- Inhibitory effect on NO production of phenolic compounds from Myristica fragrans
[作者:Cuong, TD; Hung, TM; Na, M; Ha, DT; Kim, JC; Lee, D; Ryoo, S; Lee, JH; Choi, JS; Min, BS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6884-6887 , 文章类型: Article,,卷期:2011年21-22]
- Three new phenolics: ((7S)-8'-(benzo[3',4']dioxol-1'-yl)-7-hydroxypropyl)benzene-2,4-diol (1), ((7S)-8'- (4'-hydroxy-3'-methoxyphenyl)-7-hydroxypropyl)benzene-2,4-diol (2) and ((8R,8'S)-7-(4-hydroxy-3-methoxyphenyl)-8'-m...
- Identification and SAR of selective inducible nitric oxide synthase (iNOS) dimerization inhibitors
[作者:Gahman, TC; Herbert, MR; Lang, H; Thayer, A; Symons, KT; Nguyen, PM; Massari, ME; Dozier, S; Zhang, Y; Sablad, M; Rao, TS; Noble, SA; Shiau, AK; Hassig, CA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6888-6894 , 文章类型: Article,,卷期:2011年21-22]
- We have identified and synthesized a series of imidazole containing dimerization inhibitors of inducible nitric oxide synthase (iNOS). The necessity of key imidazole and piperonyl functionality was demonstrated and SAR s...
- Design, synthesis, and biological activity of a novel series of 2,5-disubstituted furans/pyrroles as HIV-1 fusion inhibitors targeting gp41
[作者:Jiang, SB; Tala, SR; Lu, H; Zou, P; Avan, I; Ibrahim, TS; Abo-Dya, NE; Abdelmajeid, A; Debnath, AK; Katritzky, AR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6895-6898 , 文章类型: Article,,卷期:2011年21-22]
- Based on molecular docking analysis of earlier results, we designed a series of 2,5-disubstituted furans/pyrroles (5a-h) as HIV-1 entry inhibitors. Compounds were synthesized by Suzuki-Miyaura cross coupling, followed by...
- Identification of novel NK(1)/NK(3) dual antagonists for the potential treatment of schizophrenia
[作者:Catalani, MP; Alvaro, G; Bernasconi, G; Bettini, E; Bromidge, SM; Heer, J; Tedesco, G; Tommasi, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6899-6904 , 文章类型: Article,,卷期:2011年21-22]
- During the lead optimization of NK(1)/NK(3) receptor antagonists program, a focused exploration of molecules bearing a lactam moiety was performed. The aim of the investigation was to identify the optimal position of the...
- Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors
[作者:Thompson, LA; Shi, JL; Decicco, CP; Tebben, AJ; Olson, RE; Boy, KM; Guernon, JM; Good, AC; Liauw, A; Zheng, CS; Copeland, RA; Combs, AP; Trainor, GL; Camac, DM; Muckelbauer, JK; Lentz, KA; Grace, JE; Burton, CR; Toyn, JH; Barten, DM; Marcinkeviciene, J; Meredith, JE; Albright, CF; Macor, JE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6909-6915 , 文章类型: Article,,卷期:2011年21-22]
- The synthesis, evaluation, and structure-activity relationships of a set of related constrained diaminopropane inhibitors of BACE-1 are described. The full in vivo profile of an optimized inhibitor in both normal and P-g...
- Monosubstituted gamma-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of beta-secretase (BACE)
[作者:Boy, KM; Guernon, JM; Shi, JL; Toyn, JH; Meredith, JE; Barten, DM; Burton, CR; Albright, CF; Marcinkeviciene, J; Good, AC; Tebben, AJ; Muckelbauer, JK; Camac, DM; Lentz, KA; Bronson, JJ; Olson, RE; Macor, JE; Thompson, LA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6916-6924 , 文章类型: Article,,卷期:2011年21-22]
- The synthesis, evaluation, and structure-activity relationships of a class of gamma-lactam 1,3-diaminopropan-2-ol transition-state isostere inhibitors of BACE are discussed. Two strategies for optimizing lead compound 1a...
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