- The synthesis of phenylalanine-derived C5-substituted rhodanines and their activity against selected methicillin-resistant Staphylococcus aureus (MRSA) strains
[作者:Hardej, D; Ashby, CR; Khadtare, NS; Kulkarni, SS; Singh, S; Talele, TT,期刊:European Journal of Medicinal Chemistry, 页码:5827-5832 , 文章类型: Article,,卷期:2010年45-12]
- A series of rhodanine compounds containing various substituents at the N3- and C5-positions were synthesized and their in vitro activity against a panel of clinically relevant MRSA strains was determined. The anti-MRSA a...
- Synthesis, biological activity, and evaluation of the mode of action of novel antitubercular benzofurobenzopyrans substituted on A ring
[作者:Termentzi, A; Khouri, I; Gaslonde, T; Prado, S; Saint-Joanis, B; Bardou, F; Amanatiadou, EP; Vizirianakis, IS; Kordulakova, J; Jackson, M; Brosch, R; Janin, YL; Daffe, M; Tillequin, F; Michel, S,期刊:European Journal of Medicinal Chemistry, 页码:5833-5847 , 文章类型: Article,,卷期:2010年45-12]
- The 8-, 9-, 10-, and 11-halo, hydroxy, and methoxy derivatives of the antimycobacterial 3,3-dimethyl-3H-benzofuro[3,2-f][1]benzopyran were synthesized by condensation of the diazonium salts of 2-chloroani-lines (13-17) w...
- Post Groebke-Blackburn multicomponent protocol: Synthesis of new polyfunctional imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrimidine derivatives as potential antimicrobial agents
[作者:Al-Tel, TH; Al-Qawasmeh, RA,期刊:European Journal of Medicinal Chemistry, 页码:5848-5855 , 文章类型: Article,,卷期:2010年45-12]
- New antimicrobial agents [imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrimidine] have been synthesized. Their antimicrobial activities were conducted against various Gram-positive and Gram-negative bacteria including Staph...
- Synthesis, antitrichinnellosis and antiprotozoal activity of some novel thieno[2,3-d]pyrimidin-4(3H)-ones containing benzimidazole ring
[作者:Mavrova, AT; Vuchev, D; Anichina, K; Vassilev, N,期刊:European Journal of Medicinal Chemistry, 页码:5856-5861 , 文章类型: Article,,卷期:2010年45-12]
- Some novel thieno[2,3-d]pyrimidin-4(3H)-ones containing benzimidazol-2-yl-thioethyl- and benzimidazol-2-yl-methanethioethyl moiety in second position of the pyrimidine ring were synthesized in order to determine their an...
- Molecular properties prediction, synthesis and antimicrobial activity of some newer oxadiazole derivatives
[作者:Bakht, MA; Yar, MS; Abdel-Hamid, SG; Al Qasoumi, SI; Samad, A,期刊:European Journal of Medicinal Chemistry, 页码:5862-5869 , 文章类型: Article,,卷期:2010年45-12]
- In present investigation a series of 28 oxadiazole analogues (AB1-AB28) were subjected to molecular properties prediction, drug-likeness by Molinspiration (Molinspiration, 2008) & MolSoft (MolSoft, 2007) softwares, lipop...
- Synthesis and anticonvulsant activity of N-3-arylamide substituted 5,5-cyclopropanespirohydantoin derivatives
[作者:He, XR; Zhong, M; Zhang, T; Wu, W; Wu, ZY; Yang, J; Xiao, YL; Pan, YH; Qiu, GF; Hu, XM,期刊:European Journal of Medicinal Chemistry, 页码:5870-5877 , 文章类型: Article,,卷期:2010年45-12]
- In the present study on the development of new anticonvulsants, twenty new N-3-arylamide substituted 5,5-cyclopropanespirohydantoin derivatives were synthesized and tested for anticonvulsant activity using the maximal el...
- Synthesis and biological evaluation of new N-alkyl 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides as cannabinoid receptor ligands
[作者:Silvestri, R; Ligresti, A; La Regina, G; Piscitelli, F; Gatti, V; Lavecchia, A; Brizzi, A; Pasquini, S; Allara, M; Fantini, N; Carai, MAM; Bigogno, C; Rozio, MG; Sinisi, R; Novellino, E; Colombo, G; Di Marzo, V; Dondio, G; Corelli, F,期刊:European Journal of Medicinal Chemistry, 页码:5878-5886 , 文章类型: Article,,卷期:2010年45-12]
- A series of N-alkyl 1-ary1-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides were synthesized as new ligands of the human recombinant receptor hCB(1). n-Alkyl carboxamides brought out different SARs from the branched subgrou...
- Design, synthesis and structure-activity relationship study of novel pyrazole-based heterocycles as potential antitumor agents
[作者:Farag, AM; Ali, KAK; El-Debss, TMA; Mayhoub, AS; Amr, AGE; Abdel-Hafez, NA; Abdulla, MM,期刊:European Journal of Medicinal Chemistry, 页码:5887-5898 , 文章类型: Article,,卷期:2010年45-12]
- The versatile hitherto unreported 3-[(E)-3-(dimethylamino)acryloyl]-1,5-diphenyl-1H-pyrazole-4-carbonitrile (3) was prepared via the reaction of 3-acetyl-1,5-diphenyl-1H-pyrazole-4-carbonitrile (1) with dimethylformamid-...
