- Discovery of new S-adenosylmethionine decarboxylase inhibitors for the treatment of Human African Trypanosomiasis (HAT)
[作者:Hirth, B; Barker, RH; Celatka, CA; Klinger, JD; Liu, HL; Nare, B; Nijjar, A; Phillips, MA; Sybertz, E; Willert, EK; Xiang, YB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2916-2919 , 文章类型: Article,,卷期:2009年19-11]
- Modification of the structure of trypanosomal AdoMetDC inhibitor 1 (MDL73811) resulted in the identification of a new inhibitor 7a, which features a methyl substituent at the 8-position. Compound 7a exhibits improved pot...
- Structural insight into human CK2 alpha in complex with the potent inhibitor ellagic acid
[作者:Sekiguchi, Y; Nakaniwa, T; Kinoshita, T; Nakanishi, I; Kitaura, K; Hirasawa, A; Tsujimoto, G; Tada, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2920-2923 , 文章类型: Article,,卷期:2009年19-11]
- We determined the 2.35-angstrom crystal structure of a human CK2 catalytic subunit (referred to as CK2 alpha complexed with the ATP-competitive, potent CK2 inhibitor ellagic acid. The inhibitor binds to CK2 alpha with a ...
- Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)
[作者:Huynh, T; Chen, Z; Pang, SH; Geng, JP; Bandiera, T; Bindi, S; Vianello, P; Roletto, F; Thieffine, S; Galvani, A; Vaccaro, W; Poss, MA; Trainor, GL; Lorenzi, MV; Gottardis, M; Jayaraman, L; Purandare, AV,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2924-2927 , 文章类型: Article,,卷期:2009年19-11]
- Design, synthesis, and SAR development led to the identification of the potent, novel, and selective pyrazole based inhibitor (7f) of Coactivator Associated Arginine Methyltransferase (CARM1). (C) 2009 Elsevier Ltd. All ...
- Synthesis and structure-activity relationships of bengazole A analogs
[作者:Mulder, RJ; Shafer, CM; Dalisay, DS; Molinski, TF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2928-2930 , 文章类型: Article,,卷期:2009年19-11]
- Analogs of the potent antifungal agent, bengazole A, were prepared and evaluated against Candida spp. in both microbroth dilution and disk diffusion assays. (C) 2009 Elsevier Ltd. All rights reserved.
- Carbonic anhydrase inhibitors. Synthesis of 2,4,6-trimethylpyridinium derivatives of 2-(hydrazinocarbonyl)-3-aryl-1H-indole-5-sulfonamides acting as potent inhibitors of the tumor-associated isoform IX and XII
[作者:Guzel, O; Maresca, A; Scozzafava, A; Salman, A; Balaban, AT; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2931-2934 , 文章类型: Article,,卷期:2009年19-11]
- A series of 2-(hydrazinocarbonyl)-3-aryl-1H-indole-5-sulfonamides possessing various 2-, 3- or 4- substituted phenyl groups with methyl-, halogeno- and methoxy-functionalities, or a perfluorophenyl moiety, has been deriv...
- Discovery of a novel HCV helicase inhibitor by a de novo drug design approach
[作者:Kandil, S; Biondaro, S; Vlachakis, D; Cummins, AC; Coluccia, A; Berry, C; Leyssen, P; Neyts, J; Brancale, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2935-2937 , 文章类型: Article,,卷期:2009年19-11]
- Herein we report a successful application of a computer-aided design approach to identify a novel HCV helicase inhibitor. A de novo drug design methodology was used to generate an initial set of structures that could pot...
- Synthesis and in vivo influenza virus-inhibitory effect of ester prodrug of 4-guanidino-7-O-methyl-Neu5Ac2en
[作者:Honda, T; Kubo, S; Masuda, T; Arai, M; Kobayashi, Y; Yamashita, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2938-2940 , 文章类型: Article,,卷期:2009年19-11]
- A series of ester prodrugs of 7-O-methyl derivative of Zanamivir (compound 3) was synthesized and their efficacy was evaluated in an influenza infected mice model by intranasal administration. Compound 7c (CS-8958), octa...
- Smart conferring of nuclease resistance to DNA by 3 '-end protection using 2 ',4 '-bridged nucleoside-5 '-triphosphates
[作者:Kuwahara, M; Obika, S; Takeshima, H; Hagiwara, Y; Nagashima, J; Ozaki, H; Sawai, H; Imanishi, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2941-2943 , 文章类型: Article,,卷期:2009年19-11]
- Incorporation of 2',4'-bridged nucleotides into the 3'-end of oligodeoxyribonucleotide (ODN) was examined using terminal deoxynucleotidyl transferase (TdT). The three types of 2',4'-bridged nucleoside-5'-triphospates wit...
