- Synthesis and spectral studies of 2-[(N-ethyl carbazole)-3-sulfonyl ethylenediamine]-1-N,N-2-(2-methypyridy) as a fluorescence probe for Zn2+
[作者：Zhang, J; Cui, HL; Hojo, M; Shuang, SM; Dong, C,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：343-346 , 文章类型： Article，,卷期：2012年22-1]
- A novel Zn2+ fluorescence probe, 2-[(N-ethyl carbazole)-3-sulfonyl ethylenediamine]-1-N,N-bis(2-methypyrbidy), was designed and synthesized via simple steps, and its structure was confirmed by IR and H-1 NMR. The probe g...
- 5-HT2C receptor selectivity and structure-activity relationship of N-methyl-N-(1-methylpiperidin-4-yl)benzenesulfonamide analogs
[作者：Jang, JW; Baek, JS; Choi, GD; Park, WK; Cho, YS; Baek, DJ; Pae, AN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：347-352 , 文章类型： Article，,卷期：2012年22-1]
- Agonists of the 5-HT2C receptor have attracted much attention as therapeutic agents for the treatment of obesity. Subtype selectivity against other 5-HT2 receptors is one of the most important prerequisites for reducing ...
- Synthesis and antiviral activity of substituted quercetins
[作者：Thapa, M; Kim, Y; Desper, J; Chang, KO; Hua, DH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：353-356 , 文章类型： Article，,卷期：2012年22-1]
- Influenza viruses are important pathogens that cause respiratory infections in humans and animals. In addition to vaccination, antiviral drugs against influenza virus play a significant role in controlling viral infectio...
- Discovery of potent and specific CXCR3 antagonists
[作者：Chen, XQ; Mihalic, J; Deignan, J; Gustin, DJ; Duquette, J; Du, XH; Chan, J; Fu, Z; Johnson, M; Li, AR; Henne, K; Sullivan, T; Lemon, B; Ma, J; Miao, SC; Tonn, G; Collins, T; Medina, JC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：357-362 , 文章类型： Article，,卷期：2012年22-1]
- The optimization of a series of 8-aza-quinazolinone analogs for antagonist activity against the CXCR3 receptor is reported. Compounds were optimized to avoid the formation of active metabolites and time-dependent- inhibi...
- Discovery and characterization of a potent and selective antagonist of melanin-concentrating hormone receptor 2
[作者：Chen, XQ; Mihalic, J; Fan, PC; Liang, LM; Lindstrom, M; Wong, S; Ye, QP; Fu, Y; Jaen, J; Chen, JL; Dai, K; Li, LP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：363-366 , 文章类型： Article，,卷期：2012年22-1]
- A series of spiropiperidine carbazoles were synthesized and evaluated as MCHR2 antagonists using a FLIPR assay. The pharmacokinetic properties of selected compounds have also been studied. This effort led to the discover...
- Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism
[作者：Wang, YC; Fu, Z; Schmitt, M; Wang, XM; Shen, W; Rickel, E; Martin, T; Budelsky, A; Marshall, D; Collins, T; Tang, HL; Medina, JC; Liu, JW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：367-370 , 文章类型： Article，,卷期：2012年22-1]
- We have previously reported that optimization of a series of phenylacetic acid derivatives led to the discovery of CRTH2 and DP dual antagonists, such as AMG 009 and AMG 853. During the optimization process, we discovere...
- Inhibition of noroviruses by piperazine derivatives
[作者：Dou, DF; He, GJ; Mandadapu, SR; Aravapalli, S; Kim, Y; Chang, KO; Groutas, WC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：377-379 , 文章类型： Article，,卷期：2012年22-1]
- There is currently an unmet need for the development of small-molecule therapeutics for norovirus infection. The piperazine scaffold, a privileged structure embodied in many pharmacological agents, was used to synthesize...
- 3-Mercapto-1,2,4-triazoles and N-acylated thiosemicarbazides as metallo-beta-lactamase inhibitors
[作者：Faridoon; Hussein, WM; Vella, P; Ul Islam, N; Ollis, DL; Schenk, G; McGeary, RP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：380-386 , 文章类型： Article，,卷期：2012年22-1]
- The production of beta-lactamases is an effective strategy by which pathogenic bacteria can develop resistance against beta-lactam antibiotics. While inhibitors of serine-beta-lactamases are widely used in combination th...
