The topical protective effect of soybean-germ oil against UVB-induced cutaneous erythema: an in vivo evaluation.

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

authors： Artico M,Silvestri R,Stefancich G,Massa S,Pagnozzi E,Musu D,Scintu F,Pinna E,Tinti E,La Colla P

更新日期：1995-03-01 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：:A number of 7-piperazinylquinolones carrying a functionalized 2-(furan-3-yl)ethyl moiety attached to the piperazine ring have been synthesized and evaluated as antibacterial agents against a panel of Gram-positive and Gram-negative bacteria. Most of the synthesized compounds exhibited significant antibacterial activit...

journal_title：Archiv der Pharmazie

authors： Foroumadi A,Mohammadhosseini N,Emami S,Letafat B,Faramarzi MA,Samadi N,Shafiee A

更新日期：2007-01-01 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：:To identify new agents for the treatment of American cutaneous leishmaniasis, a series of eight 1,4-bis(substituted benzalhydrazino)phthalazines was evaluated against Leishmania braziliensis and Leishmania mexicana parasites. These compounds represent a disubstituted version of the 1-chloro-4-(monoaryl/heteroarylhydra...

journal_title：Archiv der Pharmazie

authors： Romero AH,Rodríguez N,Oviedo H,Lopez SE

更新日期：2019-06-01 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：: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 regio- and stereospecific synthesis of O-methyl-chiro-inositols and O-methyl-scyllo-inositol was achieved, starting from p-benzoquinone. After preparing dimethoxy conduritol-B as a key compound, regiospecific bromination of the alkene moiety of dimethoxy conduritol-B and acid-catalyzed ring opening of dimethoxydia...

journal_title：Archiv der Pharmazie

authors： Aksu K,Akincioglu H,Gulcin I,Kelebekli L

更新日期：2020-09-30 00:00:00

abstract：:The ongoing interest in very efficient systems for the imitation of cytochrome P-450-dependent monooxygenase reactions, consisting of metalloporphyrin and oxygen donor, prompted us to develop a method to compare the catalytic activity of soluble metalloporphyrins with those which have been immobilised on different sil...

journal_title：Archiv der Pharmazie

authors： Lübbe AN,Rickerts B,Duchstein HJ

更新日期：2006-12-01 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：: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：:Three novel series of quinoline derivatives have been prepared by cyclization of the intermediate 3-(1,3-dioxolan-2-yl)-2-substituted thiocarbamoyl-hydrazinoquinolines with different alpha-halocarbonyl compounds. These series are: 3-(1,3-dioxolan-2-yl)-2-(3-substituted-4-phenylthiazolin-2-y lidene) hydrazinoquinolines...

journal_title：Archiv der Pharmazie

authors： Farghaly AM,Habib NS,Khalil MA,el-Sayed OA,Bistawroos AE

更新日期：1990-04-01 00:00:00

abstract：:6-Amino-5-imino-pyrazolo[4',3':5,6]pyrano[2,3-d]pyrimidine derivative 4 and pyrazolo-[4',3':5,6]pyrano[2,3-d]pyrimidin-5-ylhydrazine derivative 5 were prepared starting from 6-amino-3-methyl-4-(p-nitrophenyl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile 1. The synthesis and structure characterization of 9,11-dihydr...

journal_title：Archiv der Pharmazie

authors： Shamroukh AH,Zaki ME,Morsy EM,Abdel-Motti FM,Abdel-Megeid FM

更新日期：2007-07-01 00:00:00

abstract：:A series of 5-amino-3-methylisoxazole-4-carboxylic acid amides has been prepared by condensation of 5-amino-3-methylisoxazole-4-carboxylic acid with ethyl chloroformate. The resulting mixed anhydride undergoes condensation with appropriate phenylamides to form the corresponding amides 6-16. The compounds obtained were...

journal_title：Archiv der Pharmazie

authors： Ryng S,Zimecki M,Sonnenberg Z,Mokrosz MJ

更新日期：1999-05-01 00:00:00

abstract：:The complex of lanthanum (III) was synthesized reacting the respective inorganic salt with 5-aminoorotic acid in amounts equal to the metal:ligand molar ratio of 1:3. The complex was prepared by adding an aqueous solution of lanthanum (III) nitrate to an aqueous solution of the ligand, subsequently raising the pH of t...

journal_title：Archiv der Pharmazie

authors： Kostova I,Rastogi VK,Kiefer W,Kostovski A

更新日期：2006-11-01 00:00:00

abstract：:Some 2-arylpyrazolo[1,5-c][1,3]benzoxazin-5-ones 1 and 5- oxopyrazolo[1,5-c][1,3]benzoxazin-2-carboxylates 2 were prepared and biologically evaluated for their binding at benzodiazepine receptor (BZR) in rat cortical membranes. Structure-activity relationship studies suggest that, although proton donor d and proton ac...

journal_title：Archiv der Pharmazie

authors： Varano F,Catarzi D,Colotta V,Cecchi L,Filacchioni G,Galli A,Costagli C

更新日期：1996-12-01 00:00:00

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

authors： Ortmann R,Wiesner J,Silber K,Klebe G,Jomaa H,Schlitzer M

更新日期：2007-09-01 00:00:00

abstract：:The activity of 72 1,4-dihydropyridines as calcium channel antagonists was examined. The simplified molecular input-line entry system (SMILES) was used as representation of the molecular structure of the calcium channel antagonists. Quantitative structure-activity relationships (QSARs) were developed using CORAL softw...

