- Topological sub-structural molecular design approach: Radical scavenging activity
[作者:Perez-Garrido, A; Helguera, AM; Ruiz, JMM; Rentero, PZ,期刊:European Journal of Medicinal Chemistry, 页码:86-94 , 文章类型: Article,,卷期:2012年49-1]
- In the last decades phenolic compounds have gained enormous interest because of their beneficial health effects such as anti-inflammatory, anticancer, or antiviral activities. The pharmacological effects of phenolic comp...
- 1,4-Diarylpiperazines and analogs as anti-tubercular agents: Synthesis and biological evaluation
[作者:Forge, D; Cappoen, D; Laurent, J; Stanicki, D; Mayence, A; Huang, TL; Verschaeve, L; Huygen, K; Vanden Eynde, JJ,期刊:European Journal of Medicinal Chemistry, 页码:95-101 , 文章类型: Article,,卷期:2012年49-1]
- Despite progress in modern chemotherapy to combat tuberculosis, the causative pathogen Mycobacterium tuberculosis (M.tb.) is far from eradicated. Bacillary resistance to anti-mycobacterial agents, bacillary persistence a...
- New inhibitors of dihydroorotate dehydrogenase (DHODH) based on the 4-hydroxy-1,2,5-oxadiazol-3-yl (hydroxyfurazanyl) scaffold
[作者:Lolli, ML; Giorgis, M; Tosco, P; Foti, A; Fruttero, R; Gasco, A,期刊:European Journal of Medicinal Chemistry, 页码:102-109 , 文章类型: Article,,卷期:2012年49-1]
- Based on some structural analogies with leflunomide and brequinar, two well-known inhibitors of dihydroorotate dehydrogenase (DHODH), a new series of products was designed, by joining the substituted biphenyl moiety to t...
- Preparation and optimization of PIT solid lipid nanoparticles via statistical factorial design
[作者:Carbone, C; Tomasello, B; Ruozi, B; Renis, M; Puglisi, G,期刊:European Journal of Medicinal Chemistry, 页码:110-117 , 文章类型: Article,,卷期:2012年49-1]
- The objective of this study was the preparation, physico-chemical characterization and statistical optimization of cationic solid lipid nanoparticles (SLN) prepared by the PIT method as potential carrier for gene therapy...
- Novel inhibitors of nitric oxide synthase with antioxidant properties
[作者:Salerno, L; Modica, MN; Romeo, G; Pittala, V; Siracusa, MA; Amato, ME; Acquaviva, R; Di Giacomo, C; Sorrenti, V,期刊:European Journal of Medicinal Chemistry, 页码:118-126 , 文章类型: Article,,卷期:2012年49-1]
- We previously described a series of imidazole-based inhibitors substituted at N-1 with an arylethanone chain as interesting inhibitors of neuronal nitric oxide synthase (nNOS), endowed with good selectivity vs endothelia...
- Molecular drug design, synthesis and crystal structure determination of Cu(II)-Sn(IV) heterobimetallic core: DNA binding and cleavage studies
[作者:Arjmand, F; Parveen, S; Afzal, M; Toupet, L; Ben Hadda, T,期刊:European Journal of Medicinal Chemistry, 页码:141-150 , 文章类型: Article,,卷期:2012年49-1]
- A novel heterobimetallic Cu(II)-Sn(IV) complex 1 bearing bioactive 1,10-phenanthroline pharmacophore ligand scaffold was synthesized and characterized by elemental analysis, IR, UV-vis spectroscopy, Mass (ESI and FAB) an...
- Novel metal based anti-tuberculosis agent: Synthesis, characterization, catalytic and pharmacological activities of copper complexes
[作者:Joseph, J; Nagashri, K; Janaki, GB,期刊:European Journal of Medicinal Chemistry, 页码:151-163 , 文章类型: Article,,卷期:2012年49-1]
- Copper complexes of molecular formulae, [CuL(1)(OAc)], [CuL(2)(H(2)O)], [CuL(3)(H(2)O)], [CuL(4)(H(2)O)], [CuL(5)(H(2)O)] where L(1)-L(5) represents Schiff base ligands by the condensation of 3-hydroxyflavone with 4-amin...
