- Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes (vol 22, pg 1464, 2012)
[作者:Sutton, JM; Clark, DE; Dunsdon, SJ; Fenton, G; Fillmore, A; Harris, NV; Higgs, C; Hurley, CA; Krintel, SL; MacKenzie, RE; Duttaroy, A; Gangl, E; Maniara, W; Sedrani, R; Namoto, K; Ostermann, N; Gerhartz, B; Sirockin, F; Trappe, J; Hassiepen, U; Baeschlin, DK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2359-2359 , 文章类型: Correction,,卷期:2012年22-6]
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- Molecular modeling study of cyclic pentapeptide CXCR4 antagonists: New insight into CXCR4-FC131 interactions
[作者:Yoshikawa, Y; Kobayashi, K; Oishi, S; Fujii, N; Furuya, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2146-2150 , 文章类型: Article,,卷期:2012年22-6]
- CXCR4 is a G-protein coupled receptor that is associated with many diseases such as breast cancer metastasis, HIV infection, leukemic disease and rheumatoid arthritis, and is thus considered an attractive drug target. Pr...
- Synthesis and evaluation of a new series of 1 '-cyclobutyl-6-(4-piperidyloxy) spiro[benzopyran-2,4 '-piperidine] derivatives as high affinity and selective histamine-3 receptor (H3R) antagonists
[作者:Dandu, RR; Lyons, JA; Raddatz, R; Huang, ZQ; Aimone, LD; Hudkins, RL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2151-2153 , 文章类型: Article,,卷期:2012年22-6]
- A novel class of 1'-cyclobutyl-6-(4-piperidyloxy)spiro[benzopyran-2,4'-piperidine] derivatives with low nanomolar affinity for the human and rat histamine-3 receptors (H(3)Rs) are described. The spirobenzopyran piperidin...
- N-1 and C-3 substituted indole Schiff bases as selective COX-2 inhibitors: Synthesis and biological evaluation
[作者:Kaur, J; Bhardwaj, A; Huang, ZJ; Knaus, EE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2154-2159 , 文章类型: Article,,卷期:2012年22-6]
- A group of N-1 and C-3 disubstituted-indole Schiff bases bearing an indole N-1 (R' = H, CH2Ph, COPh) substituent in conjunction with a C-3-CH=N-C6H4-4-X (X = F, Me, CF3, Cl) substituent were synthesized and evaluated as ...
- N-demethylation of cyamemazine via non-classical Polonovski reaction and its conjugation to bovine serum albumin
[作者:Singh, G; Koerner, TB; Godefroy, SB; Armand, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2160-2162 , 文章类型: Article,,卷期:2012年22-6]
- A modified Polonovski reaction has been employed to obtain the N-demethylated metabolite of the neuroleptic drug cyamemazine. The synthesis involves N-oxide formation, isolation of the corresponding N-oxide, and a FeSO4 ...
- Pyrrolovesamicols-Synthesis, structure and VAChT binding of two 4-fluorobenzoyl regioisomers
[作者:Wenzel, B; Li, Y; Kraus, W; Sorger, D; Sabri, O; Brust, P; Steinbach, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2163-2166 , 文章类型: Article,,卷期:2012年22-6]
- This Letter describes the synthesis of two regioisomers of a new class of vesamicol analogs as possible ligands for imaging the vesicular acetylcholine transporter in future PET studies. The two pyrrolovesamicols (+/-)-6...
- Indolyl and dihydroindolyl N-glycinamides as potent and in vivo active NPY5 antagonists
[作者:Wu, LY; Lu, K; Packiarajan, M; Jubian, V; Chandrasena, G; Wolinsky, TC; Walker, MW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2167-2171 , 文章类型: Article,,卷期:2012年22-6]
- A novel series of indolyl and dihydroindolyl glycinamides were identified as potent NPY5 antagonists with in vivo activity from screen hit 1. The dihydroindolyl glycinamide 10a significantly inhibits NPY5 agonist induced...
- Radiosynthesis of [C-11]BBAC and [C-11]BBPC as potential PET tracers for orexin2 receptors
[作者:Liu, F; Majo, VJ; Prabhakaran, J; Castrillion, J; Mann, JJ; Martinez, D; Kumar, JSD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2172-2174 , 文章类型: Article,,卷期:2012年22-6]
- Radiosynthesis of [N-methyl-C-11](S)-N-([1,1'-biphenyl]-2-yl)-1-(2-((1-methyl-1H-benzo[d] imidazol-2-yl) thio) acetyl) pyrrolidine-2-carboxamide ([C-11] BBAC or [C-11] 3) and [N-methyl-C-11] (S)-N-([1,1'-biphenyl]- 2-yl)...
