiol DJ,Martínez A,Ferronato MJ,Quevedo MA,Grioli SM,Alonso EN,Gómez G,Fall Y,Facchinetti MM,Curino AC

更新日期：2019-05-01 00:00:00

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

authors： Ahmed NS,Elgendy M,Laufer S,Abadi AH

更新日期：2014-06-01 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

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：:The synthesis and biological evaluation of ethyl 8-oxo-5,6,7,8-tetrahydro-thiazolo[3,2-a][1,3]diazepin-3-carboxylate (HIE-124, 4), as a member of a new generation of ultra-short acting hypnotics is described. HIE-124 4 exhibited potent in-vivo activity with a very rapid onset of action and a shorter duration of action...

journal_title：Archiv der Pharmazie

authors： Kadi AA,El-Kashef HA,Abdel-Aziz AA,Hassan GS,Tettey J,Grant MH,Lehmann J,El-Subbagh HI

更新日期：2008-02-01 00:00:00

abstract：:The precise definition of the structural requirements for effective topoisomerase II poisoning by drug molecules is still an elusive issue. In the attempt to better define a pharmacophoric pattern, we prepared several conjugates combining the chemical features of two well-known topoisomerase II poisons, amsacrine and ...

journal_title：Archiv der Pharmazie

authors： Zagotto G,Gianoncelli A,Sissi C,Marzano C,Gandin V,Pasquale R,Capranico G,Ribaudo G,Palumbo M

更新日期：2014-10-01 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：:Alzheimer's disease (AD) is the most common type of dementia and related to the degeneration of hippocampal cholinergic neurons, which dramatically affects cognitive ability. Acetylcholinesterase (AChE) inhibitors are employed as drugs for AD therapy. Three series of sulfonylhydrazone compounds were designed, and thei...

journal_title：Archiv der Pharmazie

authors： Fernandes TB,Cunha MR,Sakata RP,Candido TM,Baby AR,Tavares MT,Barbosa EG,Almeida WP,Parise-Filho R

更新日期：2017-11-01 00:00:00

abstract：:A new method for the synthesis of ODN-luciferase conjugate was investigated as a signal-amplifying sensor of the target nucleic acids. The conjugation of the luciferase was successfully achieved between the cysteine residue and the 2-amino-6-vinylpurine nucleoside of the ODN probe without significant inactivation of l...

journal_title：Archiv der Pharmazie

authors： Nagatsugi F,Nakahara R,Inoue K,Sasaki S

更新日期：2008-09-01 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：:(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：: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：:Structural feature analysis of chlorogenic acid derivatives made up of varying lengths of alkyl groups as α-glucosidases inhibitors were performed by QSAR techniques. The statistically significant models derived from the study were validated by leave one out, Y-randomization and test set methods. The predictive capaci...

journal_title：Archiv der Pharmazie

authors： Narayana Moorthy NS,Ramos MJ,Fernandes PA

更新日期：2012-04-01 00:00:00

abstract：:Derivatives of the recently described potent neuroprotective 7-O-cinnamoylsilibinin ester were prepared: its hemisuccinate to improve water solubility and the dehydrosilibinin ester that was shown to form in assay media to investigate its role in overall neuroprotective effects. 7-O-Cinnamoyl-2,3-dehydrosilibinin is l...

journal_title：Archiv der Pharmazie

authors： Schramm S,Gunesch S,Lang F,Saedtler M,Meinel L,Högger P,Decker M

更新日期：2018-11-01 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：: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：:A 3D pharmacophore model predicting anticonvulsant activity was obtained for a series of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives recently disclosed as a new class of noncompetitive AMPA receptor antagonists. The training set included 17 compounds with varying potency against audiogenic seizures in DBA...

journal_title：Archiv der Pharmazie

authors： De Luca L,Gitto R,Barreca ML,Caruso R,Quartarone S,Citraro R,De Sarro G,Chimirri A

更新日期：2006-07-01 00:00:00

abstract：:[4-(Adamantane-1-carboxamido)-3-oxo-1-thia-4-azaspiro[4.4]nonan-2-yl]acetic acid (4a) and [4-(adamantane-1-carboxamido)-8-nonsubstituted/substituted-3-oxo-1-thia-4-azas-piro[4.5]decane-2-yl]acetic acid (4b-g) derivatives were synthesized; their structures were verified by elemental analysis, infrared spectroscopy, 1 H...

journal_title：Archiv der Pharmazie

authors： Turk-Erbul B,Karaman EF,Duran GN,Ozbil M,Ozden S,Goktas F

更新日期：2021-01-06 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：: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 series of potent HIV-protease inhibitors has been prepared. Several of the newly synthesized compounds showed high plasma even after oral administration to animals. Based on the overall biological profile, CGP 61755 was chosen for further preclinical evaluation. For this compound, a 10 step synthesis potentially sui...

journal_title：Archiv der Pharmazie

authors： Capraro HG,Bold G,Fässler A,Cozens R,Klimkait T,Lazdins J,Mestan J,Poncioni B,Rösel JL,Stover D,Lang M

更新日期：1996-06-01 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：:The synthesis and antitumor activity screening of novel isatin based conjugates with thiazolidine and pyrazoline moieties were performed. Reaction of 3,5-diaryl-4,5-dihydropyrazoles with chloroacetyl chloride yielded starting 2-chloro-1-(3,5-diaryl-4,5-dihydropyrazol-1-yl)-ethanones which were utilized in alkylation o...

journal_title：Archiv der Pharmazie

authors： Havrylyuk D,Kovach N,Zimenkovsky B,Vasylenko O,Lesyk R

更新日期：2011-08-01 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：:Solid-state Nuclear Magnetic Resonance (NMR) provides a general method to study molecular structure and dynamics in a non-crystalline and insoluble environment. We discuss the latest methodological progress to construct 3D molecular structures from solid-state NMR data obtained under magic-angle-spinning conditions. A...

journal_title：Archiv der Pharmazie

authors： Luca S,Heise H,Lange A,Baldus M

更新日期：2005-06-01 00:00:00

abstract：:In search of structure-activity relationships among histamine H3-receptor antagonists the imidazole ring of known H3-receptor antagonists was replaced by different heteroaromatic ring systems. Thus, azines and diazines with ether (6-13) and carbamate (15-24) moieties as functional groups were synthesized. The obtained...

journal_title：Archiv der Pharmazie

authors： Kieć-Kononowicz K,Ligneau X,Stark H,Schwartz JC,Schunack W

更新日期：1995-05-01 00:00:00

abstract：:Oxidative stress is related to the pathogenesis and progress of several human diseases. NADPH oxidase (NOX), and mainly the NOX2 isoform, produces superoxide anions (O2•- ). To date, it is known that NOX2 can be inhibited by preventing the assembly of its subunits, p47phox and p22phox. In this work, we analyzed the bi...

journal_title：Archiv der Pharmazie

authors： Macías Pérez ME,Hernández Rodríguez M,Cabrera Pérez LC,Fragoso-Vázquez MJ,Correa-Basurto J,Padilla-Martínez II,Méndez Luna D,Mera Jiménez E,Flores Sandoval C,Tamay Cach F,Rosales-Hernández MC

更新日期：2017-10-01 00:00:00