Synthesis of thiazolyl hydrazonothiazolamines and 1,3,4-thiadiazinyl hydrazonothiazolamines as a class of antimalarial agents.

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：: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：:Stress is implicated in the pathogenesis of numerous disorders such as cardiovascular diseases or neurodegeneration. The extensive overlap between diseases attributed to stress and oxidative damage is indicative of their potential relationship. We hereby study the influence of alpha-tocopherol (alpha-toc) on the devel...

journal_title：Archiv der Pharmazie

authors： Tsiakitzis K,Kourounakis AP,Tani E,Rekka EA,Kourounakis PN

更新日期：2005-07-01 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：: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：:In an attempt to find a new class of antibacterial agents, we have synthesized thirty new coumarin (2H-benzopyran-2-one) analogues. These derivatives include substituted azetidin-2-ones (beta-lactam) 3a-f, pyrrolidin-2-ones 4a-f, 2H-1,3,4-oxadiazoles 5a-f, and thiazolidin-4-ones 6a-f attached to 4-phenyl-2H-benzopyran...

journal_title：Archiv der Pharmazie

authors： Hassan GS,Farag NA,Hegazy GH,Arafa RK

更新日期：2008-11-01 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：: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：:A series of 6-chloro-3-(4-alkylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones, 7-chloro-3-(4-alkylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones, 6-bromo-3-(4-alkylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones, 6,8-dibromo-3-(4-alkylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones, 6-chloro-3-(4-alkylphenyl)-2H-1,3-ben...

journal_title：Archiv der Pharmazie

authors： Waisser K,Matyk J,Kunes J,Dolezal R,Kaustová J,Dahse HM

更新日期：2008-12-01 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：: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：: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

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：:Synthesis of 2-chloro-1,1-dimethylethyl and 2-chloro-2,2-dimethylethyl analogues of ifosfamide was performed via aziridine intermediate. In vitro metabolic activation showed that both compounds are metabolised at a rate similar to the parent drug. However, their anticancer activity against L1210 leukaemia in mice was ...

journal_title：Archiv der Pharmazie

authors： Misiura K,Kardacka K,Kusnierczyk H

更新日期：2001-09-01 00:00:00

abstract：:A facile synthesis of a group of novel thiazole-pyrazolone hybrids and their investigation for angiotensin-converting enzyme (ACE) inhibition are reported in this study. These compounds were synthesized using a well-known approach, based on the condensation of ethyl acetoacetate with thiazolylhydrazines, and character...

journal_title：Archiv der Pharmazie

authors： You H,Su X,Su G

更新日期：2020-12-01 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：:This review emphasizes the relationship of breast cancer, estrogen receptor and ligands, especially the centrality of the estrogen receptor, which mediates on one hand the hormone-induced gene transcription and on the other hand the anti-estrogen action against breast cancer. The characterization of the estrogen recep...

journal_title：Archiv der Pharmazie

authors： Bai Z,Gust R

更新日期：2009-03-01 00:00:00

abstract：:A set of 40 derivatives of 3-hydroxypicolinic acid and 2-sulfanylbenzoic acid, isosteric to salicylanilides was synthesized. The compounds were evaluated for in vitro activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium, Candida albicans, Candida tropicalis, Candida krusei, Candi...

journal_title：Archiv der Pharmazie

authors： Waisser K,Pesina M,Holý P,Pour M,Bures O,Kunes J,Klimesová V,Buchta V,Kubanová P,Kaustová J

更新日期：2003-08-01 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：:A synthesis of two new active substances, DOMCl (1-(4-chloromethyl-2, 5-dimethoxyphenyl)-2-propanamine; 2) and DOMOM (1-(2, 5-dimethoxy-4-methoxymethylphenyl)-2-propanamine; 3), was developed. Unexpectedly, the Blanc reaction permitted successful synthesis of 2, 5-dimethoxyphenylpropylamine derivatives having a substi...

journal_title：Archiv der Pharmazie

authors： Harms A,Ulmer E,Kovar KA

更新日期：2003-06-01 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：:Poly(vinyl alcohol) was crosslinked with ethylene glycol diglycidyl ether to obtain hydrogel-forming polymers. The polymers were also substituted with oleoyl chloride, providing hydrogels with weak solubility. These new polymeric materials were evaluated for the formulation of sustained drug delivery systems. Vancomyc...

journal_title：Archiv der Pharmazie

authors： Orienti I,Treré R,Luppi B,Bigucci F,Cerchiara T,Zuccari G,Zecchi V

更新日期：2002-03-01 00:00:00

abstract：:Platensimycin is a natural product isolated from various strains of Streptomyces platensis which exhibits antimicrobial activity against Gram positive bacteria, including vancomycin- and linezolide-resistant species. Analogues of platensimycin were synthesized from 3-aminobenzoic acid or other aniline derivatives and ...

journal_title：Archiv der Pharmazie

authors： Krauss J,Knorr V,Manhardt V,Scheffels S,Bracher F

更新日期：2008-06-01 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：: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：:Fifteen new indazole derivatives have been synthesized. In the Born test, compounds (4f) and (4g) were most active. They inhibited the blood platelet aggregation induced by collagen with an IC(50) = 85 or 90 microM, respectively. After oral administration to rats (60 mg/kg) three of the compounds significantly inhibit...

journal_title：Archiv der Pharmazie

authors： Yildiz AK,Rehse K,Stasch JP,Bischoff E

更新日期：2004-06-01 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：: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：:New phosphoramide mustards (6-8) have been prepared from the antibiotics 2 and 3, and from 5. The mixture of cyclophosphamides could be separated by preparative layer and column chromatography. The assignments of configuration to the isomeric phosphoramidates was based on the magnetic anisotropy of the P = O bond. The...

journal_title：Archiv der Pharmazie

authors： Csorvási A,Kövér KE,Menyhárt MM,Sztaricskai F,Dobrynin YV,Nikolaeva TG

更新日期：1998-09-01 00:00:00

abstract：:The synthesis and the pharmacological properties of some new prazosin analogues are described. ...

journal_title：Archiv der Pharmazie

authors： Rampa A,Valenti P,Da Re P,Carrara M,Zampiron S,Cima L,Giusti P

更新日期：1989-06-01 00:00:00