- Pharmacophore modeling and virtual screening for the discovery of new transforming growth factor-beta type I receptor (ALK5) inhibitors
[作者:Ren, JX; Li, LL; Zou, J; Yang, L; Yang, JL; Yang, SY,期刊:European Journal of Medicinal Chemistry, 页码:4259-4265 , 文章类型: Article,,卷期:2009年44-11]
- Inhibitors of transforming growth factor-beta Type I Receptor (ALK5) have been thought as potential drugs for the treatment of fibrosis and cancer and a considerable number of ALK5 inhibitors have been reported recently....
- Metals in anticancer therapy: Copper(II) complexes as inhibitors of the 20S proteasome
[作者:Hindo, SS; Frezza, M; Tomco, D; Heeg, MJ; Hryhorczuk, L; McGarvey, BR; Dou, QP; Verani, CN,期刊:European Journal of Medicinal Chemistry, 页码:4353-4361 , 文章类型: Article,,卷期:2009年44-11]
- Selective 20S proteasomal inhibition and apoptosis induction were observed when several lines of cancer cells were treated with a series of copper complexes described as [Cu(L-I)Cl] (1), [Cu(L-I)OAc] (2), and [Cu(HLI)(L-...
- Synthesis of some new 1,2,4-triazoles starting from isonicotinic acid hydrazide and evaluation of their antimicrobial activities
[作者:Bayrak, H; Demirbas, A; Demirbas, N; Karaoglu, SA,期刊:European Journal of Medicinal Chemistry, 页码:4362-4366 , 文章类型: Article,,卷期:2009年44-11]
- 5-Pyridin-4-yl-1,3,4-oxadiazole-2-thiol (2) was obtained from the reaction of isonicotinic acid hydrazide with carbon disulfide in basic media and converted into 4-amino-5-pyridin-4-yl-4H-1,2,4-triazole-3-thiol (5) by th...
- Synthesis and antiviral activity of beta-carboline derivatives bearing a substituted carbohydrazide at C-3 against poliovirus and herpes simplex virus (HSV-1)
[作者:Formagio, ASN; Santos, PR; Zanoli, K; Ueda-Nakamura, T; Tonin, LTD; Nakamura, CV; Sarragiotto, MH,期刊:European Journal of Medicinal Chemistry, 页码:4695-4701 , 文章类型: Article,,卷期:2009年44-11]
- Several novel 1,3-disubstituted beta-carboline derivatives bearing a substituted carbohydrazide group at C-3 were synthesized and evaluated for their antiviral activity against vaccinal poliovirus (VP) and herpes simplex...
- Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity: Part 2
[作者:Herold, F; Izbicki, L; Chodkowski, A; Dawidowski, M; Krol, M; Kleps, J; Turlo, J; Wolska, I; Nowak, G; Stachowicz, K; Dybala, M; Siwek, A; Nowak, M; Pieniazek, E; Jaronczyk, M; Sylte, I; Mazurek, AP,期刊:European Journal of Medicinal Chemistry, 页码:4702-4715 , 文章类型: Article,,卷期:2009年44-11]
- Derivatives of 4-aryl-5,6,7,8-tetrahydro-pyrido[1,2-c]pyrimidine were synthesized. These compounds contain the 3-(4-piperidyl)-1H-indole residue or its 5-methoxy or 2-methyl derivative. In vitro binding tests were perfor...
- Synthesis of substituted-phenyl-1,2,4-triazol-3-thione analogues with modified D-glucopyranosyl residues and their antiproliferative activities
[作者:Li, ZZ; Gu, Z; Yin, K; Zhang, R; Deng, Q; Xiang, JN,期刊:European Journal of Medicinal Chemistry, 页码:4716-4720 , 文章类型: Article,,卷期:2009年44-11]
- A series of D-glucopyranosyl-1,2,4-triazole-3-thione derivatives 1a-1d were synthesized by the reaction of 1,2,4-triazole-3-thione Schiff bases 5a-5d with 2,3,4,6-tetra-O-acetyl-sigma-D-glucopyranosyl bromide. We demonst...
- A new class of anticonvulsants possessing 6 Hz activity: 3,4-Dialkyloxy thiophene bishydrazones
[作者:Kulandasamy, R; Adhikari, AV; Stables, JP,期刊:European Journal of Medicinal Chemistry, 页码:4376-4384 , 文章类型: Article,,卷期:2009年44-11]
- Thirty nine new 3,4-di(substituted)oxy-N-2,N-5-bis(substituted)thiophene-2,5-dicarbohydrazides were synthesized starting from ethyl thiodiglycolate through multi-step reactions. In the synthetic sequence, 3,4-dihydroxyth...
