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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共81条记录   MMP-13 selective alpha-sulfone hydroxamates: A survey of P1 ' heterocyclic amide isosteres [作者：Barta, TE; Becker, DP; Bedell, LJ; Easton, AM; Hockerman, SL; Kiefer, J; Munie, GE; Mathis, KJ; Li, MH; Rico, JG; Villamil, CI; Williams, JM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2820-2822 , 文章类型： Article，,卷期：2011年21-10] Seeking compounds preferentially potent and selective for MMP-13, we reported in the preceding Letter on a series of hydroxamic acids with a flexible benzamide tail groups. (1a) Here, we replace the amide moiety with non... MMP-13 selective alpha-sulfone hydroxamates: Identification of selective P1 ' amides [作者：Fobian, YM; Freskos, JN; Barta, TE; Bedell, LJ; Heintz, R; Kassab, DJ; Kiefer, JR; Mischke, BV; Molyneaux, JM; Mullins, P; Munie, GE; Becker, DP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2823-2825 , 文章类型： Article，,卷期：2011年21-10] Continuing our interest in designing compounds preferentially potent and selective for MMP-13, we report on a series of hydroxamic acids with a flexible amide P1' substituents. We identify an amide which spares both MMP-... Synthesis and antifungal activity of functionalized 2,3-spirostane isomers [作者：Upadhyay, SK; Creech, CC; Bowdy, KL; Stevens, ED; Jursic, BS; Neumann, DM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2826-2831 , 文章类型： Article，,卷期：2011年21-10] Invasive fungal infections are a major complication for individuals with compromised immune systems. One of the most significant challenges in the treatment of invasive fungal infections is the increased resistance of ma... Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y(14) receptor antagonists [作者：Guay, D; Beaulieu, C; Belley, M; Crane, SN; DeLuca, J; Gareau, Y; Hamel, M; Henault, M; Hyjazie, H; Kargman, S; Chan, CC; Xu, LJ; Gordon, R; Li, LH; Mamane, Y; Morin, N; Mancini, J; Therien, M; Tranmer, G; Truong, VL; Wang, ZY; Black, WC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2832-2835 , 文章类型： Article，,卷期：2011年21-10] A weak antagonist of the pyrimidinergic receptor P2Y(14) containing a dihydropyridopyrimidine core was identified through high-throughput screening. Subsequent optimization led to potent, non-UTP competitive antagonists ... Virtual screening identification of novel severe acute respiratory syndrome 3C-like protease inhibitors and in vitro confirmation [作者：Nguyen, TTH; Ryu, HJ; Lee, SH; Hwang, S; Breton, V; Rhee, JH; Kim, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3088-3091 , 文章类型： Article，,卷期：2011年21-10] The 3C-like protease (3CL(pro)) of severe acute respiratory syndrome associated coronavirus (SARS-CoV) is vital for SARS-CoV replication and is a promising drug target. Structure based virtual screening of 308 307 chemic... Synthesis, modelling and kinetic assays of potent inhibitors of purple acid phosphatase [作者：Mohd-Pahmi, SH; Hussein, WM; Schenk, G; McGeary, RP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3092-3094 , 文章类型： Article，,卷期：2011年21-10] Purple acid phosphatases (PAPs) are binuclear metallohydrolases that have been isolated from various mammals, plants, fungi and bacteria. In mammals PAP activity is associated with bone resorption and can lead to bone me... 1,5-Substituted nipecotic amides: Selective PDE8 inhibitors displaying diastereomer-dependent microsomal stability [作者：DeNinno, MP; Wright, SW; Visser, MS; Etienne, JB; Moore, DE; Olson, TV; Rocke, BN; Andrews, MP; Zarbo, C; Millham, ML; Boscoe, BP; Boyer, DD; Doran, SD; Houseknecht, KL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3095-3098 , 文章类型： Article，,卷期：2011年21-10] The first highly potent and selective PDE8 inhibitors are disclosed. The initial tetrahydroisoquinoline hit was transformed into a nipecotic amide series in order to address a reactive metabolite issue. Reduction of lipo... Cyclic lactam hybrid alpha-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors [作者：Mayorov, AV; Cai, MY; Palmer, ES; Tanaka, DK; Cain, JP; Dedek, MM; Tan, B; Trivedi, D; Hruby, VJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3099-3102 , 文章类型： Article，,卷期：2011年21-10] A novel hybrid melanocortin pharmacophore was designed based on the topographical similarities between the pharmacophores of Agouti related protein (AGRP) an endogenous melanocortin antagonist, and alpha-melanocyte-stimu... The identification of 4,7-disubstituted naphthoic acid