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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18条记录   SAR and Lead Optimization of an HIV-1 Vif-APOBEC3G Axis Inhibitor [作者：MOHAMMED IDREES; PARAI MALOY K; JIANG XINPENG; SHAROVA NATALIA; SINGH GATIKRUSHNA; STEVENSON MARIO; RANA TARIQ M,期刊：ACS Medicinal Chemistry Letters, 页码：465-469 , 文章类型： Article，,卷期：2012年3-6] We describe structure activity relationship and optimization studies of RN-18, an HIV-1 Vif-APOBEC3G axis inhibitor. Targeted modifications of RN-18 ring C, ring B, ring A, bridge A B, and bridge B C were performed to id... Novel Cyclopropyl-Indole Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors [作者：HASSAM MOHAMMAD; BASSON ADRIAAN E; LIOTTA DENNIS C; MORRIS LYNN; VAN OTTERLO WILLEM A L; PELLY STEPHEN C,期刊：ACS Medicinal Chemistry Letters, 页码：470-475 , 文章类型： Article，,卷期：2012年3-6] The HIV pandemic represents one of the most serious diseases to face mankind in both a social and economic context, with many developing nations being the worst afflicted. Due to ongoing resistance issues associated with... Synthesis of New Hydrophilic and Hydrophobic Cobinamides as NO-Independent sGC Activators [作者：PROINSIAS KEITH O; GIEDYK MACIEJ; SHARINA IRAIDA G; MARTIN EMIL; GRYKO DOROTA,期刊：ACS Medicinal Chemistry Letters, 页码：476-479 , 文章类型： Article，,卷期：2012年3-6] Herein, the synthesis of novel hydrophobic and hydrophilic cobinamides via aminolysis of vitamin B-12 derivatives that activate soluble guanyl cyclase (sGC) is presented. Unlike other sGC regulators, they target the cata... Deciphering the Resistance-Counteracting Functions of Ferroquine in Plasmodium falciparum-Infected Erythrocytes [作者：DUBAR FAUSTINE; BOHIC SYLVAIN; DIVE DANIEL; GUERARDEL YANN; CLOETENS PETER; KHALIFE JAMAL; BIOT CHRISTOPHE,期刊：ACS Medicinal Chemistry Letters, 页码：480-483 , 文章类型： Article，,卷期：2012年3-6] The aminoquinoline chloroquine (CO) has been widely used for treating malaria since World War II. Resistance to CQ began to spread around 1957 and is now found in all malarious areas of the world. CQ resistance is caused... The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes [作者：HE SHUWEN; YE ZHIXIONG; QUANG TRUONG; SHAH SHRENIK; DU WU; GUO LIANGQIN; DOBBELAAR PETER H; LAI ZHONG; LIU JIAN; JIAN TIANYING; QI HONGBO; BAKSHI RAMAN K; HONG QINGMEI; DELLUREFICIO JAMES; PASTERNAK ALEXANDER; FENG ZHE; DEJESUS REYNALDA; YANG LIHU; REIBARKH MIKHAIL; BRADLEY SCOTT A; HOLMES MARK A; BALL RICHARD G; RUCK REBECCA T; HUFFINAN MARK A; WONG FREDERICK; SAMUEL KOPPARA; REDDY VIJAY B; MITELMAN STAN; TONG SHARON X; CHICCHI GARY G; TSAO KWEILAN; TRUSCA DONNA; WU MARGARET; SHAO QING; TRUJILLO MARIA E; EIERMANN GEORGE J; LI CAI; ZHANG BEI B; HOWARD ANDREW D; ZHOU YUNPING; NARGUND RAVI P; HAGMANN WILLIAM K,期刊：ACS Medicinal Chemistry Letters, 页码：484-489 , 文章类型： Article，,卷期：2012年3-6] A structure-activity relationship study of the imidazolyl-beta-tetrahydrocarboline series identified MK-4256 as a potent, selective SSTR3 antagonist, which demonstrated superior efficacy in a mouse oGTT model. MK-4256 re... Structure-Activity Relationship for Thiirane-Based Gelatinase Inhibitors [作者：LEE MIJOON; IKEJIRI MASAHIRO; KLIMPEL DENNIS; TOTH MARTA; ESPAHBODI MANA; HESEK DUSAN; FORBES CHRISTOPHER; KUMARASIRI MALIKA; NOLL BRUCE C; CHANG MAYLAND; MOBASHERY SHAHRIAR,期刊：ACS Medicinal Chemistry Letters, 页码：490-495 , 文章类型： Article，,卷期：2012年3-6] An extensive structure-activity relationship study with the template of 2-(4-phenoxyphenylsulfonylmethyl)thiirane (1), a potent and highly selective inhibitor for human gelatinases, is reported herein. Syntheses of 65 ne... Thermodynamic Investigation of Inhibitor Binding to 1-Deoxy-D-Xylulose-5-Phosphate Reductoisomerase [作者：CAI GUOBIN; DENG LISHENG; FRYSZCZYN BARTLOMIEJ G; BROWN NICHOLAS G; LIU ZHEN; JIANG HONG; PALZKILL TIMOTHY; SONG YONGCHENG,期刊：ACS Medicinal Chemistry Letters, 页码：496-500 , 文章类型： Article，,卷期：2012年3-6] Isothermal titration calorimetry (ITC) was used to investigate the binding of six inhibitors to 1-deoxy-Dxylulose-5-phosphate reductoisomerase (DXR), a target for developing