Design, synthesis, and biological evaluation of novel tetrahydroprotoberberine derivatives to reduce SREBPs expression for the treatment of hyperlipidemia.

abstract：:We have previously described the potent and selective (RS)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor agonist, (RS)-2-amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic acid (ACPA), and the AMPA receptor antagonist (RS)-2-amino-3-[3-(carboxymethoxy)-5-methyl-4-isoxazolyl]propionic acid (...

journal_title：European journal of medicinal chemistry

authors： Madsen U,Sløk FA,Stensbøl TB,Bräuner-Osborne H,Lützhøft HH,Poulsen MV,Eriksen L,Krogsgaard-Larsen P

更新日期：2000-01-01 00:00:00

abstract：:In order to investigate the origin of the loop-type diuretic activity of M17055 (1), several variants (3-9) were designed and synthesized by modifying the quinolinone skeleton, and their diuretic activities were compared with the lead 1 and furosemide in dogs. It was found that the negative charge distribution pattern...

journal_title：European journal of medicinal chemistry

authors： Nishijima K,Nishida H,Yamashita Y,Ito M,Onuki Y,Mizota M,Miyano S

更新日期：2000-02-01 00:00:00

abstract：:Histidine decarboxylase catalyses the decarboxylation of l-histidine to histamine using pyridoxal-5'-phosphate (PLP) as coenzyme. The PM3 quantum mechanical conformation method of analysis and heat of formation calculation were carried out for intermediates which are probably formed during the interaction of histidine...

journal_title：European journal of medicinal chemistry

authors： Tahanejad FS,Naderi-Manesh H

更新日期：2000-03-01 00:00:00

abstract：:A group of new 4-[2-(7-heterocyclemethoxynaftalen-2-ylmethoxy)ethyl]benzoic acids have been synthesized and pharmacologically evaluated as LTD(4)-antagonists. Thiazole derivatives, especially 4-[2-[7-(4-cyclobutylthiazole-2-ylmethoxyl)naphthalen- 2-ylmetho-xy]et hyl]benzoic acid, present considerable activity and impr...

journal_title：European journal of medicinal chemistry

authors： Ballart B,Martí J,Velasco D,López-Calahorra F,Pascual J,Luisa García M,Cabré F,Mauleón D

更新日期：2000-04-01 00:00:00

abstract：:The synthesis of a group of 2-phenylimidazo[1,2-b]pyridazine-3-acetic esters and acids is described. The structures of the new compounds are supported by 1H-NMR spectra. These compounds were tested in vivo for their anti-inflammatory, analgesic and ulcerogenic activity. All new compounds showed remarkable anti-inflamm...

journal_title：European journal of medicinal chemistry

authors： Sacchi A,Laneri S,Arena F,Abignente E,Gallitelli M,D'amico M,Filippelli W,Rossi F

更新日期：1999-11-01 00:00:00

abstract：:Some 1-(4-arylthiazol-2-yl)-3,5-diaryl-2-pyrazoline derivatives were synthesized by reacting 1-thiocarbamoyl-3,5-diaryl-2-pyrazoline derivatives with phenacetylbromide in ethanol. The structural elucidation of the compounds were performed by IR, 1H-NMR and Mass spectral data and elemental analyses. The hypotensive act...

journal_title：European journal of medicinal chemistry

authors： Turan-Zitouni G,Chevallet P,Kiliç FS,Erol K

更新日期：2000-06-01 00:00:00

abstract：:Several aldehydes related to methyl 9-deoxy-9-oxo-alpha-apopicropodophyllate, a selective antitumour agent against the HT-29 colon carcinoma, have been prepared and evaluated for their cytotoxic activities on four neoplastic cell lines (P-388, A-549, HT-29 and MEL-28). All of them lacked the lactone ring but maintaine...

journal_title：European journal of medicinal chemistry

authors： Gordaliza M,Castro MA,Miguel del Corral JM,López-Vázquez ML,A García P,García-Grávalos MD,San Feliciano A