- Ceric ammonium nitrate-promoted oxidative coupling reaction for the synthesis and evaluation of a series of anti-tumor amide anhydrovinblastine analogs
[作者：Song, WB; Lei, M; Zhao, K; Hu, LJ; Meng, YH; Guo, D; Liu, X; Hu, LH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：387-390 , 文章类型： Article，,卷期：2012年22-1]
- A new, practical and efficient method for the synthesis of anhydrovinblastine AVBL (1f) by oxidative coupling of vindoline and catharanthine in the presence of ceric ammonium nitrate (CAN) was developed. Under the optimi...
- Towards a modern definition of vitamin E-evidence for a quinone hypothesis
[作者：Shrader, WD; Amagata, A; Barnes, A; Hinman, A; Jankowski, O; Lee, E; Kheifets, V; Komatsuzaki, R; Mollard, P; Murase, K; Rioux, P; Wesson, K; Miller, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：391-395 , 文章类型： Article，,卷期：2012年22-1]
- We report on the synthesis, biological and pharmacological activity of the tocoquinone natural product, alpha-tocopherol quinone (ATQ); an oxidative metabolite of alpha-tocopherol. ATQ is a potent cellular protectant aga...
- Discovery of a novel EP2/EP4 dual agonist with high subtype-selectivity
[作者：Kambe, T; Maruyama, T; Nakano, M; Nakai, Y; Yoshida, T; Matsunaga, N; Oida, H; Konaka, A; Maruyama, T; Nakai, H; Toda, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：396-401 , 文章类型： Article，,卷期：2012年22-1]
- A series of gamma-lactam prostaglandin E(1) analogs bearing a 16-phenyl moiety in the omega-chain and aryl moiety in the alpha-chain were synthesized and biologically evaluated. Among the tested compounds, gamma-lactam P...
- In vitro inhibition of translation initiation by N,N '-diarylureas-potential anti-cancer agents
[作者：Denoyelle, S; Chen, T; Chen, LM; Wang, YB; Klosi, E; Halperin, JA; Aktas, BH; Chorev, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：402-409 , 文章类型： Article，,卷期：2012年22-1]
- Symmetrical N,N'-diarylureas: 1,3-bis(3,4-dichlorophenyl)-, 1,3-bis[4-chloro-3-(trifluoromethyl)phenyl]- and 1,3-bis[3,5-bis(trifluoromethyl)phenyl]urea, were identified as potent activators of the eIF2 alpha kinase heme...
- One-pot regioselective synthesis of tetrahydroindazolones and evaluation of their antiproliferative and Src kinase inhibitory activities
[作者：Rao, VK; Chhikara, BS; Tiwari, R; Shirazi, AN; Parang, K; Kumar, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：410-414 , 文章类型： Article，,卷期：2012年22-1]
- A number of 2-substituted tetrahydroindazolones were synthesized by three-component condensation reaction of 1,3-diketones, substituted hydrazines, benzaldehydes, and Yb(OTf)(3) as a catalyst in [bmim][BF4] ionic liquid ...
- A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity
[作者：Filipski, KJ; Bian, JW; Ebner, DC; Lee, ECY; Li, JC; Sammons, MF; Wright, SW; Stevens, BD; Didiuk, MT; Tu, MH; Perreault, C; Brown, J; Atkinson, K; Tan, BJ; Salatto, CT; Litchfield, J; Pfefferkorn, JA; Guzman-Perez, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：415-420 , 文章类型： Article，,卷期：2012年22-1]
- A novel series of glucagon receptor antagonists has been discovered. These pyrazole ethers and aminopyrazoles have lower molecular weight and increased polarity such that the molecules fall into better drug-like property...
- Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: Identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H-1-antihistamines for insomnia
[作者：Ravula, SB; Yu, JH; Tran, JA; Arellano, M; Tucci, FC; Moree, WJ; Li, BF; Petroski, RE; Wen, JY; Malany, S; Hoare, SRJ; Madan, A; Crowe, PD; Beaton, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：421-426 , 文章类型： Article，,卷期：2012年22-1]
- The structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles, 2-morpholine and 2-thiomorpholin-2-yl-1H-benzimidazoles are described. In the lead optimization process, the pK(a) and/or logP of benzimidazol...
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