- Design, synthesis and structure-activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists
[作者:Laine, DI; Yan, HX; Xie, HB; Davis, RS; Dufour, J; Widdowson, KL; Palovich, MR; Wan, ZH; Foley, JJ; Schmidt, DB; Hunsberger, GE; Burman, M; Bacon, AM; Webb, EF; Luttmann, MA; Salmon, M; Sarau, HM; Umbrecht, ST; Landis, PS; Peck, BJ; Busch-Petersen, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3366-3369 , 文章类型: Article,,卷期:2012年22-9]
- A novel series of N-substituted tropane derivatives was characterized as potent muscarinic acetylcholine receptor antagonists (mAChRs). Kinetic washout studies showed that the N-endosubstituted analog 24 displayed much s...
- Dimerization of beta-tryptase inhibitors, does it work for both basic and neutral P1 groups?
[作者:Liang, GY; Choi-Sledeski, YM; Chen, X; Gong, Y; MacMillan, EW; Tsay, J; Sides, K; Cairns, J; Kulitzscher, B; Aldous, DJ; Morize, I; Pauls, HW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3370-3376 , 文章类型: Article,,卷期:2012年22-9]
- The tetrameric folding of beta-tryptase and the pair-wise distribution of its substrate binding sites offer a unique opportunity for development of inhibitors that span two adjacent binding sites. A series of dimeric inh...
- Design, synthesis, and biological evaluation of chalcone oxime derivatives as potential immunosuppressive agents
[作者:Luo, Y; Song, R; Li, Y; Zhang, S; Liu, ZJ; Fu, J; Zhu, HL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3039-3043 , 文章类型: Article,,卷期:2012年22-9]
- A series of deoxybenzoin oximes were recently reported as potent immunosuppressive agents by our group. In order to continue the original research for potential immunosuppressive agents with high efficacy and low toxicit...
- Preparation, antibacterial evaluation and preliminary structure-activity relationship (SAR) study of benzothiazol- and benzoxazol-2-amine derivatives
[作者:Ouyang, L; Huang, YH; Zhao, YW; He, G; Xie, YM; Liu, J; He, J; Liu, B; Wei, YQ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3044-3049 , 文章类型: Article,,卷期:2012年22-9]
- In this study, a novel benzothiazol- and benzooxazol-2-amine scaffold with antibacterial activity was designed and synthesized. Preliminary structure-activity relationship analysis displayed that compound 8t with a 5,6-d...
- Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases
[作者:Ple, PA; Jung, F; Ashton, S; Hennequin, L; Laine, R; Lambert-van der Brempt, C; Morgentin, R; Pasquet, G; Taylor, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3050-3055 , 文章类型: Article,,卷期:2012年22-9]
- A new series of quinoline ether inhibitors, which potently and selectively inhibit PDGFR tyrosine kinases, is described in this Letter. Compounds 23 and 33 are selective, low nanomolar inhibitors of PDGFR alpha and beta,...
- Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors
[作者:Fernandez, MC; Escribano, A; Mateo, AI; Parthasarathy, S; de la Nava, EMM; Wang, XD; Cockerham, SL; Beyer, TP; Schmidt, RJ; Cao, GQ; Zhang, YY; Jones, TM; Borel, A; Sweetana, SA; Cannady, EA; Stephenson, G; Frank, S; Mantlo, NB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3056-3062 , 文章类型: Article,,卷期:2012年22-9]
- This Letter describes the discovery and SAR optimization of 1,5-tetrahydronaphthyridines, a new class of potent CETP inhibitors. The effort led to the identification of 21b and 21d with in vitro human plasma CETP inhibit...
- Flavones and structurally related 4-chromenones inhibit carbonic anhydrases by a different mechanism of action compared to coumarins
[作者:Balboni, G; Congiu, C; Onnis, V; Maresca, A; Scozzafava, A; Winum, JY; Maietti, A; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3063-3066 , 文章类型: Article,,卷期:2012年22-9]
- An inhibition study of several carbonic anhydrase (CA, EC 4.2.1.1) isoforms with flavones and aminoflavones, compounds possessing a rather similar scaffold with the coumarins, recently discovered inhibitors of this enzym...
- Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities
[作者:Chang, M; Lee, SH; Kim, HJ; Koh, JS; Kim, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3067-3071 , 文章类型: Article,,卷期:2012年22-9]
- Metabolism of LB42908, a novel farnesyl transferase inhibitor, was investigated for preclinical development. In vitro hepatic metabolism of LB42908 gave rise to at least 9 metabolites via phase I biotransformation pathwa...
- Design, synthesis and anticonvulsant activities of novel 1-(substituted/unsubstituted benzylidene)-4-(4-(6,8-dibromo-2-(methyl/phenyl)-4-oxoquinazolin-3(4H)-yl)phenyl) semicarbazide derivatives
[作者:Saravanan, G; Alagarsamy, V; Prakash, CR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3072-3078 , 文章类型: Article,,卷期:2012年22-9]
- Novel quinazolinone derivatives 5a-5n were designed, synthesized and screened for antiepileptic activity using MES and scPTZ seizures tests. Neurotoxicity study was performed by rotorod test. Compounds 5c, 5d, 5g, 5j and...
- Development of rationally designed DNA N6 adenine methyltransferase inhibitors
[作者:Hobley, G; McKelvie, JC; Harmer, JE; Howe, J; Oyston, PCF; Roach, PL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3079-3082 , 文章类型: Article,,卷期:2012年22-9]
- A series of bisubstrate inhibitors for DNA N6 adenine methyltransferase (Dam) have been synthesized by linking an amine analogue of S-adenosylmethionine to an aryl moiety designed to probe the binding pocket of the DNA a...
- Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P(3)-sparing S1P(1) agonists
[作者:Asano, M; Nakamura, T; Sekiguchi, Y; Mizuno, Y; Yamaguchi, T; Tamaki, K; Shimozato, T; Doi-Komuro, H; Kagari, T; Tomisato, W; Inoue, R; Yuita, H; Oguchi-Oshima, K; Kaneko, R; Nara, F; Kawase, Y; Masubuchi, N; Nakayama, S; Koga, T; Namba, E; Nasu, H; Nishi, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3083-3088 , 文章类型: Article,,卷期:2012年22-9]
- We have previously disclosed 1,2,4-oxadiazole derivative 3 as a potent S1P(3)-sparing S1P(1) agonist. Although compound 3 exhibits potent and manageable immunosuppressive efficacy in various in vivo models, recent studie...
- Quinolinyl- and phenantridinyl-acetamides as bradykinin B1 receptor antagonists
[作者:Eles, J; Beke, G; Vago, I; Bozo, E; Huszar, J; Tarcsay, A; Kolok, S; Schmidt, E; Vastag, M; Hornok, K; Farkas, S; Domany, G; Keseru, GM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3095-3099 , 文章类型: Article,,卷期:2012年22-9]
- A new series of quinolinyl- and phenantridinyl-acetamides were synthesizer and evaluated against bradykinin B1 receptor. In vitro metabolic stability data were reported for the key compounds. The analgesic effect of comp...
- Synthesis, characterization, molecular docking and cytotoxic activity of novel plumbagin hydrazones against breast cancer cells
[作者:Dandawate, P; Khan, E; Padhye, S; Gaba, H; Sinha, S; Deshpande, J; Swamy, KV; Khetmalas, M; Ahmad, A; Sarkar, FH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3104-3108 , 文章类型: Article,,卷期:2012年22-9]
- Novel plumbagin hydrazonates were prepared, structurally characterized and evaluated for anti-proliferative activity against estrogen receptor-positive MCF-7 and triple negative MDA-MB-231 and MDA-MB-468 breast cancer ce...
- Discovery of small molecule HIV-1 integrase dimerization inhibitors
[作者:Tintori, C; Demeulemeester, J; Franchi, L; Massa, S; Debyser, Z; Christ, F; Botta, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3109-3114 , 文章类型: Article,,卷期:2012年22-9]
- Human immunodeficiency virus-1 integrase (HIV-1 IN) inserts the viral DNA into host cell chromatin in a multistep process. This enzyme exists in equilibrium between monomeric, dimeric, tetrameric and high order oligomeri...
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