更新日期：2000-07-01 00:00:00

abstract：:The synthesis and evaluation of the biological activity of new 4-chloro-5-¿4-[2-(2-methoxyphenoxy)-ethyl]-1-piperazinyl¿-3(2H)-pyrid azinone derivatives are reported. The blocking activity of these compounds was determined on the pre- and postsynaptic alpha-adrenoceptors of isolated rat vas deferens. ...

journal_title：European journal of medicinal chemistry

authors： Strappaghetti G,Barbaro R,Marucci G

更新日期：2000-07-01 00:00:00

abstract：:A group of 9-substituted acridine and azacridine derivatives (m-AMSA analogues) were synthesised following classical procedures as potential antitumour agents with inhibitory effects on DNA topoisomerase II. Some were found to have noticeable cytotoxicity against human HL-60 and HeLa cells grown in culture. Their non-...

journal_title：European journal of medicinal chemistry

authors： Ferlin MG,Marzano C,Chiarelotto G,Baccichetti F,Bordin F

更新日期：2000-09-01 00:00:00

abstract：:Di- and tripeptide analogues containing alpha-ketoamide as a new core structure and incorporating allophenylnorstatine (Apns) as a transition state mimic, were designed and synthesized in the hope of obtaining a novel structural type of HIV-1 protease inhibitors. The immediate precursor, Apns-Thz-NHBu(t) was prepared ...

journal_title：European journal of medicinal chemistry

authors： Sheha MM,Mahfouz NM,Hassan HY,Youssef AF,Mimoto T,Kiso Y

更新日期：2000-10-01 00:00:00

abstract：:The syntheses, structural elucidation based on NMR spectroscopy and X-ray analysis of 8 as well as antitumor activities of novel 2,4-diamino-1,3,5-triazine derivatives 5 and 7-22 are described. Screenings performed at NCI showed that most derivatives possessed a moderate to strong growth inhibition activity on various...

journal_title：European journal of medicinal chemistry

authors： Brzozowski Z,Saczewski F,Gdaniec M

更新日期：2000-12-01 00:00:00

abstract：:Metal complexes of a sulfonamide possessing strong carbonic anhydrase (CA) inhibitory properties have been obtained from the sodium salt of the sulfonamide or from the free sulfonamide in the presence of ammonia, and the following metal ions: Mg(II); Zn(II); Mn(II); Cu(II); Co(II); Ni(II); Be(II); Cd(II); Pb(II); Al(I...

journal_title：European journal of medicinal chemistry

authors： Supuran CT,Scozzafava A,Mincione F,Menabuoni L,Briganti F,Mincione G,Jitianu M

更新日期：1999-07-01 00:00:00

abstract：:In the search for new agents with estrogenic activity mediated by estrogen receptors (ER), six 6,12-dihydro-1-benzopyrano[3,4-b][1,4]benzothiazin-6-ones 3a-f were synthesized. These compounds were readily prepared by the addition of 2-aminothiophenol 2 to substituted 4-hydroxycoumarin derivatives 1a-e. The estrogenic ...

journal_title：European journal of medicinal chemistry

authors： Jacquot Y,Bermont L,Giorgi H,Refouvelet B,Adessi GL,Daubrosse E,Xicluna A

更新日期：2001-02-01 00:00:00

abstract：:A group of imidazo[1,2-a]quinoxalines have been synthesised from quinoxaline by condensation of an appropriate haloester or intramolecular cyclisation of a keto moiety on an intracyclic nitrogen atom. The reactivity of the heterocycle was explored through diverse reactions such as electrophilic substitution, lithiatio...

journal_title：European journal of medicinal chemistry

authors： Parra S,Laurent F,Subra G,Deleuze-Masquefa C,Benezech V,Fabreguettes J,Vidal J,Pocock T,Elliott K,Small R,Escale R,Michel A,Chapat J,Bonnet P

更新日期：2001-03-01 00:00:00

abstract：:New carbocylic analogues of distamycin and netropsin with chlorambucil moieties 5-8 have been synthesised. Data from the ethidium displacement assay showed that these compounds bind in the minor groove of DNA. The observed reduced affinity to AT pairs and increased affinity towards GC sequences of the carbocyclic lexi...

