- CB 1/2 dual agonists with 3-carbamoyl 2-pyridone derivatives as antipruritics: Reduction of CNS side effects by introducing polar functional groups
[作者：Odan, M; Ishizuka, N; Hiramatsu, Y; Inagaki, M; Hashizume, H; Fujii, Y; Mitsumori, S; Morioka, Y; Soga, M; Deguchi, M; Yasui, K; Arimura, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2894-2897 , 文章类型： Article，,卷期：2012年22-8]
- Our lead compound 1 showed high affinity for both CB1 and CB2 receptors, suggesting the possibility of inducing psychoactive side effects through the CB1 receptor in the brain. To solve this issue, polar functional group...
- Discovery of S-444823, a potent CB1/CB2 dual agonist as an antipruritic agent
[作者：Odan, M; Ishizuka, N; Hiramatsu, Y; Inagaki, M; Hashizume, H; Fujii, Y; Mitsumori, S; Morioka, Y; Soga, M; Deguchi, M; Yasui, K; Arimura, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2898-2901 , 文章类型： Article，,卷期：2012年22-8]
- The optimization of a series of 3-carbamoyl 2-pyridone derivatives as CB agonists is reported. These efforts resulted in the discovery of 3-(2-(1-(cyclohexylmethyl)-2-oxo-1,2,5,6,7,8,9,10-octahydrocycloocta[b]pyridine-3-...
- Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis
[作者：Sureram, S; Senadeera, SPD; Hongmanee, P; Mahidol, C; Ruchirawat, S; Kittakoop, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2902-2905 , 文章类型： Article，,卷期：2012年22-8]
- Bisbenzylisoquinoline alkaloids, tiliacorinine (1), 2'-nortiliacorinine (2), and tiliacorine (3), isolated from the edible plant, Tiliacora triandra, as well as a synthetic derivative, 13'-bromo-tiliacorinine (4), were t...
- Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active gamma-secretase modulators
[作者：Pettersson, M; Johnson, DS; Subramanyam, C; Bales, KR; Ende, CWA; Fish, BA; Green, ME; Kauffman, GW; Lira, R; Mullins, PB; Navaratnam, T; Sakya, SM; Stiff, CM; Tran, TP; Vetelino, BC; Xie, LF; Zhang, LM; Pustilnik, LR; Wood, KM; O'Donnell, CJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2906-2911 , 文章类型： Article，,卷期：2012年22-8]
- We report the discovery and optimization of a novel series of dihydrobenzofuran amides as gamma-secretase modulators (GSMs). Strategies for aligning in vitro potency with drug-like physicochemical properties and good mic...
- Calcitonin gene-related peptide (CGRP) receptor antagonists: Novel aspartates and succinates
[作者：Luo, GL; Chen, L; Pin, SS; Xu, C; Conway, CM; Macor, JE; Dubowchik, GM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2912-2916 , 文章类型： Article，,卷期：2012年22-8]
- Novel aspartate and succinate CGRP full antagonists were identified through core modification of a potent lead CGRP antagonist, BMS-694153. While aspartates were much less active and had a flat SAR, some of the succinate...
- Calcitonin gene-related peptide (CGRP) receptor antagonists: Pyridine as a replacement for a core amide group
[作者：Luo, GL; Chen, L; Civiello, R; Pin, SS; Xu, C; Kostich, W; Kelley, M; Conway, CM; Macor, JE; Dubowchik, GM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2917-2921 , 文章类型： Article，,卷期：2012年22-8]
- In our continuing efforts to identify CGRP receptor antagonists that can be dosed orally for the treatment of migraine headache, we have investigated a pyridine bioisosteric replacement of a polar amide portion of a prev...
- The design and synthesis of novel, phosphonate-containing transient receptor potential melastatin 8 (TRPM8) antagonists
[作者：Matthews, JM; Qin, N; Colburn, RW; Dax, SL; Hawkins, M; McNally, JJ; Reany, L; Youngman, MA; Baker, J; Hutchinson, T; Liu, Y; Lubin, ML; Neeper, M; Brandt, MR; Stone, DJ; Flores, CM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2922-2926 , 文章类型： Article，,卷期：2012年22-8]
- A series of benzothiophene-based phosphonates was synthesized and many analogs within the series were shown to be potent antagonists of the TRPM8 channel. The compounds were obtained as a racemic mixture in 5 synthetic s...
- Melanogenesis inhibitory bisabolane-type sesquiterpenoids from the roots of Angelica koreana
[作者：Lee, JW; Yun, CY; Roh, E; Lee, C; Jin, Q; Bang, KK; Jung, SH; Lee, D; Lee, MK; Kim, Y; Hwang, BY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2927-2931 , 文章类型： Article，,卷期：2012年22-8]
- Bioactivity-guided isolation of the methanolic extract of the roots of Angelica koreana led to the isolation of four new bisabolane-type sesquiterpenoids, osterivolones A-D (1-4) together with four known compounds, bisab...
- Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain
[作者：Adam, JM; Clark, JK; Davies, K; Everett, K; Fields, R; Francis, S; Jeremiah, F; Kiyoi, T; Maidment, M; Morrison, A; Ratcliffe, P; Prosser, A; Schulz, J; Wishart, G; Baker, J; Boyce, S; Campbell, R; Cottney, JE; Deehan, M; Martin, I,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2932-2937 , 文章类型： Article，,卷期：2012年22-8]
- Novel, low brain penetrant, orally bioavailable CB1 receptor agonists were designed starting from a mature lead series of potent brain penetrant CB1 receptor agonists. Increasing the calculated polar surface area was fou...
- Inhibition of hepatitis C virus NS5A by fluoro-olefin based gamma-turn mimetics
[作者：Chang, W; Mosley, RT; Bansal, S; Keilman, M; Lam, AM; Furman, PA; Otto, MJ; Sofia, MJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2938-2942 , 文章类型： Article，,卷期：2012年22-8]
- The HCV non-structural protein NS5A has been established as a viable target for the development of direct acting antiviral therapy. From computational modeling studies strong intra-molecular hydrogen bonds were found to ...
- Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists
[作者：Cameron, KO; Beretta, EE; Chen, Y; Chu-Moyer, M; Fernando, D; Gao, H; Kohrt, J; Lavergne, S; Jardine, PD; Guzman-Perez, A; Hoth, C; Perry, DA; Hadcock, JR; Gautreau, D; Makowski, M; Perez, S; Polivkova, J; Rogers, L; Scott, DO; Swick, AG; Thiede, L; Trebino, CE; Trilles, RV; Wilmowski, J; Zhang, YX,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2943-2947 , 文章类型： Article，,卷期：2012年22-8]
- New cholecystokinin-1 receptor (CCK1R) agonist 'triggers' were identified using iterative library synthesis. Structural activity relationship studies led to the discovery of compound 10e, a potent CCK1R agonist that demo...
- Synthesis and biological evaluation of novel small non-peptidic HIV-1 PIs: The benzothiophene ring as an effective moiety
[作者：Chiummiento, L; Funicello, M; Lupattelli, P; Tramutola, F; Berti, F; Marino-Merlo, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2948-2950 , 文章类型： Article，,卷期：2012年22-8]
- Synthesis and biological evaluation of a new series of potential HIV-1 protease inhibitors incorporating different heterocycles are described. The variation of heteroatom in such molecules has displayed totally different...
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