- The discovery of a structurally novel class of inhibitors of the type 1 glycine transporter
[作者:Lowe, JA; Hou, XJ; Schmidt, C; Tingley, FD; McHardy, S; Kalman, M; DeNinno, S; Sanner, M; Ward, K; Lebel, L; Tunucci, D; Valentine, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2974-2976 , 文章类型: Article,,卷期:2009年19-11]
- The type 1 glycine transporter plays an important in regulating homeostatic glycine levels in the brain that are relevant to the activation of the NMDA receptor by the excitatory neurotransmitter glutamate. We describe h...
- Discovery of aminoheterocycles as a novel beta-secretase inhibitor class: pH dependence on binding activity part 1
[作者:Stachel, SJ; Coburn, CA; Rush, D; Jones, KLG; Zhu, H; Rajapakse, H; Graham, SL; Simon, A; Holloway, MK; Allison, TJ; Munshi, SK; Espeseth, AS; Zuck, P; Colussi, D; Wolfe, A; Pietrak, BL; Lai, MT; Vacca, JP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2977-2980 , 文章类型: Article,,卷期:2009年19-11]
- We have developed a novel series of heteroaromatic BACE-1 inhibitors. These inhibitors interact with the enzyme in a unique fashion that allows for potent binding in a non-traditional paradigm. In addition to the elucida...
- Synthesis, spectral, crystal and antimicrobial studies of biologically potent oxime ethers of nitrogen, oxygen and sulfur heterocycles
[作者:Parthiban, P; Aridoss, G; Rathika, P; Ramkumar, V; Kabilan, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2981-2985 , 文章类型: Article,,卷期:2009年19-11]
- Three series of oxime ethers viz, 2,6-diarylpiperidin-4-one O-benzyloximes 5a-o, 2,6-diaryltetrahydropyran-4-one O-benzyloximes 7a-e and 2,6-diaryltetrahydrothiopyran-4-one O-benzyloximes 11a-b and 12a-c were synthesized...
- Synthesis of novel cholesterol-based cationic lipids for gene delivery
[作者:Kim, BK; Doh, KO; Nam, JH; Kang, H; Park, JG; Moon, IJ; Seu, YB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2986-2989 , 文章类型: Article,,卷期:2009年19-11]
- The new cholesterol-based cationic lipids B, C, and D with an ether linked spacer were synthesized by using aminopropyl chain extension with acrylonitrile. The cholesterol-based cationic lipid A with carbamoyl linkage we...
- Conformational analysis of N,N-disubstituted-1,4-diazepane orexin receptor antagonists and implications for receptor binding
[作者:Cox, CD; McGaughey, GB; Bogusky, MJ; Whitman, DB; Ball, RG; Winrow, CJ; Renger, JJ; Coleman, PJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2997-3001 , 文章类型: Article,,卷期:2009年19-11]
- NMR spectroscopy, X-ray crystallography, and molecular modeling studies indicate that N,N-disubstituted-1,4-diazepane orexin receptor antagonists exist in an unexpected low-energy conformation that is characterized by an...
- Synthesis and P2Y receptor activity of nucleoside 5 '-phosphonate derivatives
[作者:Cosyn, L; Van Calenbergh, S; Joshi, BV; Ko, H; Carter, RL; Harden, TK; Jacobson, KA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3002-3005 , 文章类型: Article,,卷期:2009年19-11]
- Ribose-based nucleoside 5'-diphosphates and triphosphates and related nucleotides were compared in their potency at the P2Y receptors with the corresponding nucleoside 5'-phosphonate derivatives. Phosphonate derivatives ...