journal_title：European journal of medicinal chemistry

authors： Bartulewicz D,Bielawski K,Bielawska A,Rózański A

更新日期：2001-05-01 00:00:00

abstract：:New compounds with naphtho-fused systems were synthesized and evaluated as antitumor agents. The naphtho-fused systems 6 and 7, synthesized from the hydroxy-acetal, exhibit antitumor activity. The bis(phenylthio) derivatives were considered as possible precursors for lignan lactones (11). The hydroxy-naphthalen 6 show...

journal_title：European journal of medicinal chemistry

authors： Capilla AS,Sánchez I,Caignard DH,Renard P,Pujol MD

更新日期：2001-04-01 00:00:00

abstract：:Ten new 3,5-diphenyl-2-pyrazoline derivatives were synthesised by reacting 1,3-diphenyl-2-propen-1-one with hydrazine hydrate. The chemical structures of the compounds were proved by means of their IR, 1H-NMR spectroscopic data and microanalyses. The antidepressant activities of these compounds were evaluated by the '...

journal_title：European journal of medicinal chemistry

authors： Palaska E,Aytemir M,Uzbay IT,Erol D

更新日期：2001-06-01 00:00:00

abstract：:Ethylenediamine was reacted with suitable aromatic aldehydes in order to prepare their respective diSchiff bases. These compounds were then reduced to give the corresponding tetrahydrodiSchiff bases, which were low melting in nature. Finally, these derivatives were condensed with different aromatic aldehydes to give t...

journal_title：European journal of medicinal chemistry

authors： Sharma V,Khan MS

更新日期：2001-07-01 00:00:00

abstract：:A number of selected imidazo[2,1-b]thiazoles entered the screening at the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF) and one of these compounds, 2-chloro-6-phenylimidazo[2,1-b]thiazole, showed antitubercular activity. On this basis we planned the synthesis of new analogues bearing a subst...

journal_title：European journal of medicinal chemistry

authors： Andreani A,Granaiola M,Leoni A,Locatelli A,Morigi R,Rambaldi M

更新日期：2001-09-01 00:00:00

abstract：:Indole-3-carbinol is a natural product which has been shown to reduce the incidence of spontaneous and carcinogen-induced mammary tumours in animals. Eighteen unsymmetrical methylene derivatives of indoles were prepared by reaction of Mannich bases of 7-hydroxycoumarins with substituted indoles in acetic or propionic ...

journal_title：European journal of medicinal chemistry

authors： Mazzei M,Miele M,Nieddu E,Barbieri F,Bruzzo C,Alama A

更新日期：2001-11-01 00:00:00

abstract：:Synthesis of 1,3-disubstituted indoles derivatives as potential glycoprotein (GP) IIb/IIIa antagonists was reported. Substitution of the indolic nitrogen atom by piperidino or benzamidino moieties was used as mimics of an arginine residue. The acid carboxylic group was linked to the indole scaffold in position-3 via a...

journal_title：European journal of medicinal chemistry

authors： Grumel V,Mérour JY,Lesur B,Giboulot T,Frydman A,Guillaumet G

更新日期：2002-01-01 00:00:00

abstract：:A series of 36 phenoxypropanolamines was examined to determine the structure--activity relationships of beta-adrenoceptor (beta-AR) antagonists for the human beta(1)-AR. The binding affinities of all the compounds were determined for human beta(1)-ARs expressed in Chinese hamster ovary cells and the antagonist potency...

journal_title：European journal of medicinal chemistry

authors： Louis SN,Rezmann-Vitti LA,Nero TL,Iakovidis D,Jackman GP,Louis WJ

更新日期：2002-02-01 00:00:00

abstract：:Two novel series of 4-thiazolidinone derivatives, namely 2-substituted-3-([4-(4-methoxybenzoylamino)benzoyl]amino)-4-thiazolidinones (7a-e) and 2-[4-(4-methoxybenzoylamino)benzoylhydrazono]-3-alkyl-4-thiazolidinones (5a-c) together with 2-[4-(4-methoxybenzoylamino)phenyl]-5-(substituted phenyl)amino-1,3,4-oxadiazoles ...

