- Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors
[作者：Zhang, MZ; Jovic, F; Vickers, T; Dyck, B; Tamiya, J; Grey, J; Tran, JA; Fleck, BA; Pick, R; Foster, AC; Chen, C,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3682-3686 , 文章类型： Article，,卷期：2008年18-13]
- Compounds with various activities and selectivities were discovered through structure -activity relationship studies of bicifadine analogs as monoamine transporter inhibitors. The norepinephrine-selective 2-thienyl compo...
- Insight from molecular modeling into different conformation and SAR of natural steroids and unnatural 7-oxa-steroids
[作者：Kang, FA; Chen, X; Jain, N; Allan, G; Tannenbaum, P; Lundeen, S; Sui, ZH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3687-3690 , 文章类型： Article，,卷期：2008年18-13]
- Replacement of the 7-CH2 group of natural steroid with an oxygen atom led to identification of unnatural 7-oxa-steroids as potent and selective progesterone receptor antagonists. The unnatural 7-oxa-steroids exhibited a ...
- Protein subtype-targeting through ligand epimerization: Talose-selectivity of galectin-4 and galectin-8
[作者：Oberg, CT; Blanchard, H; Leffler, H; Nilsson, UJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3691-3694 , 文章类型： Article，,卷期：2008年18-13]
- A series of O2 and O3-derivatized methyl beta-D-talopyranosides were synthesized and evaluated in vitro as inhibitors of the galactose-binding galectin-1, -2, -3, -4 ( N- and C-terminal domains), 8 ( N- terminal domain),...
- Novel benzimidazole derivatives as selective CB2 agonists
[作者：Page, D; Balaux, E; Boisvert, L; Liu, ZP; Milburn, C; Tremblay, M; Wei, ZY; Woo, SM; Luo, XH; Cheng, YX; Yang, H; Srivastava, S; Zhou, F; Brown, W; Tomaszewski, M; Walpole, C; Hodzic, L; St-Onge, S; Godbout, C; Salois, D; Payza, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3695-3700 , 文章类型： Article，,卷期：2008年18-13]
- The preparation and evaluation of a novel class of CB2 agonists based on a benzimidazole moiety are reported. They showed binding affinities up to 1 nM towards the CB2 receptor with partial to full agonist potencies. The...
- Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design
[作者：Liang, GB; Qian, XX; Biftu, T; Singh, S; Gao, YD; Scapin, G; Patel, S; Leiting, B; Patel, R; Wuc, J; Zhang, XP; Thornberry, NA; Weber, AE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3706-3710 , 文章类型： Article，,卷期：2008年18-13]
- Probing with tool molecules, and by modeling and X-ray crystallography the binding modes of two structurally distinct series of DPP-4 inhibitors led to the discovery of a rare aromatic fluorine H-bond and the spatial req...
- Discovery and biological evaluation of novel alpha-glucosidase inhibitors with in vivo antidiabetic effect
[作者：Park, H; Hwang, KY; Kim, YH; Oh, KH; Lee, JY; Kim, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3711-3715 , 文章类型： Article，,卷期：2008年18-13]
- Discovery of alpha-glucosidase inhibitors has been actively pursued with the aim to develop therapeutics for the treatment of diabetes and the other carbohydrate-mediated diseases. We have identified four novel alpha-glu...
- Discovery of potent, orally active benzimidazole glucagon receptor antagonists
[作者：Kim, RM; Chang, J; Lins, AR; Brady, E; Candelore, MR; Dallas-Yang, Q; Ding, V; Dragovic, J; Iliff, S; Jiang, GQ; Mock, S; Qureshi, S; Saperstein, R; Szalkowski, D; Tamvakopoulos, C; Tota, L; Wright, M; Yang, XD; Tata, JR; Chapman, K; Zhang, BB; Parmee, ER,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3701-3705 , 文章类型： Article，,卷期：2008年18-13]
- The discovery and optimization of potent and selective aminobenzimidazole glucagon receptor antagonists are described. One compound possessing moderate pharmacokinetic properties in multiple preclinical species was orall...
- Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles
[作者：McAtee, JJ; Dodson, JW; Dowdell, SE; Erhard, K; Girard, GR; Goodman, KB; Hil, MA; Jin, J; Sehon, CA; Sha, DY; Shi, DC; Wang, F; Wang, GZ; Wang, N; Wang, YH; Viet, AQ; Yuan, CCK; Zhang, DH; Aiyar, NV; Behm, DJ; Carballo, LH; Evans, CA; Fries, HE; Nagilla, R; Roethke, TJ; Xu, XP; Douglas, SA; Neeb, MJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3716-3719 , 文章类型： Article，,卷期：2008年18-13]
- Lead compound 1 was successfully redesigned to provide compounds with improved pharmacokinetic profiles for this series of human urotensin-II antagonists. Replacement of the 2-pyrrolidinylmethyl-3-phenyl-piperidine core ...
- Fungicidal activity of truncated analogues of dihydrosphingosine
[作者：Thevissen, K; Hillaert, U; Meert, EMK; Chow, KK; Cammue, BPA; Van Calenbergh, S; Francois, IEJA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3728-3730 , 文章类型： Article，,卷期：2008年18-13]
- The minimal fungicidal concentration (MFC) of dihydrosphingosine (DHS), phytosphingosine (PHS), and five short-chain DHS derivatives was determined for Candida albicans and Candida glabrata. In this respect, a C15-and a ...
- Antimycotic activity of 4-thioisosteres of flavonoids towards yeast and yeast-like microorganisms
[作者：Buzzini, P; Menichetti, S; Pagliuca, C; Viglianisi, C; Branda, E; Turchetti, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3731-3733 , 文章类型： Article，,卷期：2008年18-13]
- Different substituted methoxy- and hydroxy-4-thioisosteres of flavonoids were prepared and their in vitro antimycotic activity towards yeast (Candida spp., Clavispora spp., Cryptococcus spp., Filobasidiella spp., Issatch...
- Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline
[作者：Sparatore, A; Basilico, N; Casagrande, M; Parapini, S; Taramelli, D; Brun, R; Wittlin, S; Sparatore, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3737-3740 , 文章类型： Article，,卷期：2008年18-13]
- Two pyrrolizidinylalkyl derivatives of 4-amino-7-chloroquinoline (MG2 and MG3) were prepared and tested in vitro against CQ-sensitive and CQ-resistant strains of Plasmodium falciparum and in vivo in a Plasmodium berghei ...
- Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum
[作者：Colabufo, NA; Berardi, F; Contino, M; Inglese, C; Niso, M; Perrone, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3741-3744 , 文章类型： Article，,卷期：2008年18-13]
- Several reference compounds such as Cyclosporin A, Tamoxifen, Verapamil, and our compound 1, known as P-gp modulators, have been tested for their P-gp modulating activity in isolated organ bath. Compound 1 showed the bes...
- Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells
[作者：Bagley, MC; Davis, T; Dix, MC; Murziani, PGS; Rokicki, MJ; Kipling, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3745-3748 , 文章类型： Article，,卷期：2008年18-13]
- 5-Aminopyrazol-4-yl ketones are prepared rapidly and efficiently using microwave dielectric heating from beta-ketonitriles by treatment with N, N'-diphenylformamidine followed by heterocyclocondensation by irradiation wi...
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