- Substituted N-aryl-6-pyrimidinones: A new class of potent, selective, and orally active p38 MAP kinase inhibitors
[作者：Devadas, B; Selness, SR; Xing, L; Madsen, HM; Marrufo, LD; Shieh, H; Messing, DM; Yang, JZ; Morgan, HM; Anderson, GD; Webb, EG; Zhang, J; Devraj, RV; Monahan, JB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3856-3860 , 文章类型： Article，,卷期：2011年21-13]
- A novel series of highly potent and selective p38 MAP kinase inhibitors was developed originating from a substituted N-aryl-6-pyrimidinone scaffold. SAR studies coupled with in vivo evaluations in rat arthritis model cul...
- A concise synthesis and antimicrobial activities of 3-polyamino-23,24-bisnorcholanes as steroid-polyamine conjugates
[作者：Kim, HS; Khan, SN; Jadhav, JR; Jeong, JW; Jung, K; Kwak, JH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3861-3865 , 文章类型： Article，,卷期：2011年21-13]
- A series of steroid-polyamine conjugates were synthesized and evaluated for their antimicrobial activity. This study was focused on the effect of stereochemistry at the C-3 and C-5 of steroids and types of polyamine at C...
- Rhamnetin production based on the rational design of the poplar O-methyltransferase enzyme and its biological activities
[作者：Lee, S; Shin, SY; Lee, Y; Park, Y; Kim, BG; Ahn, JH; Chong, Y; Lee, YH; Lim, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3866-3870 , 文章类型： Article，,卷期：2011年21-13]
- To produce rhamnetin using enzymatic engineering, poplar O-methyltransferase-7 and its mutants were prepared based on the rational enzyme design, and the production of rhamnetin was compared with the results obtained usi...
- Phenyl isoxazole voltage-gated sodium channel blockers: Structure and activity relationship
[作者：Macsari, I; Sandberg, L; Besidski, Y; Gravenfors, Y; Ginman, T; Bylund, J; Bueters, T; Eriksson, AB; Lund, PE; Venyike, E; Arvidsson, PI,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3871-3876 , 文章类型： Article，,卷期：2011年21-13]
- Blocking of certain sodium channels is considered to be an attractive mechanism to treat chronic pain conditions. Phenyl isoxazole carbamate 1 was identified as a potent and selective Na(V)1.7 blocker. Structural analogu...
- Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors
[作者：Zificsak, CA; Theroff, JP; Aimone, LD; Angeles, TS; Albom, MS; Cheng, MG; Mesaros, EF; Ott, GR; Quail, MR; Underiner, TL; Wan, WH; Dorsey, BD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3877-3880 , 文章类型： Article，,卷期：2011年21-13]
- The incorporation of R,R-1,2-diaminocyclohexane at C4 in a series of 2,4-diaminopyrimidines led to a number of ALK inhibitors in which optimized activity was achieved by conversion of the 2-amino group into a methanesulf...
- Synthesis and antimycobacterial activity of highly functionalized tetrahydro-4(1H)-pyridinones
[作者：Raja, VPA; Perumal, S; Yogeeswari, P; Sriram, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3881-3884 , 文章类型： Article，,卷期：2011年21-13]
- A series of 35 2e, 3e, 6e-triaryltetrahydro-4(1H)-pyridinones, 2e,3e,5e,6e-tetraaryltetrahydro-4(1H)-pyridinones and their N-nitroso and N-cyano analogs have been prepared. All these 35 compounds obtained were screened f...
- Discovery of S1P agonists with a dihydronaphthalene scaffold
[作者：Kurata, H; Kusumi, K; Otsuki, K; Suzuki, R; Kurono, M; Takada, Y; Shioya, H; Komiya, T; Mizuno, H; Ono, T; Hagiya, H; Minami, M; Nakade, S; Habashita, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3885-3889 , 文章类型： Article，,卷期：2011年21-13]
- Structure-activity relationship of sphingosine-1-phosphate receptor agonists was examined. Cinnamyl derivative 1 was modified to improve S1P(1) agonistic activity as well as selectivity over S1P(3) agonistic activity. Di...
