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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53条记录   Synthesis and cytotoxic activity of heterocyclic ring-substituted betulinic acid derivatives [作者：Kumar, V; Rani, N; Aggarwal, P; Sanna, VK; Singh, AT; Jaggi, M; Joshi, N; Sharma, PK; Irchhaiya, R; Burman, AC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5058-5062 , 文章类型： Article，,卷期：2008年18-18] A new series of betulinic acid derivatives have been synthesized by introducing heterocyclic ring between C-2 and C-3 positions of betulinic acid. Further modi. cations were also carried out by reduction of C-20(29) unsa... Synthesis and evaluation of cis-3,4-disubstituted piperidines as potent CC chemokine receptor 2 (CCR2) antagonists [作者：Cherney, RJ; Nelson, DJ; Lo, YC; Yang, GJ; Scherle, PA; Jezak, H; Solomon, KA; Carter, PH; Decicco, CP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5063-5065 , 文章类型： Article，,卷期：2008年18-18] A series of cis-3,4-disubstituted piperidines was synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. Compound 24 emerged with an attractive pro. le, possessing excellent binding ( CCR2 IC50 = 3.4 nM... Carbonic anhydrase inhibitors: Inhibition of the beta-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with simple anions [作者：Innocenti, A; Muhlschlegel, FA; Hall, RA; Steegborn, C; Scozzafava, A; Supuran, CT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5066-5070 , 文章类型： Article，,卷期：2008年18-18] The catalytic activity and inhibition of the beta-carbonic anhydrases (CAs, EC 4.2.1.1) from the pathogenic fungi Candida albicans ( Nce103) and Cryptococcus neoformans (Can2) with inorganic anions such as halogenides, p... Design, synthesis and preliminary biological evaluation of new hydroxamate histone deacetylase inhibitors as potential antileukemic agents [作者：Guandalini, L; Cellai, C; Laurenzana, A; Scapecchi, S; Paoletti, F; Romanelli, MN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5071-5074 , 文章类型： Article，,卷期：2008年18-18] This study concerns the synthesis of new histone deacetylase inhibitors (HDACi) characterized by a 1,4-benzodiazepine ring used as the cap, joined through an amide function or a triple bond as connection units, to a line... Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands [作者：Fang, J; Akwabi-Ameyaw, A; Britton, JE; Katamreddy, SR; Navas, F; Miller, AB; Williams, SP; Gray, DW; Orband-Miller, LA; Shearin, J; Heyer, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5075-5077 , 文章类型： Article，,卷期：2008年18-18] A series of estrogen receptor ligands based on a 3-alkyl naphthalene scaffold was synthesized using an intramolecular enolate-alkyne cycloaromatization as the key step. Several of these compounds bearing a C6-OH group we... Design, synthesis, and antibacterial activities of novel 3,6-bicyclolide oximes: Length optimization and zero carbon linker oximes [作者：Tang, DT; Gai, YH; Polemeropoulos, A; Chen, ZG; Wang, Z; Or, YS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5078-5082 , 文章类型： Article，,卷期：2008年18-18] We designed and synthesized a series of novel 3,6-bicyclolide oximes, possessing linkers of varying lengths to the secondary binding site. The E isomers exhibited excellent antibacterial profiles against a broad spectrum... Discovery and optimization of (R)-prolinol-derived agonists of the Growth Hormone Secretagogue receptor (GHSR) [作者：Zhai, WX; Flynn, N; Longhi, DA; Tino, JA; Murphy, BJ; Slusarchyk, D; Gordon, DA; Pendri, A; Shi, SH; Stoffel, R; Ma, BQ; Sofia, MJ; Gerritz, SW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5083-5086 , 文章类型： Article，,卷期：2008年18-18] The discovery and optimization of a novel series of prolinol-derived GHSR agonists is described. This series emerged from a 11,520-member solid-phase library targeting the GPCR protein superfamily, and the rapid optimiza... Synthesis and antibacterial activity of the C-7 side chain of 3-aminoquinazolinediones [作者：Hutchings, KM; Tran, TP; Ellsworth, EL; Watson, BM; Sanchez, JP; Showalter, HDH; Stier, MA; Shapiro, M; Joannides, ET; Huband, M; Nguyen, DQ; Maiti, S; Li, T; Tailor, J; Thomas, G; Ha, C; Singh, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5087-5090 , 文章类型： Article，,卷期：2008年18-18] A novel series of bacterial topoisomerase (3-aminoquinazolinediones) inhibitors are described. The