journal_title：European journal of medicinal chemistry

authors： Küçükgüzel SG,Oruç EE,Rollas S,Sahin F,Ozbek A

更新日期：2002-03-01 00:00:00

abstract：:Two new nitrosoureas (TNUs), containing tyrosine derivatives as carriers of nitrosourea cytotoxic group have been synthesised. The physicochemical properties such as half-life time (tau(0.5)), alkylating and carbamoylating activities were determined. The nitrosoureas showed a higher inhibiting effect on the DOPA-oxida...

journal_title：European journal of medicinal chemistry

authors： Gadjeva V

更新日期：2002-04-01 00:00:00

abstract：:Artificial membrane permeability measurement is a potentially high throughput and low cost alternative for in vitro assessment of drug absorption potential. It will be an ideal screening/profiling tool in the lead generation program of drug discovery research if it is proven to be generally applicable for classifying ...

journal_title：European journal of medicinal chemistry

authors： Zhu C,Jiang L,Chen TM,Hwang KK

更新日期：2002-05-01 00:00:00

abstract：:A series of hydrazones of 1,2-benzisothiazole hydrazides 1a-m, 2a-m, 3a-m, 4a-m, 5a-m as well as their cyclic (1 and 4) and acyclic (2, 3 and 5) 1,2-benzisothiazole parent hydrazides, were synthesised and evaluated as antibacterial and antifungal agents. All of the 2-amino-1,2-benzisothiazol-3(2H)-one derivatives, bel...

journal_title：European journal of medicinal chemistry

authors： Vicini P,Zani F,Cozzini P,Doytchinova I

更新日期：2002-07-01 00:00:00

abstract：:1,3-Diphenylpyrazole-4-carboxaldehyde and 1-(4-nitrophenyl)-3-phenylpyrazole-4-carboxaldehyde were obtained from the appropriated phenylhydrazones via the Vilsmeier-Haack reaction. These two aldehydes were functionalized by various substituted anilines or substituted benzylamines. Antiparasitic activities of the corre...

journal_title：European journal of medicinal chemistry

authors： Rathelot P,Azas N,El-Kashef H,Delmas F,Di Giorgio C,Timon-David P,Maldonado J,Vanelle P

更新日期：2002-08-01 00:00:00

abstract：:The synthesis of new planar derivatives characterised by the presence of an indolonaphthyridine nucleus, carrying a dimethylaminoethyl or a dimethylaminopropyl side chain is reported. The antiproliferative activity of the new products was tested by means of an in vitro assay on human tumour cell lines (HL-60 and HeLa)...

journal_title：European journal of medicinal chemistry

authors： Dalla Via L,Gia O,Marciani Magno S,Da Settimo A,Primofiore G,Da Settimo F,Simorini F,Marini AM

更新日期：2002-06-01 00:00:00

abstract：:A series of glycosylated beta-amino acids was prepared and evaluated against Mycobacterium tuberculosis, M. avium, M. fortuitum and M. smegmatis. The compounds were designed to mimic the enzyme D-alanine racemase and glycosyl transferase involved in the biosynthesis of essential cell wall peptidoglycan and arabinogala...

journal_title：European journal of medicinal chemistry

authors： Tripathi RP,Tripathi R,Tiwari VK,Bala L,Sinha S,Srivastava A,Srivastava R,Srivastava BS

更新日期：2002-09-01 00:00:00

abstract：:Several appropriately substituted 4-(dialkylamino-alkyl)-substituted-styryl-alkyl ketones or acetophenones were prepared and subjected to the Mannich reaction to yield compounds that would incorporate both alpha,beta-unsaturated keto groups and a substituted aminomethyl function with or without another olefinic moiety...

journal_title：European journal of medicinal chemistry

authors： Kumaria N,Dwivedi AK,Maikhuri JP,Gupta G,Habib S,Dhar JD,Singh S

更新日期：2002-11-01 00:00:00