Aminopeptidase inhibitory properties and analgesic activity of (2S,3R)-3,7-diamino-2-hydroxy-heptanoic acid containing tripeptide analogues of the N-terminal tripeptide of probestin.

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 4-amino-7,8-dimethoxy-5H-pyrimido[5,4-b]indole derivatives has been synthesized. These compounds resemble carbazeram and other pyridazino compounds with activity in the cardiovascular system. Some of these new compounds possess inotropic activity (Table 2), with a complementary effect on the inhibition of ...

journal_title：Archiv der Pharmazie

authors： Monge A,Martínez-Crespo FJ,Villanueva MA,Font M,Santiago E,Martínez de Irujo JJ,Alberdi E,López-Unzu MJ,Cenarruzabeitia E,Castiella E

更新日期：1993-11-01 00:00:00

abstract：:A series of novel N-(4,5-dihydroimidazol-2-yl)-1,3-dihydrobenzimidazole derivatives 2a-d, 3a-d and 4a-p were prepared and their structure was determined by IR and NMR spectroscopic data as well as X-ray analysis of carbonitrile 2a. The compounds were studied as potential inhibitors of the human blood platelet aggregat...

journal_title：Archiv der Pharmazie

authors： Saczewski F,Debowski T,Petrusewicz J,Trzeciak H,Krzystanek E,Krzystanek M,Gdaniec M,Nowakowska E

更新日期：1998-07-01 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：:1-Substiuted 6-(3-cyanobenzoyl) and [(3-cyanophenyl)fluoromethyl]-5-ethyl-uracils were synthesized and evaluated in cell-based assays against HIV-1 wild-type and its clinically relevant non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant mutants. Some of the synthesized compounds showed activity against H...

journal_title：Archiv der Pharmazie

authors： Loksha YM,Pedersen EB,Loddo R,La Colla P

更新日期：2009-09-01 00:00:00

abstract：:The objective of this work was to develop a liver-specific antihepato carcinoma agent. A series of 5-fluorouracil / cholic acid conjugates (5-FU-cholic acid conjugates) were prepared and tested for their chemical characteristics and bio-distribution properties. The in-vitro stability trial showed 5-FU-cholic acid conj...

journal_title：Archiv der Pharmazie

authors： Qian S,Wu JB,Wu XC,Li J,Wu Y

更新日期：2009-09-01 00:00:00

abstract：:In the present study, a novel series of polyfunctionalized imidazopyrimidines 6a-u and 9a-d were efficiently constructed by a domino reaction between 2-imino-6-substituted-2,3-dihydropyrimidin-4(1H)-ones 4a-d or 8a-c and 2-bromoacetophenones 5a-i under mild basic conditions. The synthesized series were screened for th...

journal_title：Archiv der Pharmazie

authors： Abdel-Mohsen HT,Abood A,Flanagan KJ,Meindl A,Senge MO,El Diwani HI

更新日期：2020-03-01 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：:This paper describes the use of the multivariate image analysis-quantitative structure-activity relationship (MIA-QSAR) methodology, which is a method capable of relating chemical structures with their biological activities. This in silico method has been shown to be extremely reliable and provides excellent results, ...

journal_title：Archiv der Pharmazie

authors： Bitencourt M,Freitas MP,Rittner R

更新日期：2012-09-01 00:00:00

abstract：:A series of novel N(1)-[5-(4-substituted phenyl)-1,3,4-thiadiazol-2-yl]-N(4)-(4-substituted benzaldehyde)-semicarbazone 1-12, N(1)-[5-(4-substituted phenyl)-1,3,4-thiadiazol-2-yl]-N(4)-[1-(4-substituted phenyl)ethanone]-semicarbazone 13-16, and N(1)-[5-(4-substituted phenyl)-1,3,4-thiadiazol-2-yl]-N(4)-[1-(4-substitut...

journal_title：Archiv der Pharmazie

authors： Rajak H,Deshmukh R,Aggarwal N,Kashaw S,Kharya MD,Mishra P

更新日期：2009-08-01 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：:Esters of beta-carboline-3-carboxylic acid with alicyclic substituents were prepared and tested with respect to their affinity for the benzodiazepine receptor in mouse brain membranes. Compounds 3d,f and 4b showed high affinities (less than 70 nmol). In the case of 3f the benzodiazepine moiety may be responsible for t...