side-chain SAR against Gram-positive and Gram-negative organisms as well as DNA gyrase activity is reported. (C) 2008 Els... Design, synthesis, and bioactivity of putative tubulin ligands with adamantane core [作者：Zefirova, ON; Nurieva, EV; Lemcke, H; Ivanov, AA; Shishov, DV; Weiss, DG; Kuznetsov, SA; Zefirov, NS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5091-5094 , 文章类型： Article，,卷期：2008年18-18] Several adamantane-based taxol mimetics were synthesized and found to be cytotoxic at micromolar concentrations and to cause tubulin aggregation. The extent of the aggregation is maximal for N-benzoyl(2R,3S)-phenylisoser... Discovery of novel potent and selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors [作者：Raboisson, P; Lin, TI; de Kock, H; Vendeville, S; de Vreken, WV; McGowan, D; Tahri, A; Hu, L; Lenz, O; Delouvroy, F; Surleraux, D; Wigerinck, P; Nilsson, M; Rosenquist, A; Samuelsson, B; Simmen, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5095-5100 , 文章类型： Article，,卷期：2008年18-18] Starting from the previously reported HCV NS3/4A protease inhibitor BILN 2061 (1), we have used a fast-follower approach to identify a novel series of HCV NS3/4A protease inhibitors in which (i) the P3 amino moiety and i... Synthesis and evaluation of a spiro-isobenzofuranone class of histamine H-3 receptor inverse agonists [作者：Jitsuoka, M; Tsukahara, D; Ito, S; Tanaka, T; Takenaga, N; Tokita, S; Sato, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5101-5106 , 文章类型： Article，,卷期：2008年18-18] Spiro-isobenzofuranones 1a and 1b were discovered as potent, selective, and brain-penetrable non-imidazole H-3 receptor inverse agonists. Our corporate sample collection was screened to identify 2a as a lead. Recognizing... Bradykinin B-1 receptor antagonists: An alpha-hydroxy amide with an improved metabolism profile [作者：Kuduk, SD; Chang, RK; DiPardo, RM; Di Marco, CN; Murphy, KL; Ransom, RW; Reiss, DR; Tang, CY; Prueksaritanont, T; Pettibone, DJ; Bock, MG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5107-5110 , 文章类型： Article，,卷期：2008年18-18] A series of carbo-and heterocyclic alpha-hydroxy amide-derived bradykinin B-1 antagonists were prepared and evaluated. A 4,4-difluorocyclohexyl alpha-hydroxy amide was incorporated along with a 2-methyl tetrazole in lieu... Novel hypoglycemic dihydropyridones serendipitously discovered from O- versus C-alkylation in the synthesis of VMAT2 antagonists [作者：Xie, YL; Raffo, A; Ichise, M; Deng, SX; Harris, PE; Landry, DW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5111-5114 , 文章类型： Article，,卷期：2008年18-18] Vesicular monoamine transporter type 2 (VMAT2) is a newly emerging target for both diagnostic and therapeutic applications in diabetes mellitus. In pursuit of novel VMAT2 antagonists, we identified a potent hypoglycemic ... Discovery of amido-benzisoxazoles as potent c-Kit inhibitors [作者：Kunz, RK; Rumfelt, S; Chen, N; Zhang, D; Tasker, AS; Burli, R; Hungate, R; Yu, V; Nguyen, Y; Whittington, DA; Meagher, KL; Plant, M; Tudor, Y; Schrag, M; Xu, Y; Ng, GY; Hu, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5115-5117 , 文章类型： Article，,卷期：2008年18-18] Deregulation of the receptor tyrosine kinase c-Kit is associated with an increasing number of human diseases, including certain cancers and mast cell diseases. Interference of c-Kit signaling with multi-kinase inhibitors... Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists [作者：Stec, MM; Bo, YX; Chakrabarti, PP; Liao, LL; Ncube, M; Tamayo, N; Tamir, R; Gavva, NR; Treanor, JJS; Norman, MH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5118-5122 , 文章类型： Article，,卷期：2008年18-18] Clinical candidate AMG 517 (1) is a potent antagonist toward multiple modes of activation of TRPV1; however, it suffers from poor solubility. Analogs with various substituents at the R region of 3 were prepared to improv... Synthesis and anti-CVB 3 evaluation of substituted 5-nitro-2-phenoxybenzonitriles [作者：Purstinger, G; De Palma, AM; Zimmerhofer, G; Huber, S; Ladurner, S; Neyts, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5123-5125 , 文章类型： Article，,卷期：2008年18-18] The synthesis and SAR of a series of 60 substituted 2-phenoxy-5-nitrobenzonitriles (analogues of MDL-860) as inhibitors of enterovirus replication (in particular of coxsackievirus B3 (CVB 3)) are reported. Several of the...