Novel pyridine-2,4,6-tricarbohydrazide thiourea compounds as small key organic molecules for the potential treatment of type-2 diabetes mellitus: In vitro studies against yeast α- and β-glucosidase and in silico molecular modeling.

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：: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：:The syntheses, conformational studies, and investigations on the estrogen receptor binding of [R/S-1-(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]platinum(II) complexes (1-PtL2, 2L = leaving groups) are described. A Strecker synthesis using the 2,6-dichloro-4-methoxybenzaldehyde, NaCN, and NH4Cl afforded the cyanoami...

journal_title：Archiv der Pharmazie

authors： Gust R,Lubczyk V,Schmidt K,Shihada U

更新日期：2001-03-01 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：:Synthesis of a new series of 3,4-diarylpyrazole-1-carboxamide derivatives is described. Their antiproliferative activity against A375P human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The biological results indicated that five synthesized compounds (Ig...

journal_title：Archiv der Pharmazie

authors： El-Gamal MI,Choi HS,Cho HG,Hong JH,Yoo KH,Oh CH

更新日期：2011-11-01 00:00:00

abstract：:The 2-(2-Bromophenyl)-acetaldehyde acetals 8 are treated with n-BuLi and the aldehydes 7 and 11 to form the hydroxyacetales 9 and 12, respectively. 9 is cyclized under acidic conditions to the epoxybenzoxocine 2; analogously 12 yields the epoxydibenzoxocine 14. ...

journal_title：Archiv der Pharmazie

authors： Wünsch B

更新日期：1990-11-01 00:00:00

abstract：:Viral gastroenteritis is a serious viral infection which affects a large number of individuals around the world, most of them being children. The infection may occur due to different viruses, for example, coxsackievirus, adenovirus, and rotavirus. There is no available cure for such infections, and the treatment mainl...

journal_title：Archiv der Pharmazie

authors： Mohamed MS,Abd El-Hameed RH,Sayed AI,Soror SH

更新日期：2015-03-01 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：: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：: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：: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：:1-Acetylcarbazoles are readily converted to 3-desazacanthin-4-ones upon treatment with Bredereck's reagent, but in contrast to canthin-4-ones, these do not undergo ring transformation reactions with guanidine. Only after N-protection (methyl or 2-(trimethylsilyl)ethoxymethyl group), 2-desaza analogues of the alkaloid ...

journal_title：Archiv der Pharmazie

authors： Strödke B,Gehring AP,Bracher F

更新日期：2015-02-01 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：:Isatin and azole moieties, which have the ability to form various noncovalent interactions with different therapeutic targets, are common pharmacophores in drug development. Isatin and azole derivatives possess promising in vitro and in vivo anticancer activity, and many of them, such as semaxanib, sunitinib, and carb...

journal_title：Archiv der Pharmazie

authors： Hou Y,Shang C,Wang H,Yun J

更新日期：2020-01-01 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：:10 is a beta-carboline analogue of the neuroleptic flutroline2a,b) with significant lower affinity at the dopamine D2 binding site. Various synthetic routes to 10 and the solid state structure of 8 are described, structure activity relations, in particular the importance of the "S-shape" and the rigid dopamine conform...

journal_title：Archiv der Pharmazie

authors： Lehmann J,Knoch F,Jiang N

更新日期：1993-12-01 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：:Ten pyrazole derivatives were synthesized and evaluated for their ability to inhibit the replication of influenza virions. All the compounds were synthesized in good-to-excellent yield, and the structures were ascertained with the help of (1) H NMR, (13) C NMR, mass, and elemental analysis. Among the tested series, co...

journal_title：Archiv der Pharmazie

authors： Meng FJ,Sun T,Dong WZ,Li MH,Tuo ZZ

更新日期：2016-03-01 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：:Both 2-nitrooxymethyl-4-phenyl- (2) and 4-nitrooxymethylphenyl-1,4-dihydropyridines (3) represent new combinations of two different vasodilating structures. 2 could not be isolated due to its spontaneous lactonization. Derivatives of 3 were obtained via Hantzsch synthesis using nitrooxymethylated benzaldehydes. The in...

journal_title：Archiv der Pharmazie

authors： Lehmann J,Kahlich R,Meyer zum Gottesberge C,Fricke U

更新日期：1997-08-01 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：: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：: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：:Despite cellular complexity, a limited number of small molecules act as intracellular second messengers. Protein kinase A (PKA) is the main transducer of the information carried by cyclic adenosine monophosphate (cAMP). Recently, cellular imaging has achieved major technical advancements, although the search for more ...

journal_title：Archiv der Pharmazie

authors： Ribaudo G,Zagotto G,Ongaro A,Ricci A,Caretta A,Mucignat-Caretta C

更新日期：2020-04-01 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：:The aim of this study was to develop a novel nanosize drug candidate for cancer therapy. For this purpose, (S)-methyl 2-[(7-hydroxy-2-oxo-4-phenyl-2H-chromen-8-yl)methyleneamino]-3-(1H-indol-3-yl)propanoate (ND3) was synthesized by the condensation reaction of 8-formyl-7-hydroxy-4-phenylcoumarin with l-tryptophan meth...

journal_title：Archiv der Pharmazie

authors： Budama-Kilinc Y,Kecel-Gunduz S,Ozdemir B,Bicak B,Akman G,Arvas B,Aydogan F,Yolacan C

更新日期：2020-11-01 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：:Herein, we report the synthesis of novel tetrahydro-β-carbolines that induce cell death via the autophagic pathway. Five of the new compounds induced cell death in a panel of patient-derived human metastatic melanoma cells. The autophagic pathway was confirmed using LC3 autophagosome markers; the involvement of ATG7 a...

journal_title：Archiv der Pharmazie

authors： Ahmed NS,Elgendy M,Laufer S,Abadi AH

更新日期：2014-06-01 00:00:00

abstract：:The plant pentacyclic alkaloid camptothecin and its structural analogs were extensively studied. These compounds are interesting due to the antitumor activity associated with their ability to inhibit topoisomerase I in tumor cells. During the last decades of the 20th century, a large number of the silicon-containing c...

journal_title：Archiv der Pharmazie

authors： Lazareva NF,Baryshok VP,Lazarev IM

更新日期：2018-01-01 00:00:00

abstract：:Furfurylidenemalononitriles and thienylidenemalononitriles were treated with 1,3-cyclohexanediones to afford 2-amino-4-hetaryl-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile derivatives. The molluscicidal activity of these compounds was investigated. ...

journal_title：Archiv der Pharmazie

authors： Abdelrazek FM,Metz P,Farrag EK

更新日期：2004-09-01 00:00:00