Synthesis and in-vitro inotropic evaluation of 2-(4-substitutedbenzyl-1,4-diazepan-1-yl)-N-(4,5-dihydro-1-phenyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamides.

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 synthesis of new bischromone derivatives (4a-c and 5a-c) as potential anticancer drugs is described. The difference in the reactivity between 4-oxo-4H-chromene-3-carboxylic acid 2 (or its methyl ester 3) and 4-oxo-4H-chromene-3-carbonyl chloride 1 with three different polyamines: 3,3'-diamino-N-methyldipropylamine...

journal_title：Archiv der Pharmazie

authors： Szulawska-Mroczek A,Szumilak M,Szczesio M,Olczak A,Nazarski RB,Lewgowd W,Czyz M,Stanczak A

更新日期：2013-01-01 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：:The synthesis of 4-Methoxyphenyl-[5-methyl-6-(2-(4-morpholinyl)-ethyl)-6H-thieno[2,3- b]pyrrol-4-yl)phenylmethanone (1), a thiophene analogue of the analgesic Pravadoline B, is described. Starting with the acetylprotected thienylhydrazine 2b compound 7 was obtained in a Fischer-analogue cyclication in two steps. Use o...

journal_title：Archiv der Pharmazie

authors： Binder D,Schnait H,Rovenszky F,Enzenhofer R,Stroissnig H

更新日期：1991-04-01 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：: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：:Three series of imidazolidinium ligands (NHC precursors) substituted with 4-vinylbenzyl, 2-methyl-1,4-benzodioxane, and N-propylphthalimide were synthesized. N-Heterocyclic carbene (NHC) precursors were prepared from N-alkylimidazoline and alkyl halides. The novel NHC precursors were characterized by 1 H NMR, 13 C NMR...

journal_title：Archiv der Pharmazie

authors： Aktaş A,Taslimi P,Gülçin İ,Gök Y

更新日期：2017-06-01 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：:3-Ethyl 5-methyl 1,4-dihydro-2-[(2-hydroxyethoxy) methyl]-6-methyl-4-(2,3-dichlorophenyl)-3,5-pyridinedicarboxylate (13), a bioisostere of amlodipine, was prepared by the reaction of ethyl 4-(2-hydroxyethoxy)acetoacetate (11) with methyl 2-(2,3-dichlorobenzylidene)acetoacetate (12) and NH4OAc. Compound 13 was elaborat...

journal_title：Archiv der Pharmazie

authors： Yiu SH,Knaus EE

更新日期：1999-10-01 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：:Cancer can invade or spread to almost all parts of the body. The increasing morbidity and high mortality of cancer create a great demand for the development of novel anticancer drugs. Coumarin derivatives are ubiquitous in nature and can readily interact with diverse enzymes and receptors in cancer cells via weak bond...

journal_title：Archiv der Pharmazie

authors： Song XF,Fan J,Liu L,Liu XF,Gao F

更新日期：2020-08-01 00:00:00

abstract：:36 Novel heterocyclic chalcone derivatives were synthesized and tested for their anti-bacterial activity. Some compounds presented good anti-microbial activities against Gram-positive bacteria (including the multidrug-resistant clinical isolates). This class of compounds presented high potency against Streptococcus mu...

journal_title：Archiv der Pharmazie

authors： Zheng CJ,Jiang SM,Chen ZH,Ye BJ,Piao HR

更新日期：2011-10-01 00:00:00

abstract：:Several derivatives of 1H-benzimidazole-2-carboxylic acid (BICA, 2a) were tested in vitro in comparison to 1H-indole-2-carboxylic acid (ICA, 1e) for their ability to displace [3H]glycine from rat hippocampal membranes. Compound 2a was 8 times more potent than 1e (Ki 5.3 microM, as compared to 42 microM). However, intr...

journal_title：Archiv der Pharmazie

authors： Berger ML,Schödl C,Noe CR

更新日期：1996-03-01 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：:Chemical modification of cinnoxacin was studied with the aim of improving its antibacterial activity and spectrum. A series of 4-imino-1, 4-dihydrocinnoline-3-carboxylic acid derivatives was synthesized and their in vitro antibacterial activity was evaluated. These derivatives were designed as isosteric analogues of f...

journal_title：Archiv der Pharmazie

authors： Stańczak A,Ochocki Z,Martynowski D,Główka M,Nawrot E

更新日期：2003-03-01 00:00:00

abstract：:In this study, the synthesis of a new series of 3,6-disubstituted-7H-1,2,4-triazolo[3,4-b][1,3,4]thiadiazine 1a-4c compounds derived from 4-amino-3-substituted-1,2,4-triazole-5-thiones 1-4 is described. All of the synthesized compounds were screened for their possible analgesic / anti-inflammatory, antioxidant activit...

