- Discovery of triazolinone non-nucleoside inhibitors of HIV reverse transcriptase
[作者：Sweeney, ZK; Acharya, S; Briggs, A; Dunn, JP; Elworthy, TR; Fretland, J; Giannetti, AM; Heilek, G; Li, Y; Kaiser, AC; Martin, M; Saito, YD; Smith, M; Suh, JM; Swallow, S; Wu, J; Hang, JQ; Zhou, AS; Klumpp, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4348-4351 , 文章类型： Article，,卷期：2008年18-15]
- Novel non-nucleoside inhibitors of HIV-RT that contain pyridazinone isosteres were prepared, and a series of triazolinones were found to be potent inhibitors of HIV replication. These compounds were active against severa...
- Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase
[作者：Sweeney, ZK; Dunn, JP; Li, Y; Heilek, G; Dunten, P; Elworthy, TR; Han, X; Harris, SF; Hirschfeld, DR; Hogg, JH; Huber, W; Kaiser, AC; Kertesz, DJ; Kim, W; Mirzadegan, T; Roepel, MG; Saito, YD; Silva, TMPC; Swallow, S; Tracy, JL; Villasenor, A; Vora, H; Zhou, AS; Klumpp, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4352-4354 , 文章类型： Article，,卷期：2008年18-15]
- A series of benzyl pyridazinones were evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Several members of this series showed good activity against the wild-type virus and NNRTI-resistant virus...
- Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity
[作者：Fish, PV; Barta, NS; Gray, DLF; Ryckmans, T; Stobie, A; Wakenhut, F; Whitlock, GA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4355-4359 , 文章类型： Article，,卷期：2008年18-15]
- Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine are disclosed as a new series of noradrenaline reuptake inhibitors (NRI). Carboxamide 9e, carbamate 11b and sulfonamide 13a were identified as potent NRIs wit...
- Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP)
[作者：Haffner, CD; Diaz, CJ; Miller, AB; Reid, RA; Madauss, KP; Hassell, A; Hanlon, MH; Porter, DJT; Becherer, JD; Carter, LH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4360-4363 , 文章类型： Article，,卷期：2008年18-15]
- We report the synthesis and in vitro activity of a series of novel pyrrolidinyl pyridones and pyrazinones as potent inhibitors of prolyl oligopeptidase (POP). Within this series, compound 39 was co-crystallized within th...
- Exploring 9-benzyl purines as inhibitors of glutamate racemase (MurI) Gram-positive bacteria
[作者：Geng, B; Breault, G; Comita-Prevoir, J; Petrichko, R; Eyermann, C; Lundqvist, T; Doig, P; Gorseth, E; Noonan, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4368-4372 , 文章类型： Article，,卷期：2008年18-15]
- An early SAR study of a screening hit series has generated a series of 9-benzyl purines as inhibitors of bacterial glutamate racemase (MurI) with micromolar enzyme potency and improved physical properties. X-ray co-cryst...
- The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase
[作者：Takle, AK; Bamford, MJ; Davies, S; Davis, RP; Dean, DK; Gaiba, A; Irving, EA; King, FD; Naylor, A; Parr, CA; Ray, AM; Reith, AD; Smith, BB; Staton, PC; Steadman, JGA; Stean, TO; Wilson, DM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4373-4376 , 文章类型： Article，,卷期：2008年18-15]
- Modification of the potent imidazole-based B-Raf inhibitor SB-590885 resulted in the identification of a series of furan-based derivatives with enhanced CNS penetration. One such compound, SB-699393 (17), was examined in...
- Successful kinase bypass with new acyclovir phosphoramidate prodrugs
[作者：McGuigan, C; Derudas, M; Bugert, JJ; Andrei, G; Snoeck, R; Balzarini, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4364-4367 , 文章类型： Article，,卷期：2008年18-15]
- Novel phosphoramidates of acyclovir have been prepared and evaluated in vitro against acyclovir-sensitive and -resistant herpes simplex virus (HSV) types 1 and 2 and varicella-zoster virus (VZV). Unlike the parent nucleo...