journal_title：Archiv der Pharmazie

authors： Veselinović AM,Milosavljević JB,Toropov AA,Nikolić GM

更新日期：2013-02-01 00:00:00

abstract：:A new series of pyrazole, phenylpyrazole, and pyrazoline analogs of diarylpentanoids (excluding compounds 3a, 4a, 5a, and 5b) was pan-assay interference compounds-filtered and synthesized via the reaction of diarylpentanoids with hydrazine monohydrate and phenylhydrazine. Each analog was evaluated for its anti-inflamm...

journal_title：Archiv der Pharmazie

authors： Mohd Faudzi SM,Leong SW,Auwal FA,Abas F,Wai LK,Ahmad S,Tham CL,Shaari K,Lajis NH,Yamin BM

更新日期：2021-01-01 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：: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

authors： García-López MT,González-Muñiz R,Hartoa JR,Gómez-Monterrey I,Pérez C,De Ceballos ML,López E,Del Río J

更新日期：1992-01-01 00:00:00

abstract：:Non-steroidal anti-inflammatory drugs (NSAIDs), which are widely used for the treatment of rheumatic arthritis, pain, and many different types of inflammatory disorders, cause serious gastrointestinal (GI) side effects. The free carboxylic acid group existing on their chemical structure is correlated with GI toxicity ...

journal_title：Archiv der Pharmazie

authors： Koksal M,Ozkan-Dagliyan I,Ozyazici T,Kadioglu B,Sipahi H,Bozkurt A,Bilge SS

更新日期：2017-09-01 00:00:00

abstract：:In this study, a number of 2,5-disubstituted 1,3,4-thiadiazoles were synthesized using an appropriate synthetic route, and their anticonvulsant activity was determined by the maximal electroshock seizure (MES) test and their neurotoxicity was evaluated by the rotarod test. Additionally, their hypnotic activity was tes...

journal_title：Archiv der Pharmazie

authors： Toolabi M,Khoramjouy M,Aghcheli A,Ayati A,Moghimi S,Firoozpour L,Shahhosseini S,Shojaei R,Asadipour A,Divsalar K,Faizi M,Foroumadi A

更新日期：2020-12-01 00:00:00

abstract：:Salicylamide amino acid conjugates were prepared utilizing 5-formyl-, 5-dicyanoethenyl-, and 5-nitroethenylsalicylic acid. 5-Substituted salicylanilides were treated with glycine and formaldehyde in a Mannich type reaction affording the corresponding 3-(N-glycino)salicylanilides. The reactions of anilines with pyrans ...

journal_title：Archiv der Pharmazie

authors： Nawwar GA

更新日期：1994-04-01 00:00:00

abstract：:Twelve ethoxycarbonyl or phenylsulfonyl derivatives as prodrugs of hydroxylamine or phenylhydroxylamine were prepared and tested for antiplatelet (in vitro, Born test) antithrombotic (in vivo thrombosis model), and antihypertensive (in vivo, SHR rats) effects. In the Born test N,N-bisphenylsulfonylhydroxylamine (10) w...

journal_title：Archiv der Pharmazie

authors： Rehse K,Shahrouri T

更新日期：1998-11-01 00:00:00

abstract：:The synthesis of some new analogs of quinolin-4-one and 1,7-naphthyridin-4-one is described. The prepared compounds were tested for their in vitro antitumor and cdc2 kinase or cdc25 phosphatase inhibitory activity. Compound ethyl 7-oxo-2,3-dihydro-7H-pyrido [1,2,3-de][2,3-b]pyrido-1,4-thiazine-6-carboxylate (6b) showe...

journal_title：Archiv der Pharmazie

authors： el-Subbagh HI,Abadi AH,al-Khawad IE,al-Rashood KA

更新日期：1999-01-01 00:00:00

abstract：:JL 13 (5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b]- [1,5]benzoxazepine fumarate) and JL 3 (10-(4-methylpiperazin-1- yl)pyrido[4,3-b][1,4]benzothiazepine), two pyridobenzazepine derivatives structurally related to clozapine, were selected for further development. Due to their structural similarity to clozapine, t...

journal_title：Archiv der Pharmazie

authors： Liégeois JF,Zahid N,Bruhwyler J,Uetrecht J

更新日期：2000-03-01 00:00:00

abstract：:The effect of triterpenes and flavonoids on the activity of several hyaluronic acid-splitting enzymes was investigated. Studies showed that the inhibitory effect of the triterpenes glycyrrhizin and glycyrrhetinic acid is dependent on the source of hyaluronate lyase. Hyaluronate lyase from Streptococcus agalactiae (Hya...

journal_title：Archiv der Pharmazie

authors： Hertel W,Peschel G,Ozegowski JH,Müller PJ

更新日期：2006-06-01 00:00:00

abstract：:A novel series of N-(2-(piperazin-1-yl)phenyl)aryl carboxamide derivatives were simply synthesized by Ugi-multicomponent reaction as β-secretase (BACE1) inhibitors. The BACE1 inhibitory activity of the synthesized compounds was examined using a Forester resonance energy transfer (FRET)-based assay. Among the tested co...

journal_title：Archiv der Pharmazie

authors： Edraki N,Firuzi O,Fatahi Y,Mahdavi M,Asadi M,Emami S,Divsalar K,Miri R,Iraji A,Khoshneviszadeh M,Firoozpour L,Shafiee A,Foroumadi A

更新日期：2015-05-01 00:00:00

abstract：:Permeability glycoprotein (P-gp) is involved in the pathology of various diseases including cancer and epilepsy, mainly through the translocation of some medicines across the cell membrane. Here, we employed image-based quantitative structure-activity relationship (QSAR) models to predict the P-gp inhibitory activity ...

journal_title：Archiv der Pharmazie

authors： Shayanfar S,Shayanfar A,Ghandadi M

更新日期：2016-02-01 00:00:00