- Antibacterial activity of chalcones, hydrazones and oxadiazoles against methicillin-resistant Staphylococcus aureus
[作者:Osorio, TM; Delle Monache, F; Chiaradia, LD; Mascarello, A; Stumpf, TR; Zanetti, CR; Silveira, DB; Barardi, CRM; Smania, EDA; Viancelli, A; Garcia, LAT; Yunes, RA; Nunes, RJ; Smania, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:225-230 , 文章类型: Article,,卷期:2012年22-1]
- The increase in antibiotic resistance due to multiple factors has encouraged the search for new compounds which are active against multidrug-resistant pathogens. In this context, chalcones, dihydrochalcones, hydrazones a...
- Synthesis and evaluation of near-infrared fluorescent sulfonamide derivatives for imaging of hypoxia-induced carbonic anhydrase IX expression in tumors
[作者:Groves, K; Bao, B; Zhang, J; Handy, E; Kennedy, P; Cuneo, G; Supuran, CT; Yared, W; Peterson, JD; Rajopadhye, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:653-657 , 文章类型: Article,,卷期:2012年22-1]
- A series of human carbonic anhydrase (hCA) IX inhibitors conjugated to various near-infrared fluorescent dyes was synthesized with the aim of imaging hypoxia-induced hCA IX expression in tumor cells in vitro, ex vivo and...
- The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors
[作者:Graham, TH; Shen, HC; Liu, WS; Xiong, YS; Verras, A; Bleasby, K; Bhatt, UR; Chabin, RM; Chen, DL; Chen, Q; Garcia-Calvo, M; Geissler, WM; He, HB; Lassman, ME; Shen, Z; Tong, XC; Tung, EC; Xie, D; Xu, SY; Colletti, SL; Tata, JR; Hale, JJ; Pinto, S; Shen, DM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:658-665 , 文章类型: Article,,卷期:2012年22-1]
- Novel prolylcarboxypeptidase (PrCP) inhibitors with nanomolar IC50 values were prepared by replacing the previously described dichlorobenzimidazole-substituted pyrrolidine amides with a variety of substituted benzylamine...
- Synthesis, antitubercular evaluation and 3D-QSAR study of N-phenyl-3-(4-fluorophenyl)-4-substituted pyrazole derivatives
[作者:Khunt, RC; Khedkar, VM; Chawda, RS; Chauhan, NA; Parikh, AR; Coutinho, EC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:666-678 , 文章类型: Article,,卷期:2012年22-1]
- As a part of our ongoing research to develop novel antitubercular agents, a series of N-phenyl-3-(4-fluorophenyl)-4-substituted pyrazoles have been synthesized and tested for antimycobacterial activity in vitro against M...
- Characterisation of [C-11]PR04.MZ in Papio anubis baboon: A selective high-affinity radioligand for quantitative imaging of the dopamine transporter
[作者:Riss, PJ; Hooker, JM; Shea, C; Xu, YW; Carter, P; Warner, D; Ferrari, V; Kim, SW; Aigbirhio, FI; Fowler, JS; Roesch, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:679-682 , 文章类型: Article,,卷期:2012年22-1]
- N-(4-fluorobut-2-yn-1-yl)-2 beta-carbomethoxy-3 beta-(4'-tolyl) nortropane (PR04.MZ, 1) is a PET radioligand for the non-invasive exploration of the function of the cerebral dopamine transporter (DAT). A reliable automat...
- Inhibitors of human 2,3-oxidosqualene cyclase (OSC) discovered by virtual screening
[作者:Takumi, W; Kurata, I; Umezawa, Y; Takahashi, Y; Akamatsu, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:231-234 , 文章类型: Article,,卷期:2012年22-1]
- Five human 2,3-oxidosqualnene cyclase (OSC) inhibitors were discovered using the combination of a virtual screening based on a docking study and an isotope-free assay system. All of these inhibitors were revealed to have...
- Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia
[作者:Yang, SW; Smotryski, J; McElroy, WT; Tan, Z; Ho, G; Tulshian, D; Greenlee, WJ; Guzzi, M; Zhang, X; Mullins, D; Xiao, L; Hruza, A; Chan, TM; Rindgen, D; Bleickardt, C; Hodgson, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:235-239 , 文章类型: Article,,卷期:2012年22-1]
- A series of pyrazoloquinoline analogs have been synthesized and shown to bind to PDE10 with high affinity. From the SAR study and our lead optimization efforts, compounds 16 and 27 were found to possess potent oral antip...
- Discovery of pyrrolidine-based beta-secretase inhibitors: Lead advancement through conformational design for maintenance of ligand binding efficiency
[作者:Stachel, SJ; Steele, TG; Petrocchi, A; Haugabook, SJ; McGaughey, G; Holloway, MK; Allison, T; Munshi, S; Zuck, P; Colussi, D; Tugasheva, K; Wolfe, A; Graham, SL; Vacca, JP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:240-244 , 文章类型: Article,,卷期:2012年22-1]
- We have developed a novel series of pyrrolidine derived BACE-1 inhibitors. The potency of the weak initial lead structure was enhanced using library-based SAR methods. The series was then further advanced by rational des...
- Cytotoxic esterified diterpenoid alkaloid derivatives with increased selectivity against a drug-resistant cancer cell line
[作者:Wada, K; Ohkoshi, E; Morris-Natschke, SL; Bastow, KF; Lee, KH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:249-252 , 文章类型: Article,,卷期:2012年22-1]
- C-6 Esterifications of delpheline (1) were carried out to provide 20 new diterpenoid alkaloid derivatives (4-22, 24). Three natural alkaloids (1-3) and all synthesized compounds (4-25) were evaluated for cytotoxic activi...
- Hoiamide D, a marine cyanobacteria-derived inhibitor of p53/MDM2 interaction
[作者:Malloy, KL; Choi, H; Fiorilla, C; Valeriote, FA; Matainaho, T; Gerwick, WH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:683-688 , 文章类型: Article,,卷期:2012年22-1]
- Bioassay-guided fractionation of two cyanobacterial extracts from Papua New Guinea has yielded hoiamide D in both its carboxylic acid and conjugate base forms. Hoiamide D is a polyketide synthase (PKS)/non-ribosomal pept...
- From libraries to candidate: The discovery of new ultra long-acting dibasic beta(2)-adrenoceptor agonists
[作者:Alcaraz, L; Bailey, A; Cadogan, E; Connolly, S; Jewell, R; Jordan, S; Kindon, N; Lister, A; Lawson, M; Mullen, A; Dainty, I; Nicholls, D; Paine, S; Pairaudeau, G; Stocks, MJ; Thorne, P; Young, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:689-695 , 文章类型: Article,,卷期:2012年22-1]
- Libraries of dibasic compounds designed around the molecular scaffold of the DA(2)/beta(2) dual agonist sibenadet (Viozan (TM)) have yielded a number of promising starting points that have been further optimised into nov...
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