derivatives as UDP-competitive antagonists of P2Y(14) [作者：Gauthier, JY; Belley, M; Deschenes, D; Fournier, JF; Gagne, S; Gareau, Y; Hamel, M; Henault, M; Hyjazie, H; Kargman, S; Lavallee, G; Levesque, JF; Li, LH; Mamane, Y; Mancini, J; Morin, N; Mulrooney, E; Robichaud, J; Therien, M; Tranmer, G; Wang, ZY; Wu, J; Black, WC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2836-2839 , 文章类型： Article，,卷期：2011年21-10] A weak, UDP-competitive antagonist of the pyrimidinergic receptor P2RY(14) with a naphthoic acid core was identified through high-throughput screening. Optimization provided compounds with improved potency but poor pharm... New monoterpene glycosides and phenolic compounds from Distylium racemosum and their inhibitory activity against ribonuclease H [作者：Kim, JA; Yang, SY; Wamiru, A; McMahon, JB; Le Grice, SFJ; Beutler, JA; Kim, YH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2840-2844 , 文章类型： Article，,卷期：2011年21-10] Two new monoterpene glycosides, distyloside A-B (1-2), and a new megastigmane glucoside, iso-dihydrodendranthemoside A (3) were isolated from twigs and leaves of Distylium racemosum, along with five known phenolic compou... Cytotoxic and PPARs transcriptional activities of sterols from the Vietnamese soft coral Lobophytum laevigatum [作者：Quang, TH; Ha, TT; Van Minh, C; Van Kiem, P; Huong, HT; Nguyen, TTN; Nhiem, NX; Tung, NH; Thao, NP; Thuy, DTT; Song, SB; Boo, HJ; Kang, HK; Kim, YH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2845-2849 , 文章类型： Article，,卷期：2011年21-10] A new unusual sterol, named lobophytosterol (1), and five known metabolites (2-6) were isolated from the methanol extract of the soft coral Lobophytum laevigatum. Their chemical structures were elucidated by extensive sp... Revisiting glitazars: Thiophene substituted oxazole containing alpha-ethoxy phenylpropanoic acid derivatives as highly potent PPAR alpha/gamma dual agonists devoid of adverse effects in rodents [作者：Raval, P; Jain, M; Goswami, A; Basu, S; Gite, A; Godha, A; Pingali, H; Raval, S; Giri, S; Suthar, D; Shah, M; Patel, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3103-3109 , 文章类型： Article，,卷期：2011年21-10] In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, novel thiophene substituted oxazole containing alpha-alkoxy-phenylpropanoic acid derivatives are designed as highly potent ... Design, synthesis and antiproliferative activity of novel aminosubstituted benzothiopyranoisoindoles [作者：Christodoulou, A; Kostakis, IK; Kourafalos, V; Pouli, N; Marakos, P; Trougakos, IP; Tsitsilonis, OE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3110-3112 , 文章类型： Article，,卷期：2011年21-10] The synthesis of a number of new benzothiopyrano[4,3,2-cd] isoindole aminoderivatives designed as structural analogues of the key metabolite of the anticancer agent Ledacrine ( nitracrine) and their in vitro cytotoxic ac... Triamino pyrimidines and pyridines as histamine H-4 receptor modulators [作者：Meduna, SP; Savall, BM; Cai, H; Edwards, JP; Thurmond, RL; McGovern, PM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3113-3116 , 文章类型： Article，,卷期：2011年21-10] Two series of triamino pyrimidines and a series of triamino pyridines have been synthesized and their structure-activity relationships evaluated for activity at the H-4 receptor in competitive binding and functional assa... Synthesis and antiproliferative activity of new cytotoxic azanaphthoquinone pyrrolo-annelated derivatives: Part II [作者：Shanab, K; Schirmer, E; Wulz, E; Weissenbacher, B; Lassnig, S; Slanz, R; Fosleitner, G; Holzer, W; Spreitzer, H; Schmidt, P; Aicher, B; Muller, G; Gunther, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3117-3121 , 文章类型： Article，,卷期：2011年21-10] A series of 6-azanaphthoquinone pyrrolo-annelated derivatives carrying different basic side chains have been synthesized. The antiproliferative activities of all compounds were evaluated on at least four different cell l... Synthesis and in vitro evaluation of [F-18]fluoroethyl triazole labelled [Tyr(3)]octreotate analogues using click chemistry [作者：Iddon, L; Leyton, J; Indrevoll, B; Glaser, M; Robins, EG; George, AJT; Cuthbertson, A; Luthra, SK; Aboagye, EO,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3122-3127 , 文章类型： Article，,卷期：2011年21-10] A novel class of alkyne linked [Tyr(3)]octreotate analogues have been labelled by a copper catalysed azide-alkyne cycloaddition reaction (CuAAC) to form a 1,4-substituted triazole using the reagent [F-18]2-fluoroethyl az...