- Synthesis, antibacterial evaluation and QSAR studies of 7-[4-(5-aryl-1,3,4-oxadiazole-2-yl)piperazinyl] quinolone derivatives
[作者:Kumar, R; Kumar, A; Jain, S; Kaushik, D,期刊:European Journal of Medicinal Chemistry, 页码:3543-3550 , 文章类型: Article,,卷期:2011年46-9]
- A series of 7-[4-(5-aryl-1,3,4-oxadiazole-2-yl)piperazinyl] quinolones (I-XXI) were synthesized using an appropriate synthetic route and characterized by elemental and spectral analysis. The antibacterial activities of a...
- Design, synthesis and anti-tubercular evaluation of new 2-acylated and 2-alkylated amino-5-(4-(benzyloxy)phenyl)thiophene-3-carboxylic acid derivatives. Part 1
[作者:Lu, XY; Wan, BJ; Franzblau, SG; You, QD,期刊:European Journal of Medicinal Chemistry, 页码:3551-3563 , 文章类型: Article,,卷期:2011年46-9]
- A series of 2-acylated and 2-alkylated amino-5-(4-(benzyloxy)phenyl)thiophene-3-carboxylic acid derivatives were synthesized and evaluated for anti-tubercular activity. Among these compounds, 10d, 15, 12h and 12k inhibit...
- Design, synthesis, bioconversion, and pharmacokinetics evaluation of new ester prodrugs of olmesartan
[作者:Chang, JS; El-Gamal, MI; Lee, WS; Anbar, HS; Chung, HJ; Kim, HI; Cho, YJ; Lee, BS; Lee, SA; Moon, JY; Lee, DJ; Jeon, HR; Lee, J; Choi, YW; Oh, CH,期刊:European Journal of Medicinal Chemistry, 页码:3564-3569 , 文章类型: Article,,卷期:2011年46-9]
- Synthesis of new ester prodrugs of olmesartan is described. Their in vitro stabilities in simulated gastric juice, rat plasma, and rat liver microsomes were tested. And the pharmacokinetic parameters for olmesartan after...
- Design, synthesis and antiproliferative activities of biarylolefins based on polyhydroxylated and carbohydrate scaffolds
[作者:Novoa, A; Pellegrini-Moise, N; Bourg, S; Thoret, S; Dubois, J; Aubert, G; Cresteil, T; Chapleur, Y,期刊:European Journal of Medicinal Chemistry, 页码:3570-3580 , 文章类型: Article,,卷期:2011年46-9]
- A series of diversely substituted biarylolefins based on carbohydrate and dihydroxyethylene scaffolds were synthesized and evaluated for antiproliferative activity against a panel of human tumor cell lines. Among the thi...
- In-vitro metabolic inhibition and antifertility effect facilitated by membrane alteration: Search for novel antifertility agent using nifedipine analogues
[作者:Waghmare, A; Kanyalkar, M; Joshi, M; Srivastava, S,期刊:European Journal of Medicinal Chemistry, 页码:3581-3589 , 文章类型: Article,,卷期:2011年46-9]
- In search of non-hormonal male contraceptives, analogues of nifedipine, which causes reversible infertility, have been synthesized and their interaction at molecular level with model membrane has been probed. Analogues a...
- Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones
[作者:Drabczynska, A; Yuzlenko, O; Kose, M; Paskaleva, M; Schiedel, AC; Karolak-Wojciechowska, J; Handzlik, J; Karcz, T; Kuder, K; Muller, CE; Kiec-Kononowicz, K,期刊:European Journal of Medicinal Chemistry, 页码:3590-3607 , 文章类型: Article,,卷期:2011年46-9]
- Syntheses and physicochemical properties of N-cycloalkyl-substituted imidazo-, pyrimido- and 1,3-diazepino[2,1-f]purinediones are described. These derivatives were synthesized by cyclization of 7-halogenoalkyl-8-bromo-1,...
- 7-Substituted pterins provide a new direction for ricin A chain inhibitors
[作者:Pruet, JM; Jasheway, KR; Manzano, LA; Bai, Y; Anslyn, EV; Robertus, JD,期刊:European Journal of Medicinal Chemistry, 页码:3608-3615 , 文章类型: Article,,卷期:2011年46-9]
- Ricin is a potent toxin found in castor seeds. The A chain, RTA, enzymaticlly depurinates a specific adenosine in ribosomal RNA, inhibiting protein synthesis. Ricin is a known chemical weapons threat having no effective ...
- A new nitrosyl ruthenium complex: Synthesis, chemical characterization, in vitro and in vivo antitumor activities and probable mechanism of action
[作者:Heinrich, TA; Von Poelhsitz, G; Reis, RI; Castellano, EE; Neves, A; Lanznaster, M; Machado, SP; Batista, AA; Costa-Neto, CM,期刊:European Journal of Medicinal Chemistry, 页码:3616-3622 , 文章类型: Article,,卷期:2011年46-9]
- This study describes the synthesis of a new ruthenium nitrosyl complex with the formula [RuCl(2)NO(BPA)] [BPA = (2-hydroxybenzyl)(2-methylpyridyl)amine ion], which was synthesized and characterized by spectroscopy, cycli...
