- Synthesis and evaluation of 5-benzylidene(thio)barbiturate-beta-D-glycosides as mushroom tyrosinase inhibitors
[作者：Yan, Q; Cao, RH; Yi, W; Yu, L; Chen, ZY; Ma, L; Song, HC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4055-4058 , 文章类型： Article，,卷期：2009年19-15]
- A series of 5-benzylidene(thio)barbiturate-beta-D-glycosides were designed, synthesized and evaluated as a new class of mushroom tyrosinase inhibitors. The results demonstrated that most of compounds had more potent inhi...
- Amidine derived inhibitors of acid-sensing ion channel-3 (ASIC3)
[作者：Kuduk, SD; Chang, RK; Wai, JMC; Di Marco, CN; Cofre, V; DiPardo, RM; Cook, SP; Cato, MJ; Jovanovska, A; Urban, MO; Leitl, M; Spencer, RH; Kane, SA; Hartman, GD; Bilodeau, MT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4059-4063 , 文章类型： Article，,卷期：2009年19-15]
- A series of indole amidines modified at the 2-position of the indole ring were evaluated as inhibitors of Acid-Sensing Ion Channel-3 (ASIC3), a novel target for the treatment of chronic pain. (C) 2009 Elsevier Ltd. All r...
- Synthesis and fungicidal activity of 3,5-dichloropyrazin-2(1H)-one derivatives
[作者：Francois, IEJA; Cammue, BPA; Bresseleers, S; Fleuren, H; Hoornaert, G; Mehta, VP; Modha, SG; Van der Eycken, EV; Thevissen, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4064-4066 , 文章类型： Article，,卷期：2009年19-15]
- We synthesized a family of 3,5-dichloropyrazin-2(1H)-one derivatives and assessed their in vitro fungicidal activity against Candida albicans. Compounds 11 and 20 were most active against C. albicans and induced accumula...
- Bis-anthracenyl isoxazolyl amides have enhanced anticancer activity
[作者：Gajewski, MP; Beall, H; Schnieder, M; Stranahan, SM; Mosher, MD; Rider, KC; Natale, NR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4067-4069 , 文章类型： Article，,卷期：2009年19-15]
- Dimeric analogs of Anthracenyl Isoxazole Amides (AIMs) (the designation AIM is in honor of the memory of Professor Albert I. Meyers) were prepared and dimer 6 exhibited the highest efficacy to date for this class of anti...
- Synthesis and biological evaluation of amide derivatives of diflunisal as potential anti-tumor agents
[作者：Zhong, GX; Chen, LL; Li, HB; Liu, FJ; Hu, JQ; Hu, WX,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4399-4402 , 文章类型： Article，,卷期：2009年19-15]
- To discover the new medicinal activity, the structure of diflunisal has been modified. Forty amide derivatives of diflunisal were synthesized starting from diflunisal in three steps. Their inhibition growth rate of human...
- Rapid assessment of a novel series of selective CB2 agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis
[作者：Ryckmans, T; Edwards, MP; Horne, VA; Correia, AM; Owen, DR; Thompson, LR; Tran, I; Tutt, MF; Young, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4406-4409 , 文章类型： Article，,卷期：2009年19-15]
- A series of libraries were designed using the 1-(cyclopropylmethyl)-2-alkyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c] pyridin-5-ium templates 2a-b, and Sulfonamide derivatives 11a-n proved to be potent agonists of the CB2 rec...
- Discovery of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers. 2. Identification of more aqueous soluble analogs as potential anticancer agents
[作者：Kemnitzer, W; Kuemmerle, J; Zhang, HZ; Kasibhatla, S; Tseng, B; Drewe, J; Cai, SX,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4410-4415 , 文章类型： Article，,卷期：2009年19-15]
- As a continuation of our efforts to discover and develop the 3-aryl-5-aryl-1,2,4-oxadiazole series of apoptosis inducers as potential anticancer agents, we explored substitutions at the 2-and 3-positions of the 3-aryl gr...
- Design, synthesis and identification of novel colchicine-derived immunosuppressant
[作者：Chang, DJ; Yoon, EY; Lee, GB; Kim, SO; Kim, WJ; Kim, YM; Jung, JW; An, H; Suh, YG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4416-4420 , 文章类型： Article，,卷期：2009年19-15]
- Synthesis and biological evaluation of various colchicine analogues through the mixed-lymphocyte reaction (MLR), lymphoproliferation, and inhibitory effects on the inflammatory genes are described. In addition, a new ser...
- Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors
[作者：Koltun, DO; Zilbershtein, TM; Migulin, VA; Vasilevich, NI; Parkhill, EQ; Glushkov, AI; McGregor, MJ; Brunn, SA; Chu, N; Hao, J; Mollova, N; LeungF, K; Chisholm, JW; Zablocki, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4070-4074 , 文章类型： Article，,卷期：2009年19-15]
- Two structurally distinct series of SCD (Delta 9 desaturase) inhibitors (1 and 2) have been previously reported by our group. In the present work, we merged the structural features of the two series. This led to the disc...
- Development of a selective and potent radioactive ligand for histamine H-3 receptors: A compound potentially useful for receptor occupancy studies
[作者：Mitobe, Y; Ito, S; Mizutani, T; Nagase, T; Sato, N; Tokita, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4075-4078 , 文章类型： Article，,卷期：2009年19-15]
- Radioligands are powerful tools for examining the pharmacological profiles of chemical leads and thus facilitate drug discovery. In this study, we identified and characterized 3-([1,1,1-H-3]methyl)-2-(4-{[3-(1-pyrrolidin...
- Synthesis of novel macrolide derivatives with imidazo[4,5-b]pyridinyl sulfur contained alkyl side chains and their antibacterial activity
[作者：Xu, P; Liu, L; Chen, XZ; Li, Y; Liu, J; Jin, ZP; Wang, GQ; Lei, PS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4079-4083 , 文章类型： Article，,卷期：2009年19-15]
- In an effort to find new antibiotics, a novel series of 14-membered macrolides with imidazo[4,5-b]pyridinyl sulfur contained alkyl side chains has been synthesized based on commercially available clarithromycin. Chemical...
- Peperomins as anti-inflammatory agents that inhibit the NF-kappa B signaling pathway
[作者：Tsutsui, C; Yamada, Y; Ando, M; Toyama, D; Wu, JL; Wang, LY; Taketani, S; Kataoka, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4084-4087 , 文章类型： Article，,卷期：2009年19-15]
- The transcription factor nuclear factor kappa B (NF-kappa B) induces the expression of various inflammatory genes. In the common NF-kappa B signaling pathway, peperomin E and 2,6-didehydropeperomin B inhibited I kappa B ...
- Oxidative aromatization of 1,4-dihydropyridines and pyrazolines using HbA-H2O2: An efficient biomimetic catalyst system providing metabolites of drug candidates
[作者：Kumar, A; Maurya, RA; Sharma, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4432-4436 , 文章类型： Article，,卷期：2009年19-15]
- Human hemoglobin (HbA) efficiently catalyses the oxidative aromatization of 1,4-dihydropyridines (1,4-DHPs) and pyrazolines with hydrogen peroxide in phosphate buffer. The results of the study reveal that the rates of ox...
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