journal_title：Archiv der Pharmazie

authors： Geldsetzer KH,Schunack W

更新日期：1990-01-01 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：:Starting from the commercially available 6-methyl-2-pyridylamine (1) the pyrido[3,2-e][1,4]diazepine 14a was synthesized in 12 steps with 7% total yield. 14a, the N-methyl derivative 14b, the thiolactam 15a, the amidine 16, and the 1,2,4-triazole 17 were tested for anti-HIV-1-activity. None of the compounds tested pos...

journal_title：Archiv der Pharmazie

authors： Görlitzer K,Wilpert C,Rübsamen-Waigmann H,Suhartono H,Wang L,Immelmann A

更新日期：1995-03-01 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：: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：:Alzheimer's disease (AD) is a neurodegenerative disorder characterized by dementia, memory impairment, cognitive dysfunction, and speech impairment. The utility of cholinergic replacement by acetylcholinesterase (AChE) inhibitors in AD treatment has been well documented so far. Recently, studies have also evidenced th...

journal_title：Archiv der Pharmazie

authors： Kalaycı M,Türkeş C,Arslan M,Demir Y,Beydemir Ş

更新日期：2020-11-06 00:00:00

abstract：:A series of eperezolid analogs with glycinyl substitutions were prepared and their antibacterial activities were studied against a panel of susceptible and resistant Gram-positive bacteria. The compounds with N-arylacyl or N-heteroarylacyl glycinyl structural units showed good antibacterial activities. The compounds 1...

journal_title：Archiv der Pharmazie

authors： Wang XJ,Wu N,Du GJ,Zhao SQ,Yan M,Gu LQ

更新日期：2009-07-01 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：: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：:Biphalin [(Tyr-D-Ala-Gly-Phe-NH-)2 ] is an octapeptide with mixed μ/δ opioid activity. Its structure is based on two identical enkephalin-like portions linked "tail-to-tail" by a hydrazine bridge. This study presents the synthesis and in vitro and in vivo bioassays of two biphalin analogs that do not present the toxic...

journal_title：Archiv der Pharmazie

authors： Costante R,Pinnen F,Stefanucci A,Mollica A

更新日期：2014-05-01 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：: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：:Several 5-alkoxy-tetrazolo[1,5-a]quinazoline derivatives have been synthesized by reacting 2,4-dichloroquinazoline with various phenols or aliphatic alcohol and then with sodium azide. The structures of these compounds have been confirmed by IR, MS,( 1)H-NMR, and elementary analysis. Anticonvulsant activities were eva...

journal_title：Archiv der Pharmazie

authors： Wang HJ,Wei CX,Deng XQ,Li FL,Quan ZS

更新日期：2009-11-01 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：: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

authors： Wieking K,Knockaert M,Leost M,Zaharevitz DW,Meijer L,Kunick C

更新日期：2002-07-01 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：:A series of bis(benzo[g]indoles) bridged by CX-(CH2)nN(Me)(CH2)n-CX (X = O, S, H2; n = 2,3) was synthesized as bifunctional antitumor agents and evaluated for cytotoxic activity against diverse human cancer cell lines by the National Cancer Institute. The parent compounds 2a,b exhibited a good level of activity and de...

journal_title：Archiv der Pharmazie

authors： Pinna GA,Pirisi MA,Grella GE,Gherardini L,Mussinu JM,Paglietti G,Ferrari AM,Rastelli G

更新日期：2001-11-01 00:00:00

abstract：:Biphenyl nitriles 5a-c, terphenyl dinitriles 11a-d, and naphthalene-bis(benzonitrile) 11c were prepared by palladium-catalyzed cross coupling reactions and subsequently converted to biphenyl amidines 8a-c and bis(benzamidines) 4a-e. Among the biphenyl amidines 8 only the meta-derivative 8b inhibits factor Xa and tryps...

journal_title：Archiv der Pharmazie

authors： von der Saal W,Engh RA,Eichinger A,Gabriel B,Kucznierz R,Sauer J

更新日期：1996-02-01 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