- Discovery of 6-substituted indole-3-glyoxylamides as lead antiprion agents with enhanced cell line activity, improved microsomal stability and low toxicity
[作者:Thompson, MJ; Louth, JC; Ferrara, S; Jackson, MP; Sorrell, FJ; Cochrane, EJ; Gever, J; Baxendale, S; Silber, BM; Roehl, HH; Chen, BN,期刊:European Journal of Medicinal Chemistry, 页码:4125-4132 , 文章类型: Article,,卷期:2011年46-9]
- A series of highly potent indole-3-glyoxylamide based antiprion agents was previously characterized, focusing on optimization of structure-activity relationship (SAR) at positions 1-3 of the indole system. New libraries ...
- Cationic lipids containing protonated cyclen and different hydrophobic groups linked by uracil-PNA monomer: Synthesis and application for gene delivery
[作者:Liu, JL; Ma, QP; Huang, QD; Yang, WH; Zhang, J; Wang, JY; Zhu, W; Yu, XQ,期刊:European Journal of Medicinal Chemistry, 页码:4133-4141 , 文章类型: Article,,卷期:2011年46-9]
- In this report, as candidates for non-viral gene vectors, cationic lipids L1, L2 and L3 based on protonated cyclen and different hydrophobic groups (cholesterol, dodecanol or diosgenin) linked by PNA monomer were designe...
- Metronidazole prodrugs: Synthesis, physicochemical properties, stability, and ex vivo release studies
[作者:Mura, C; Valenti, D; Floris, C; Sanna, R; De Luca, MA; Fadda, AM; Loy, G,期刊:European Journal of Medicinal Chemistry, 页码:4142-4150 , 文章类型: Article,,卷期:2011年46-9]
- The aim of the present study was to develop a colon targeted delivery system for metronidazole using polymeric prodrug formulation. Two chitosan amide conjugates of metronidazole were prepared by using two different spac...
- 3-Aryl-2-[1H-benzotriazol-1-yl]acrylonitriles: A novel class of potent tubulin inhibitors
[作者:Carta, A; Briguglio, I; Piras, S; Boatto, G; La Colla, P; Loddo, R; Tolomeo, M; Grimaudo, S; Di Cristina, A; Pipitone, RM; Laurini, E; Paneni, MS; Posocco, P; Fermeglia, M; Pricl, S,期刊:European Journal of Medicinal Chemistry, 页码:4151-4167 , 文章类型: Article,,卷期:2011年46-9]
- During a screening for compounds that could act against Mycobacterium tuberculosis, a series of new cellular antiproliferative agents was identified. The most cytotoxic molecules were evaluated against a panel of human c...
- Synthesis, structural and spectroscopic characterization, in vitro cytotoxicity and in vivo activity as free radical scavengers of chlorido(p-cymene) complexes of ruthenium(II) containing N-alkylphenothiazines
[作者:Krstic, M; Sovilj, SP; Grguric-Sipka, S; Evans, IR; Borozan, S; Santibanez, JF,期刊:European Journal of Medicinal Chemistry, 页码:4168-4177 , 文章类型: Article,,卷期:2011年46-9]
- Three new ruthenium(II) complexes 1-3 containing N-alkylphenothiazine molecules were synthesized by reaction of [RuCl(2)(eta(6)-P-cymene)](2) with chlorpromazine hydrochloride (1), trifluoperazine dihydrochloride (2) or ...
- Synthesis of new 2 '-deoxy-2 '-fluoro-4 '-azido nucleoside analogues as potent anti-HIV agents
[作者:Wang, Q; Hu, WD; Wang, SY; Pan, ZL; Tao, L; Guo, XH; Qian, KD; Chen, CH; Lee, KH; Chang, JB,期刊:European Journal of Medicinal Chemistry, 页码:4178-4183 , 文章类型: Article,,卷期:2011年46-9]
- We prepared 1-(4'-azido-2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl)cytosine (10) and its hydrochloride salt (11) as potential antiviral agents based on the favorable antiviral profiles of 4'-substituted nucleosides. Comp...
- Targeting the human malaria parasite Plasmodium falciparum: In vitro identification of a new antiplasmodial hit in 4-phenoxy-2-trichloromethylquinazoline series
[作者:Castera-Ducros, C; Azas, N; Verhaeghe, P; Hutter, S; Garrigue, P; Dumetre, A; Mbatchi, L; Laget, M; Remusat, V; Sifredi, F; Rault, S; Rathelot, P; Vanelle, P,期刊:European Journal of Medicinal Chemistry, 页码:4184-4191 , 文章类型: Article,,卷期:2011年46-9]
- From the promising results we previously obtained in quinazoline series and to complete the evaluation of the in vitro antiplasmodial activity of original 2-trichloromethylquinazolines, we synthesized new quinazolines po...
- Synthesis and identification of beta-aryloxyquinolines and their pyrano[3,2-c] chromene derivatives as a new class of antimicrobial and antituberculosis agents
[作者:Mungra, DC; Patel, MR; Rajani, DP; Patel, RG,期刊:European Journal of Medicinal Chemistry, 页码:4192-4200 , 文章类型: Article,,卷期:2011年46-9]
- A new class of beta-aryloxyquinolines 3a-i and their pyrano[3,2-c]chromene derivatives 6a-r incorporating a validated molecular target has been synthesized via a nucleophilic displacement and a one-pot multicomponent rea...
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