- Synthesis and evaluation of anti-tubercular and antibacterial activities of new 4-(2,6-dichlorobenzyloxy)phenyl thiazole, oxazole and imidazole derivatives. Part 2
[作者:Lu, XY; Liu, XB; Wan, BJ; Franzblau, SG; Chen, LL; Zhou, CL; You, QD,期刊:European Journal of Medicinal Chemistry, 页码:164-171 , 文章类型: Article,,卷期:2012年49-1]
- A series of substituted 4-(2,6-dichlorobenzyloxy)phenyl thiazole, oxazole and imidazole derivatives were synthesized. The derivatives were screened for in vitro anti-tubercular activities against Mycobacterium tuberculos...
- Design, synthesis of some new (2-aminothiazol-4-yl)methylester derivatives as possible antimicrobial and antitubercular agents
[作者:Karuvalam, RP; Haridas, KR; Nayak, SK; Row, TNG; Rajeesh, P; Rishikesan, R; Kumari, NS,期刊:European Journal of Medicinal Chemistry, 页码:172-182 , 文章类型: Article,,卷期:2012年49-1]
- A series of (2-aminothiazol-4-yl)methylester (5a-t) derivatives were synthesized in good yields and characterized by (1)H NMR, (13)C NMR, mass spectral and elemental analyses. The crystal structure of 5a was evidenced by...
- Design, synthesis and biological evaluation of 6-substituted aminocarbonyl benzimidazole derivatives as nonpeptidic angiotensin II AT(1) receptor antagonists
[作者:Wang, JL; Zhang, J; Zhou, ZM; Li, ZH; Xue, WZ; Xu, D; Hao, LP; Han, XF; Fei, F; Liu, T; Liang, AH,期刊:European Journal of Medicinal Chemistry, 页码:183-190 , 文章类型: Article,,卷期:2012年49-1]
- A series of 6-substituted aminocarbonyl benzimidazole derivatives were designed and synthesized as nonpeptidic angiotensin II AT(1) receptor antagonists. The preliminary pharmacological evaluation revealed nanomolar AT(1...
- Inhibition of hepatitis C virus NS5B polymerase by S-trityl-L-cysteine derivatives
[作者:Nichols, DB; Fournet, G; Gurukumar, KR; Basu, A; Lee, JC; Sakamoto, N; Kozielski, F; Musmuca, I; Joseph, B; Ragno, R; Kaushik-Basu, N,期刊:European Journal of Medicinal Chemistry, 页码:191-199 , 文章类型: Article,,卷期:2012年49-1]
- Structure-based studies led to the identification of a constrained derivative of S-trityl-c-cysteine (STLC) scaffold as a candidate inhibitor of hepatitis C virus (HCV) NS5B polymerase. A panel of STLC derivatives were s...
- Synthesis, in vitro binding studies and docking of long-chain arylpiperazine nitroquipazine analogues, as potential serotonin transporter inhibitors
[作者:Jaronczyk, M; Wolosewicz, K; Gabrielsen, M; Nowak, G; Kufareva, I; Mazurek, AP; Ravna, AW; Abagyan, R; Bojarski, AJ; Sylte, I; Chilmonczyk, Z,期刊:European Journal of Medicinal Chemistry, 页码:200-210 , 文章类型: Article,,卷期:2012年49-1]
- It is well known that 6-nitroquipazine exhibits about 150-fold higher affinity for the serotonin transporter (SERT) than quipazine and recently we showed quipazine buspirone analogues with high to moderate SERT affinity....
- Synthesis, anti-HBV activity and renal cell toxicity evaluation of mixed phosphonate prodrugs of adefovir
[作者:Fu, XZ; Ou, Y; Pei, JY; Liu, Y; Li, J; Zhou, W; Lan, YY; Wang, AM; Wang, YL,期刊:European Journal of Medicinal Chemistry, 页码:211-218 , 文章类型: Article,,卷期:2012年49-1]
- A series of phosphonate ester prodrugs of adefovir incorporating L-amino (thio)acid and non-steroidal anti-inflammatory drug (NSAID) moieties were synthesized and their anti-HBV activity and renal cell toxicity were eval...
- Dihydroxylated 2,4,6-triphenyl pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study
[作者:Karki, R; Thapa, P; Yoo, HY; Kadayat, TM; Park, PH; Na, Y; Lee, E; Jeon, KH; Cho, WJ; Choi, H; Kwon, Y; Lee, ES,期刊:European Journal of Medicinal Chemistry, 页码:219-228 , 文章类型: Article,,卷期:2012年49-1]
- Twelve dihydroxylated 2,4,6-triphenyl pyridines were designed and synthesized which contain hydroxyl groups at ortho, meta or para position of 2- and 6-phenyl, or 2- and 4-phenyl rings attached to the central pyridine. T...
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