- Isolation and identification of antibacterial neo-compounds from the red ants of ChangBai Mountain, Tetramorium sp.
[作者:Song, ZW; Liu, P; Yin, WP; Jiang, YL; Ren, YL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2175-2181 , 文章类型: Article,,卷期:2012年22-6]
- Three novel coumarin compounds along with two known amide alkaloids were isolated from a methanol extract of the red ants of ChangBai Mountain, Tetramorium sp. Their structures were identified on the basis of IR, 2D NMR ...
- New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II
[作者:Carta, F; Vullo, D; Maresca, A; Scozzafava, A; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2182-2185 , 文章类型: Article,,卷期:2012年22-6]
- Considering phenols and coumarins as lead molecules for obtaining non-sulfonamide inhibitors of carbonic anhydrases (CAs, EC 4.2.1.1), we screened a large number of compounds possessing diverse chemotypes, but structural...
- Catalysis by molecular iodine: A rapid synthesis of 1,8-dioxo-octahydroxanthenes and their evaluation as potential anticancer agents
[作者:Mulakayala, N; Murthy, PVNS; Rambabu, D; Aeluri, M; Adepu, R; Krishna, GR; Reddy, CM; Prasad, KRS; Chaitanya, M; Kumar, CS; Rao, MVB; Pal, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2186-2191 , 文章类型: Article,,卷期:2012年22-6]
- Molecular iodine facilitated the reaction of 5,5-dimethyl-1,3-cyclohexanedione with aromatic aldehydes in iso-propanol affording a variety of 1,8-dioxo-octahydroxanthenes in high yields. Most of the compounds synthesized...
- Relationship between structure and P-glycoprotein inhibitory activity of dimeric peptides related to the Dmt-Tic pharmacophore
[作者:Ambo, A; Ohkatsu, H; Minamizawa, M; Watanabe, H; Sugawara, S; Nitta, K; Tsuda, Y; Okada, Y; Sasaki, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2192-2194 , 文章类型: Article,,卷期:2012年22-6]
- To develop novel inhibitors of P-glycoprotein (P-gp), dimeric peptides related to an opioid peptide containing the Dmt-Tic pharmacophore were synthesized and their P-gp inhibitory activities were analyzed. Of the 30 anal...
- Structure-based virtual screening approach to the discovery of p38 MAP kinase inhibitors
[作者:Choi, H; Park, HJ; Shin, JC; Ko, HS; Lee, JK; Lee, S; Park, H; Hong, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2195-2199 , 文章类型: Article,,卷期:2012年22-6]
- p38 Mitogen-activated protein kinase (MAPK) has been considered to be a promising target for the development of therapeutics for various immunologic diseases. Herein we report an example for a successful application of t...
- SAR and biological evaluation of 3-azabicyclo[3.1.0]hexane derivatives as mu opioid ligands
[作者:Lunn, G; Roberts, LR; Content, S; Critcher, DJ; Douglas, S; Fenwick, AE; Gethin, DM; Goodwin, G; Greenway, D; Greenwood, S; Hall, K; Thomas, M; Thompson, S; Williams, D; Wood, G; Wylie, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2200-2203 , 文章类型: Article,,卷期:2012年22-6]
- 3-Azabicyclo[3.1.0] hexane compounds were designed as novel achiral mu opioid receptor ligands for the treatment of pruritus in dogs. In this paper, we describe the SAR of this class of opioid ligand, highlighting change...
- Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents
[作者:Bianchi, A; Ugazzi, M; Ferrante, L; Lecis, D; Scavullo, C; Mastrangelo, E; Seneci, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2204-2208 , 文章类型: Article,,卷期:2012年22-6]
- A set of phenyl-substituted Smac mimetics/IAP inhibitor analogues of lead compound 2a was synthesized, aiming to retain its strong cell-free potency while increasing its bioavailability. Seventeen compounds 2b-r were pre...
- Antiviral effect of geraniin on human enterovirus 71 in vitro and in vivo
[作者:Yang, YJ; Zhang, LF; Fan, XX; Qin, C; Liu, JN,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2209-2211 , 文章类型: Article,,卷期:2012年22-6]
- Human enterovirus 71 infection causes hand, foot and mouth disease in children under 6 years of age and has caused mortalities in large-scale outbreaks in the Asia-Pacific region. No effective vaccine or antiviral drugs ...
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