- Novel insights for dihydroorotate dehydrogenase class 1A inhibitors discovery
[作者:Cheleski, J; Rocha, JR; Pinheiro, MP; Wiggers, HJ; da Silva, ABF; Nonato, MC; Montanari, CA,期刊:European Journal of Medicinal Chemistry, 页码:5899-5909 , 文章类型: Article,,卷期:2010年45-12]
- The enzyme dihydroorotate dehydrogenase (DHODH) has been suggested as a promising target for the design of trypanocidal agents. We report here the discovery of novel inhibitors of Trypanosoma cruzi DHODH identified by a ...
- Design, synthesis and inhibitory activity against Mycobacterium tuberculosis thymidine monophosphate kinase of acyclic nucleoside analogues with a distal imidazoquinolinone
[作者:Familiar, O; Munier-Lehmann, H; Ainsa, JA; Camarasa, MJ; Perez-Perez, MJ,期刊:European Journal of Medicinal Chemistry, 页码:5910-5918 , 文章类型: Article,,卷期:2010年45-12]
- Thymidine monophosphate kinase from Mycobacterium tuberculosis (TMPKmt) has been proposed as an attractive target in the search of new agents to fight against tuberculosis. We recently reported that thymine derivatives c...
- Structure-based approach to nanomolar, water soluble matrix metalloproteinases inhibitors (MMPIs)
[作者:Attolino, E; Calderone, V; Dragoni, E; Fragai, M; Richichi, B; Luchinat, C; Nativi, C,期刊:European Journal of Medicinal Chemistry, 页码:5919-5925 , 文章类型: Article,,卷期:2010年45-12]
- N-Arylsulfonyl-based MMPs inhibitors (MMPIs) are among the most prominent inhibitors possessing nanomolar affinity. However, their poor bioavailability remains critical for the drug development of this family of molecule...
- Structure-cytotoxicity relationship in a series of N-phosphorus substituted E,E-3,5-bis(3-pyridinylmethylene)- and E,E-3,5-bis(4-pyridinylmethylene) piperid-4-ones
[作者:Leonova, ES; Makarov, MV; Rybalkina, EY; Nayani, SL; Tongwa, P; Fonari, A; Timofeeva, TV; Odinets, IL,期刊:European Journal of Medicinal Chemistry, 页码:5926-5934 , 文章类型: Article,,卷期:2010年45-12]
- In order to give further insight on the influence of the aromatic ring nature and the presence of the phosphorus substituent at the piperidone nitrogen atom of E,E-3,5-bis((hetero)arylidene)piperid-4-ones on their antitu...
- Antiarrhythmic, serotonin antagonist and antianxiety activities of novel substituted thiophene derivatives synthesized from 2-amino-4,5,6,7-tetrahydro-N-phenylbenzo[b]thiophene-3-carboxamide
[作者:Amr, AEGE; Sherif, MH; Assy, MG; Al-Omar, MA; Ragab, I,期刊:European Journal of Medicinal Chemistry, 页码:5935-5942 , 文章类型: Article,,卷期:2010年45-12]
- A series of novel thiophene derivatives 3-17 were synthesized by initial reactions of 2-amino-4,5,6,7-tetrahydro-N-phenylbenzo[b]thiophene-3-carboxamide I and 2-amino-4,5,6,7-tetrahydro-benzo[b] thiophene-3-carbonitrile ...
- Synthesis and antibacterial activity of C-12 pyrazolinyl spiro ketolides
[作者:Hu, L; Lan, P; Song, QL; Huang, ZJ; Sun, PH; Zhuo, CA; Wang, Y; Xiao, SN; Chen, WM,期刊:European Journal of Medicinal Chemistry, 页码:5943-5949 , 文章类型: Article,,卷期:2010年45-12]
- A series of C-12 pyrazolinyl Spiro ketolide derivatives were designed and synthesized. The C-12 modifications involved replacing the natural C-12 methyl group in clarithromycin core with different pyrazolinyl spiros via ...
- Design, synthesis and discovery of 5-hydroxyaurone derivatives as growth inhibitors against HUVEC and some cancer cell lines
[作者:Cheng, HM; Zhang, LW; Liu, YX; Chen, SP; Cheng, H; Lu, X; Zheng, ZX; Zhou, GC,期刊:European Journal of Medicinal Chemistry, 页码:5950-5957 , 文章类型: Article,,卷期:2010年45-12]
- A series of 4'-substituted 5-hydroxyaurone derivatives were synthesized and their inhibitory activities against the proliferation of endothelial cells and two cancer cell lines were studied. Some of these compounds funct...
- 2-Hydroxypropyl-beta-cyclodextrin strongly improves water solubility and anti-proliferative activity of pyrazolo[3,4-d]pyrimidines Src-Abl dual inhibitors
[作者:Dreassi, E; Zizzari, AT; Mori, M; Filippi, I; Belfiore, A; Naldini, A; Carraro, F; Santucci, A; Schenone, S; Botta, M,期刊:European Journal of Medicinal Chemistry, 页码:5958-5964 , 文章类型: Article,,卷期:2010年45-12]
- The main aim of this study was to enhance the solubility of pyrazolo[3,4-d]pyrimidines 1-8 able to strongly inhibit Src and Abl tyrosine kinase phosphorylation in cell-free assays and to significantly reduce leukemic and...
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