journal_title：Archiv der Pharmazie

authors： Tozkoparan B,Aytaç SP,Aktay G

更新日期：2009-05-01 00:00:00

abstract：:Novel sulfur-containing glutethimide derivatives, substituted with either thiol or methylsulfide groups in the ortho/para positions of the aromatic ring, were synthesized and tested for both human placental aromatase and bovine adrenocortical desmolase inhibitory activities. The synthesis was achieved by the chlorosul...

journal_title：Archiv der Pharmazie

authors： Bednarski PJ,Hartmann RW

更新日期：1993-07-01 00:00:00

abstract：:Sixteen new 1-(2-methoxyphenyl)-4-(1-phenethylpiperidin-4-yl)piperazines and 1-(2-methoxyphenyl)-4-[(1-phenethylpiperidin-4-yl)methyl]piperazines were synthesized to be used as probes for mapping the dopamine D2 receptor (D2 DAR) arylpiperazine binding site. All compounds were evaluated for their affinity toward D2 DA...

journal_title：Archiv der Pharmazie

authors： Penjišević JZ,Šukalović VV,Andrić DB,Roglić GM,Šoškić V,Kostić-Rajačić SV

更新日期：2016-08-01 00:00:00

abstract：:The active form of vitamin D3, 1α,25(OH)2D3, plays a major role in maintaining calcium/phosphate homeostasis. In addition, it is a potent antiproliferative and pro-differentiating agent. Unfortunately, it usually causes hypercalcemia in vivo when effective antitumour doses are used. It has therefore been found necessa...

journal_title：Archiv der Pharmazie

authors： Ferronato MJ,Salomón DG,Fermento ME,Gandini NA,López Romero A,Rivadulla ML,Pérez-García X,Gómez G,Pérez M,Fall Y,Facchinetti MM,Curino AC

更新日期：2015-05-01 00:00:00

abstract：:Rapamycin, a potent antifungal antibiotic, was approved as immunosuppressant, and lately its derivatives have been developed into mTOR targeting anticancer drugs. Structure modification was performed at the C-42 position of rapamycin, and a novel series of rapamycin triazole hybrids (4a-d, 5a-e, 8a-e, and 9a-e) was fa...

journal_title：Archiv der Pharmazie

authors： Xie L,Huang J,Chen X,Yu H,Li K,Yang D,Chen X,Ying J,Pan F,Lv Y,Cheng Y

更新日期：2016-06-01 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：:Previously, we demonstrated that certain heterocyclic compounds derived from 3-substituted-1,2,4-triazole-5-thiones had promising analgesic/anti-inflammatory activities together with low ulcerogenic properties. Therefore, we sought to design and synthesize new derivatives of triazol-5-thiones-fused heterocycles. In th...

journal_title：Archiv der Pharmazie

authors： Sert-Ozgur S,Tel BC,Somuncuoglu EI,Kazkayasi I,Ertan M,Tozkoparan B

更新日期：2017-07-01 00:00:00

abstract：:With the purpose of expanding the structural variety of chemical compounds available as pharmacological tools for the treatment of Alzheimer's disease, we synthesized and evaluated a novel series of indole-benzoxazinones (Family I) and benzoxazine-arylpiperazine derivatives (Family II) for potential human acetylcholin...

journal_title：Archiv der Pharmazie

authors： Méndez-Rojas C,Quiroz G,Faúndez M,Gallardo-Garrido C,Pessoa-Mahana CD,Chung H,Gallardo-Toledo E,Saitz-Barría C,Araya-Maturana R,Kogan MJ,Zúñiga-López MC,Iturriaga-Vásquez P,Valenzuela-Gutiérrez C,Pessoa-Mahana H

更新日期：2018-05-01 00:00:00

abstract：:Rapamycin is an mTOR allosteric inhibitor with multiple functions such as immunosuppressive, anticancer, and lifespan prolonging activities. Its C-43 semi-synthetic derivatives temsirolimus and everolimus have been used as mTOR targeting anticancer drugs in the clinic. Following our previous research on antitumor rapa...

journal_title：Archiv der Pharmazie

authors： Huang Q,Xie L,Chen X,Yu H,Lv Y,Huang X,Ying J,Zheng C,Cheng Y,Huang J

更新日期：2018-11-01 00:00:00

abstract：:Novel thiazolyl hydrazonothiazolamines and 1,3,4-thiadiazinyl hydrazonothiazolamines were synthesized by a facile one-pot multicomponent approach by the reaction of 2-amino-4-methyl-5-acetylthiazole, thiosemicarbazide or thiocarbohydrazide and phenacyl bromides or 3-(2-bromoacetyl)-2H-chromen-2-ones in acetic acid wit...

journal_title：Archiv der Pharmazie

authors： Sujatha K,Ommi NB,Mudiraj A,Babu PP,Vedula RR

更新日期：2019-12-01 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：: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：: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 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：: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