- A microwave-assisted facile regioselective Fischer indole synthesis and antitubercular evaluation of novel 2-aryl-3,4-dihydro-2H-thieno[3,2-b]indoles
[作者:Karthikeyan, SV; Perumal, S; Shetty, KA; Yogeeswari, P; Sriram, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3006-3009 , 文章类型: Article,,卷期:2009年19-11]
- A series of novel 2-aryl-3,4-dihydro-2H-thieno[3,2-b] indoles has been synthesised regioselectively in good yields from the reaction of 5-aryldihydro-3(2H)-thiophenones and arylhydrazine hydrochloride. This reaction is f...
- Binaphthyl scaffolded peptoids via ring-closing metathesis reactions and their anti-bacterial activities
[作者:Garas, A; Bremner, JB; Coates, J; Deadman, J; Keller, PA; Pyne, SG; Rhodes, DI,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3010-3013 , 文章类型: Article,,卷期:2009年19-11]
- An efficient synthesis of four new acyclic and four new cyclic binaphthyl-based cationic peptoids is described. These compounds had anti-bacterial activities with MIC values of 4-62 mu g/mL against Staphylococcus aureus....
- Dinitroglyceryl and diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of aspirin, indomethacin and ibuprofen: Synthesis, biological evaluation and nitric oxide release studies
[作者:Abdellatif, KRA; Chowdhury, MA; Dong, Y; Das, D; Yu, G; Velazquez, CA; Suresh, MR; Knaus, EE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3014-3018 , 文章类型: Article,,卷期:2009年19-11]
- A new group of hybrid nitric oxide (NO) releasing anti-inflammatory (AI) ester prodrugs (NONO-NSAIDs) wherein a 1,3-dinitrooxy-2-propyl (12a-c), or O-2-acetoxymethyl-1-[2-(methyl)pyrrolidin-1-yl]diazen-1-ium-1,2-diolate ...
- Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase
[作者:Grey, R; Pierce, AC; Bemis, GW; Jacobs, MD; Moody, CS; Jajoo, R; Mohal, N; Green, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3019-3022 , 文章类型: Article,,卷期:2009年19-11]
- A series of substituted 3-aryl-6-amino-triazolo[4,3-b]pyridazines were identified as highly selective inhibitors of Pim-1 kinase. Initial exploration identified compound 24 as a potent, selective inhibitor, limited in it...
- Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: Effects on HDAC biology and antiproliferative activity
[作者:Tapadar, S; He, R; Luchini, DN; Billadeau, DD; Kozikowski, AP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3023-3026 , 文章类型: Article,,卷期:2009年19-11]
- A series of hydroxamic acid based histone deacetylase inhibitors 6-15, containing an isoxazole moiety adjacent to the Zn-chelating hydroxamic acid, is reported herein. Some of these compounds showed nanomolar activity in...
- Stereochemical studies of hexylitaconic acid, an inhibitor of p53-HDM2 interaction
[作者:Nakahashi, A; Miura, N; Monde, K; Tsukamoto, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3027-3030 , 文章类型: Article,,卷期:2009年19-11]
- Hexylitaconic acid (1) is an intriguing natural product possessing a chiral carbon, and both its enantiomers have been found in nature. Enantiomeric pure (+)-(1) and (-)-(1) were successfully prepared by racemic synthesi...
- Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase
[作者:Cavalli, A; Lizzi, F; Bongarzone, S; Brun, R; Krauth-Siegel, RL; Bolognesi, ML,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3031-3035 , 文章类型: Article,,卷期:2009年19-11]
- Novel quinazoline-type compounds were designed as inhibitors of the parasite specific enzyme trypanothione reductase (TR), and their biological activities were evaluated. Some of our compounds inhibited TR, showed select...
- Synthesis of aristolactam analogues and evaluation of their antitumor activity
[作者:Choi, YL; Kim, JK; Choi, SU; Min, YK; Bae, MA; Kim, BT; Heo, JN,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3036-3040 , 文章类型: Article,,卷期:2009年19-11]
- A series of natural aristolactams and their analogues have been prepared and evaluated for antitumor activity against human cancer cells, including multi-drug resistant cell lines. Naturally occurring aristolactams, such...
|