- Synthesis of some novel pyrazolo[3,4-b]pyridine and pyrazolo[3,4-d]pyrimidine derivatives bearing 5,6-diphenyl-1,2,4-triazine moiety as potential antimicrobial agents
[作者:Ali, TES,期刊:European Journal of Medicinal Chemistry, 页码:4385-4392 , 文章类型: Article,,卷期:2009年44-11]
- The reaction of 5,6-diphenyl-3-hydrazino-1,2,4-triazine (1) with bis(methylthio)methylene]malononitrile (2) afforded 5-amino-1-(5,6-diphenyl-1,2,4-triazin-3-yl)-3-(methylthio)-1H-pyrazole-4-carbonitrile (3). Compound 3 r...
- Synthesis of novel bioactive derivatives of 3-(4-chlorophenyl)-2-hydrazino-5,6,7,8-tetrahydrobenzo(b)thieno[2,3-d]pyrimidine-4(3H)-ones
[作者:Gupta, SV; Baheti, K; Bora, R; Dekhane, D; Chhabria, M; Shingare, M; Pawar, S; Shishoo, CJ; Thore, SN,期刊:European Journal of Medicinal Chemistry, 页码:4721-4725 , 文章类型: Article,,卷期:2009年44-11]
- A series of triazolo[4,3-a]tetrahydrobenzo(b)thieno[3,2-e]pyrimidine-5(4H)-ones (12a-n) were synthesized and evaluated for CNS depressant, skeletal muscle relaxant and anticonvulsant activities by photoactometer, Rotarod...
- Design, synthesis and in vitro antibacterial/antifungal evaluation of novel 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7(1-piperazinyl)quinoline-3-carboxylic acid derivatives
[作者:Yu, ZY; Shi, GY; Sun, Q; Jin, H; Teng, Y; Tao, K; Zhou, GP; Liu, W; Wen, F; Hou, TP,期刊:European Journal of Medicinal Chemistry, 页码:4726-4733 , 文章类型: Article,,卷期:2009年44-11]
- A series of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7(1-piperazinyl)quinoline-3-carboxylic acid (norfloxacin) derivatives were prepared according to the principle of combinating bioactive substructures and tested for their ac...
- 1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: Design, synthesis, and microbiological evaluation
[作者:Biava, M; Porretta, GC; Poce, G; De Logu, A; Meleddu, R; De Rossi, E; Manetti, F; Botta, M,期刊:European Journal of Medicinal Chemistry, 页码:4734-4738 , 文章类型: Article,,卷期:2009年44-11]
- During the search of novel antitubercular drugs related to BM 212, new diarylpyrroles were designed and synthesized on the basis of a structure-activity relationship analysis of many pyrroles previously described by us. ...
- Synthesis of new 4-isopropylthiazole hydrazide analogs and some derived clubbed triazole, oxadiazole ring systems - A novel class of potential antibacterial, antifungal and antitubercular agents
[作者:Mallikarjuna, BP; Sastry, BS; Kumar, GVS; Rajendraprasad, Y; Chandrashekar, SM; Sathisha, K,期刊:European Journal of Medicinal Chemistry, 页码:4739-4746 , 文章类型: Article,,卷期:2009年44-11]
- In the present study a series of 4-isopropylthiazole-2-carbohydrazide analogs, derived clubbed oxadiazole-thiazole and triazole-thiazole derivatives have been synthesized and characterized by IR, H-1 NMR, C-13 NMR, eleme...
- Synthesis, crystal structures and antibacterial activity studies of aza-derivatives of phytoalexin from cotton plant - gossypol
[作者:Przybylski, P; Pyta, K; Stefanska, J; Ratajczak-Sitarz, M; Katrusiak, A; Huczynski, A; Brzezinski, B,期刊:European Journal of Medicinal Chemistry, 页码:4393-4403 , 文章类型: Article,,卷期:2009年44-11]
- Using Gossypol (GOS) extracted from cotton seeds, a series of its Schiff bases (1-18) and hydrazones (1927) have been synthesized and evaluated for their antimicrobial activities against Gram-positive bacteria, Gram-nega...
- Heterocyclic replacement of the central phenyl core of diamine-based histamine H-3 receptor antagonists
[作者:Swanson, DM; Shah, CR; Lord, B; Morton, K; Dvorak, LK; Mazur, C; Apodaca, R; Xiao, W; Boggs, JD; Feinstein, M; Wilson, SJ; Barbier, AJ; Bonaventure, P; Lovenberg, TW; Carruthers, NI,期刊:European Journal of Medicinal Chemistry, 页码:4413-4425 , 文章类型: Article,,卷期:2009年44-11]
- A series of small molecules consisting of a heterocyclic core flanked by two basic functionalities were synthesized and screened for in vitro affinity at the human histamine H-3 receptor (hH(3)R). Nine of the twenty-eigh...
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