- Efficient synthesis, structural characterization and anti-microbial activity of chiral aryl boronate esters of 1,2-O-isopropylidene-alpha-D-xylofuranose
[作者：Trivedi, R; Reddy, ER; Kumar, CK; Sridhar, B; Kumar, KP; Rao, MS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3890-3893 , 文章类型： Article，,卷期：2011年21-13]
- A simple and efficient synthetic approach toward a series of chiral aryl boronate esters, starting from D-xylose, as anti-microbial agents, is described herein. Minimum inhibitory concentration and zone of inhibition rev...
- Synthesis and in vitro evaluation of ambrisentan analogues as potential endothelin receptor antagonists
[作者：Xia, J; Song, JF; Zhen, L; Zhang, XL; Lei, XT; Zheng, LN; Wang, QJ; Sun, HB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3894-3897 , 文章类型： Article，,卷期：2011年21-13]
- A series of novel 2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3,3-diphenyl butyric acid derivatives were synthesized and evaluated for their antagonistic activity for endothelin-1-induced contraction in rabbit aorta. Within this...
- The molecular mechanisms of interactions between bioactive peptides and angiotensin-converting enzyme
[作者：Pan, DD; Guo, HQ; Zhao, B; Cao, JX,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3898-3904 , 文章类型： Article，,卷期：2011年21-13]
- The ability of milk protein derived Ile-Pro-Ala (IPA), Phe-Pro (FP) and Gly-Lys-Pro (GKP) peptides to inhibit angiotensin I-converting enzyme (ACE), a protein with an important role in blood-pressure regulation, were ver...
- Sannastatin, a novel toxic macrolactam polyketide glycoside produced by actinomycete Streptomyces sannanensis
[作者：Yang, SX; Gao, JM; Zhang, AL; Laatsch, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3905-3908 , 文章类型： Article，,卷期：2011年21-13]
- A new rare 20-membered macrocyclic lactam incorporating a diene conjugated olefin, designated sannastatin (1), together with the known structurally related vicenistatin (2), has been isolated from the cultures of Strepto...
- Synthesis of novel pyrazolo[1,5-a]pyrazin-4(5H)-one derivatives and their inhibition against growth of A549 and H322 lung cancer cells
[作者：Zheng, LW; Shao, JH; Zhao, BX; Miao, JY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3909-3913 , 文章类型： Article，,卷期：2011年21-13]
- A series of substituted pyrazolo[1,5-a]pyrazin-4(5H)-one was synthesized by the reaction of ethyl 1-(2-oxo-2-phenylethyl)-3-phenyl-1H-pyrazole-5-carboxylate derivatives and 2-(2-aminoethoxy) ethanol or 2-morpholinoethana...
- Design, synthesis and biological activity of novel peptidyl benzyl ketone FVIIa inhibitors
[作者：Storgaard, M; Henriksen, ST; Zaragoza, F; Peschke, B; Tanner, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3918-3922 , 文章类型： Article，,卷期：2011年21-13]
- Herein is described the synthesis of a novel class of peptidyl FVIIa inhibitors having a C-terminal benzyl ketone group. This class is designed to be potentially suitable as stabilization agents of liquid formulations of...
- Benzoxazinones as potent positive allosteric AMPA receptor modulators: Part I
[作者：Mueller, R; Li, YX; Hampson, A; Zhong, S; Harris, C; Marrs, C; Rachwal, S; Ulas, J; Nielsson, L; Rogers, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3923-3926 , 文章类型： Article，,卷期：2011年21-13]
- AMPA receptors (AMPARs) are an increasingly important therapeutic target in the CNS. Aniracetam, the first identified potentiator of AMPARs, led to the rigid and more potent CX614. This lead molecule was optimized in ord...
- Substituted benzoxazinones as potent positive allosteric AMPA receptor modulators: Part II
[作者：Mueller, R; Rachwal, S; Tedder, ME; Li, YX; Zhong, S; Hampson, A; Ulas, J; Varney, M; Nielsson, L; Rogers, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3927-3930 , 文章类型： Article，,卷期：2011年21-13]
- AMPA receptors (AMPARs) are an important therapeutic target in the CNS. A series of substituted benzoxazinone derivatives with good to very good in vitro activity as positive allosteric AMPAR modulators was synthesized a...
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