- Design and synthesis of regioisomerically pure unsymmetrical xanthene derivatives for staining live cells and their photochemical properties
[作者：Kamino, S; Ichikawa, H; Wada, SI; Horio, Y; Usami, Y; Yamaguchi, T; Koda, T; Harada, A; Shimanuki, K; Arimoto, M; Doi, M; Fujita, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4380-4384 , 文章类型： Article，,卷期：2008年18-15]
- We have demonstrated the synthesis of regioisomerically pure unsymmetrical xanthene derivatives consisting of three units which can be independently modified to control their physical properties. The photochemical proper...
- Synthesis and antitumor activity of cyclodepsipeptide zygosporamide and its analogues
[作者：Wang, Y; Zhang, FR; Zhang, YH; Liu, JO; Ma, DW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4385-4387 , 文章类型： Article，,卷期：2008年18-15]
- The synthesis and structure-activity relationships of zygosporamide, a known potent and selective cytotoxic natural product against SF-268 and RXF 393 cell lines, are described. The potencies of the synthetic zygosporami...
- Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors
[作者：Cuny, GD; Yu, PB; Laha, JK; Xing, XC; Liu, JF; Lai, CS; Deng, DY; Sachidanandan, C; Bloch, KD; Peterson, RT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4388-4392 , 文章类型： Article，,卷期：2008年18-15]
- A structure-activity relationship study of dorsomorphin, a previously identified inhibitor of SMAD 1/5/8 phosphorylation by bone morphogenetic protein (BMP) type 1 receptors ALK2, 3, and 6, revealed that increased inhibi...
- Discovery of imidazole carboxamides as potent and selective CCK1R agonists
[作者：Zhu, C; Hansen, AR; Bateman, T; Chen, ZS; Holt, TG; Hubert, JA; Karanam, BV; Lee, SJ; Pan, J; Qian, S; Reddy, VBG; Reitman, ML; Strack, AM; Tong, V; Weingarth, DT; Wolff, MS; MacNeil, DJ; Weber, AE; Duffy, JL; Edmondson, SD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4393-4396 , 文章类型： Article，,卷期：2008年18-15]
- High-throughput screening revealed diaryl pyrazole 3 as a selective albeit modest cholecystokinin 1 receptor (CCK1R) agonist. SAR studies led to the discovery and optimization of a novel class of 1,2-diaryl imidazole car...
- Synthesis and biological evaluation of a focused library of beauveriolides
[作者：Nagai, K; Doi, T; Ohshiro, T; Sunazuka, T; Tomoda, H; Takahashi, T; Omura, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4397-4400 , 文章类型： Article，,卷期：2008年18-15]
- Fungal beauveriolide III (1b), discovered as an inhibitor of lipid droplet accumulation in mouse macrophages and showing antiatherogenic activity in mouse model, consists of L-Phe, L-Ala, D-allo-Ile, and (3S, 4S)-3-hydro...
- Sialyl alpha(2 -> 3) lactose clusters using carbosilane dendrimer core scaffolds as influenza hemagglutinin blockers
[作者：Oka, H; Onaga, T; Koyama, T; Guo, CT; Suzuki, Y; Esumi, Y; Hatano, K; Terunuma, D; Matsuoka, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4405-4408 , 文章类型： Article，,卷期：2008年18-15]
- An efficient synthesis of a series of carbosilane dendrimers uniformly functionalized with sialyl alpha(2 -> 3) lactose (Neu5Ac alpha(2 -> 3)Gal beta(1 -> 4)Glc beta 1 ->) moieties was accomplished. The results of a prel...
- Synthesis and anti-inflammatory activity of 2-(2-aroylaroxy)-4,6-dimethoxy pyrimidines
[作者：Venu, TD; Khanum, SA; Firdouse, A; Manuprasad, BK; Shashikanth, S; Mohamed, R; Vishwanth, BS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4409-4412 , 文章类型： Article，,卷期：2008年18-15]
- Reaction of 6a-f individually with 2-methylsulfonyl-4,6-dimethoxypyrimidine yielded 7a-f in excellent yield. The newly synthesized heterocycles were characterized by IR, H-1 NMR, and mass spectral data. Compounds 7a-f wa...
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