- Acetoxybenzhydrols as highly active and stable analogues of 1 ' S-1 '-acetoxychavicol, a potent antiallergic principal from Alpinia galanga
[作者:Yasuhara, T; Manse, Y; Morimoto, T; Wang, QL; Matsuda, H; Yoshikawa, M; Muraoka, O,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2944-2946 , 文章类型: Article,,卷期:2009年19-11]
- Through SAR studies on 1'S-1'-acetoxychavicol acetate (1) against Type I antiallergic activity by indexing release of beta-hexosaminidase, a marker of antigen-IgE-mediated degranulation in RBL-2H3 cells, more stable and ...
- Crown-capped imidacloprid: A novel design and insecticidal activity
[作者:Kagabu, S; Takagi, M; Ohno, I; Mikawa, T; Miyamoto, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2947-2948 , 文章类型: Article,,卷期:2009年19-11]
- Imidacloprid (IMI) derivatives conjugated with benzo-15-crown-5 and benzo-18-crown-6 structures, applied for the first time to explore novel insecticidal molecule, elicited strong excitatory toxic signs to the house flie...
- Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors
[作者:Deore, V; Yewalkar, N; Bhatia, D; Desai, N; Gupte, RD; Dadarkar, SS; Jadhav, MG; Tannu, AA; Bhatt, P; Nemmani, KVS; Vishwakarma, RA; Sharma, S; Roychowdhury, A; Dagia, NM; Bhonde, MR; Kumar, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2949-2952 , 文章类型: Article,,卷期:2009年19-11]
- A series of novel cyanopyridyl based molecules (1-14) were designed, synthesized and probed for inhibition of mammalian target of rapamycin (mTOR) activity. Compound 14 was found to be a potent inhibitor of mTOR activity...
- Synthesis and biological evaluation of arylhydrazinocyanoacrylates and N-aryl pyrazolecarboxylates
[作者:Liu, YX; Liu, SH; Li, YH; Song, HB; Wang, QM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2953-2956 , 文章类型: Article,,卷期:2009年19-11]
- A series of arylhydrazino-substituted cyanoacrylates 3 and N-aryl pyrazolecarboxylates 6 were synthesized and their bioactivities were evaluated. Though compounds 3 were designed as herbicide, some of them showed fungici...
- Synthesis and biological applications of two novel fluorescent proteins-labeling probes
[作者:Wu, XL; Tian, M; He, HZ; Sun, W; Li, JL; Shi, Z,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2957-2959 , 文章类型: Article,,卷期:2009年19-11]
- Two novel chlorinated fluoresceins 2',4',5',7'-tetrachloro-6-(5-carboxypentyl)-4,7-dichloro fluorescein succinimidyl ester (1G) and 2',4',5',7'- tetrachloro-6-(3-carboxypropyl)-4,7-dichlorofluorescein succinimidyl ester ...
- Synthesis, antimicrobial activity and QSAR studies of new 2,3-disubstituted-3,3a,4,5,6,7-hexahydro-2H-indazoles
[作者:Minu, M; Thangadurai, A; Wakode, SR; Agrawal, SS; Narasimhan, B,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2960-2964 , 文章类型: Article,,卷期:2009年19-11]
- Antimicrobial activity of synthesized 2,3-disubstituted-3,3a,4,5,6,7-hexahydro-2H-indazole derivatives indicated that 3-(4-chlorophenyl)-2-(4-nitrophenylsulfonyl)-3,3a, 4,5,6,7-hexahydro-2H-indazole (6) and 3-(4-fluoroph...
- Spiroimidazolidinone NPC1L1 inhibitors. 1: Discovery by 3D-similarity-based virtual screening
[作者:McMasters, DR; Garcia-Calvo, M; Maiorov, V; McCann, ME; Meurer, RD; Bull, HG; Lisnock, J; Howell, KL; DeVita, RJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2965-2968 , 文章类型: Article,,卷期:2009年19-11]
- A series of spiroimidazolidinone NPC1L1 inhibitors was discovered by virtual screening of the Merck corporate sample repository using 3D-similarity-based screening. Selection of 330 compounds for testing in an in vitro N...
- Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064
[作者:Bass, JY; Caldwell, RD; Caravella, JA; Chen, LH; Creech, KL; Deaton, DN; Madauss, KP; Marr, HB; McFadyen, RB; Miller, AB; Parks, DJ; Todd, D; Williams, SP; Wisely, GB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2969-2973 , 文章类型: Article,,卷期:2009年19-11]
- Starting from the known FXR agonist GW 4064 1a, a series of alternately 3,5-substituted isoxazoles was prepared. Several of these analogs were potent full FXR agonists. A subset of this series, with a tether between the ...
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