Novel calcitriol analogue with an oxolane group: In vitro, in vivo, and in silico studies.

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：:We report in this work the synthesis, cytotoxicity, and antimicrobial activity of ([1,2,4]triazolo[1,5-c]quinazolin-2-ylthio)carboxylic acid amides 4-7 in connection with our previous research in the preparation of triazoloquinazoline derivatives. Due to simplicity, general availability of starting materials, and high...

journal_title：Archiv der Pharmazie

authors： Antipenko LN,Karpenko AV,Kovalenko SI,Katsev AM,Komarovska-Porokhnyavets EZ,Novikov VP

更新日期：2009-11-01 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 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：: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

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：:Prevention of the formation of advanced glycation end-products (AGEs) is a reliable approach to achieve control over hyperglycemia and the associated pathogenesis of diabetic vascular complications. In these terms, new synthetic approaches to 6-nitroazolo[1,5-a]pyrimidines have been developed on the basis of the promi...

journal_title：Archiv der Pharmazie

authors： Spasov AA,Babkov DA,Sysoeva VA,Litvinov RA,Shamshina DD,Ulomsky EN,Savateev KV,Fedotov VV,Slepukhin PA,Chupakhin ON,Charushin VN,Rusinov VL

更新日期：2017-12-01 00:00:00

abstract：:A new series of 1,2,4-triazolo[4,3-c]quinazoline derivatives was designed and synthesized as Topo II inhibitors and DNA intercalators. The cytotoxic effect of the new members was evaluated in vitro against a group of cancer cell lines including HCT-116, HepG-2, and MCF-7. Compounds 14c , 14d , 14e , 14e , 15b , 18b , ...

journal_title：Archiv der Pharmazie

authors： Alesawy MS,Al-Karmalawy AA,Elkaeed EB,Alswah M,Belal A,Taghour MS,Eissa IH

更新日期：2020-11-23 00:00:00

abstract：:Syntheses of a new series of biologically potent α-aminophosphonates were accomplished by one-pot Kabachnik-Fields reaction using TiO2-SiO2 as solid supported catalyst under microwave irradiation conditions. The chemical structures of all the newly synthesized compounds were confirmed by analytical and spectral (IR, 1...

journal_title：Archiv der Pharmazie

authors： Chinthaparthi RR,Bhatnagar I,Gangireddy CS,Syama SC,Cirandur SR

更新日期：2013-09-01 00:00:00

abstract：:The photochemical stability of 2, 6, 6-trimethyl-3-carbmethoxy-4-phenyl-5-oxo-1, 4, 5, 6, 7, 8-hexahydroquinoline (HHQ) derivatives with different substituents on the phenyl ring (-Cl, -NO(2), -CF(3), -CH(3), -OCH(3)) has been studied.The process of photodegradation was studied by UV spectrophotometry. The rate of pho...

journal_title：Archiv der Pharmazie

authors： Mielcarek J,Safak C,Simsek R,Matloka A

更新日期：2002-05-01 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：: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：:Although a large number of pharmaceutical therapies are available to treat cardiovascular diseases like heart failure, in many medical conditions treatment is still not optimal and, therefore, the need for innovative, safe and efficacious drugs is still very high in this indication. Biomarkers are an important tool in...

journal_title：Archiv der Pharmazie

authors： Kramer F,Dinh W

更新日期：2016-06-01 00:00:00

abstract：:Polyketide-derived macrolactones like zearalenone (1), zearalane (2) or curvularin (3) display a wide range of interesting pharmacological activities. Here, we present a short and efficient approach towards this class of natural products by a combination of the Sonogashira and Mitsunobu reactions. The resulting lacton...

journal_title：Archiv der Pharmazie

authors： Krauss J,Unterreitmeier D,Neudert C,Bracher F

更新日期：2005-12-01 00:00:00

abstract：:A series of 1-¿omega-(4-aryl-1-piperazinyl)alkyl]indolin-2(1H)-one derivatives 2-14 was synthesized in order to obtain ligands with a dual 5-HT1A/5-HT2A activity. The majority of those compounds (2-5, 7, 10-13) exhibited a high 5-HT1A (Ki = 2-44 nM) and/or 5-HT2A affinity (Ki = 51 and 39 for 5 and 7, respectively). In...

journal_title：Archiv der Pharmazie

authors： Mokrosz MJ,Duszyńska B,Misztal S,Kłodzińska A,Tatarczyńska E,Chojnacka-Wójcik E,Dziedzicka-Wasylewska M

更新日期：1998-10-01 00:00:00

abstract：:A series of hydroxy-substituted chalcone oxime derivatives were synthesized. These compounds were then evaluated for their inhibitory activities on tyrosinase and melanogenesis in murine B16F10 melanoma cells. The structures of the synthesized compounds were confirmed by (1) H NMR, (13) C NMR, FTIR, and HRMS. Two of t...

journal_title：Archiv der Pharmazie

authors： Radhakrishnan SK,Shimmon RG,Conn C,Baker AT

更新日期：2016-01-01 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：:Styrylquinazoline derivatives were prepared by Perkin condensation and evaluated for inhibitory activity against HIV-1 integrase. Among them, compound 5c containing a free catechol ring was the most potent (IC(50)=0.8 +/- 1.9 microM)and showed 6-fold more potency than the corresponding styrylquinoline compound (IC(50)...

journal_title：Archiv der Pharmazie

authors： Lee JY,Park JH,Lee SJ,Park H,Lee YS

更新日期：2002-06-01 00:00:00

abstract：:A new series of 4-hydroxycoumarin derivatives 3a-d was synthesized by the reaction of 3-bromo-4-hydroxy coumarin 1 with various heteroaldehydes 2a-d in good yields. The synthesized compounds were characterized on the basis of their elemental and spectral (IR, (1)H-NMR and mass spectrometry) analysis. All target compou...

journal_title：Archiv der Pharmazie

authors： Siddiqui ZN,N MM,Ahmad A,Khan AU

更新日期：2011-06-01 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：: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：: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：: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：: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：: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：:A series of 5-(o-tolyl)-1H-tetrazole derivatives were synthesized and evaluated for their anticonvulsant activities. 1-(2-Methylbenzyl)-5-(o-tolyl)-1H-tetrazole (3h) showed important anticonvulsant activity against the MES-induced seizures, as well as lower neurotoxicity with an ED50 value of 12.7 mg/kg and a TD50 val...

journal_title：Archiv der Pharmazie

authors： Dong S,Wang T,Wang H,Qian K,Zhang Z,Zuo Y,Luo G,Jin Y,Wang Z

更新日期：2017-05-01 00:00:00

abstract：:New, non-imidazole histamine H3 receptor antagonists were prepared and in vitro tested as H3 receptor antagonists measured as the electrically evoked contraction of the guinea-pig jejunum. The 2-(1-piperidinyl)- and 2-(1-pyrrolidinyl)benzothiazoles show no or very poor activity; 2-[1-(4-amino)piperidinyl]- and 2-(1,2-...

journal_title：Archiv der Pharmazie

authors： Walczyński K,Guryn R,Zuiderveld OP,Timmerman H

更新日期：1999-11-01 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：: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：:An overview of the rhodopsin crystal structure provides a structural basis for understanding the structures and functions of other G-protein coupled receptors (GPCRs). All of the structural details observed to date for rhodopsin will not necessarily carry over to other GPCRs, but major features such as the arrangement...

journal_title：Archiv der Pharmazie

authors： Stenkamp RE,Teller DC,Palczewski K

更新日期：2005-06-01 00:00:00