novel anti-infectives. The binding of hydroxam... Discovery of Imidazoquinolines with Toll-Like Receptor 7/8 Independent Cytokine Induction [作者：SHI CE; XIONG ZHENGMING; CHITTEPU PADMAJA; ALDRICH COURTNEY C; OHLFEST JOHN R; FERGUSON DAVID M,期刊：ACS Medicinal Chemistry Letters, 页码：501-504 , 文章类型： Article，,卷期：2012年3-6] Toll-like receptors (TLRs) are key targets in the design of immunomodulating agents for use as vaccine adjuvants and anticancer treatments. The imidazoquinolines, imiquimod and resiquimod, have been shown to activate TLR... Discovery of HDAC Inhibitors That Lack an Active Site Zn2+-Binding Functional Group [作者：VICKERS CHRIS J; OLSEN CHRISTIAN A; LEMAN LUKE J; GHADIRI M REZA,期刊：ACS Medicinal Chemistry Letters, 页码：505-508 , 文章类型： Article，,卷期：2012年3-6] Natural and synthetic histone deacetylase (HDAC) inhibitors generally derive their strong binding affinity and high potency from a key functional group that binds to the Zn2+ ion within the enzyme active site. However, t... Biotin Analogues with Antibacterial Activity Are Potent Inhibitors of Biotin Protein Ligase [作者：DA COSTA TATIANA P SOARES; TIEU WILLIAM; YAP MIN Y; ZVAREC ONDREJ; BELL JAN M; TURNIDGE JOHN D; WALLACE JOHN C; BOOKER GRANT W; WILCE MATTHEW C J; ABELL ANDREW D; POLYAK STEVEN W,期刊：ACS Medicinal Chemistry Letters, 页码：509-514 , 文章类型： Article，,卷期：2012年3-6] There is a desperate need to develop new antibiotic agents to combat the rise of drug-resistant bacteria, such as clinically important Staphylococcus aureus. The essential multifunctional enzyme, biotin protein ligase (B... Getting the MAX out of Computational Models: The Prediction of Unbound-Brain and Unbound-Plasma Maximum Concentrations [作者：MENTE SCOT; DORAN ANGELA; WAGER TRAVIS T,期刊：ACS Medicinal Chemistry Letters, 页码：515-519 , 文章类型： Article，,卷期：2012年3-6] The objective of this work was to establish that unbound maximum concentrations may be reasonably predicted from a combination of computed molecular properties assuming subcutaneous (SQ) dosing. Additionally, we show tha... Increasing Market Exclusivity for New Drugs, the Cure for What Ails Us? [作者：MILLER CHRIS P,期刊：ACS Medicinal Chemistry Letters, 页码：437-439 , 文章类型： Editorial Material，,卷期：2012年3-6] A New Era for Hepatitis C-New Diagnostics Tools and New Weapons [作者：SORIANO VICENTE,期刊：ACS Medicinal Chemistry Letters, 页码：440-441 , 文章类型： Editorial Material，,卷期：2012年3-6] Drug Repurposing and the Medicinal Chemist [作者：AUBE JEFFREY,期刊：ACS Medicinal Chemistry Letters, 页码：442-444 , 文章类型： Editorial Material，,卷期：2012年3-6] Drug repurposing is an approach to finding new uses for older drugs and has been gaining popularity in recent years. The role of traditional medicinal chemistry in the context of these efforts is considered. Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors [作者：CHO YOUNG SHIN; ANGOVE HAYLEY; BRAIN CHRISTOPHER; CHEN CHRISTINE HIUTUNG; CHENG HONG; CHENG ROBERT; CHOPRA RAJIV; CHUNG KRISTY; CONGREVE MILES; DAGOSTIN CLAUDIO; DAVIS DEBORAH J; FELTEN RUTH; GIRALDES JOHN; HISCOCK STEVEN D; KIM SUNKYU; KOVATS STEVEN; LAGU BHARAT; LEWRY KIM; LOO ALICE; LU YIPIN; LUZZIO MICHAEL; MANIARA WIESIA; MCMENAMIN RACHEL; MORTENSON PAUL N; BENNING RAJDEEP; OREILLY MARC; REES DAVID C; SHEN JUNQING; SMITH TROY; WANG YAPING; WILLIAMS GLYN; WOOLFORD ALISON J A; WRONA WOJCIECH; XU MEI; YANG FAN; HOWARD STEVEN,期刊：ACS Medicinal Chemistry Letters, 页码：445-449 , 文章类型： Article，,卷期：2012年3-6] Herein, we describe the discovery of potent and highly selective inhibitors of both CDK4 and CDK6 via structure-guided optimization of a fragment-based screening hit. CDK6 X-ray crystallography and pharmacokinetic data s... Synthesis and Biochemical Evaluation of Thiochromanone Thiosemicarbazone Analogues as Inhibitors of Cathepsin L [作者：SONG JIANGLI; JONES LINDSAY M; KUMAR G D KISHORE; CONNER ELIZABETH S; BAYEH LIELA; CHAVARRIA GUSTAVO E; CHARLTONSEVCIK AMANDA K; CHEN SHENEN; CHAPLIN DAVID J; TRAWICK MARY LYNN; PINNEY KEVIN G,期刊：ACS Medicinal Chemistry Letters, 页码：450-453 , 文章类型： Article，,卷期：2012年3-6] A series of 36 thiosemicarbazone analogues containing the thiochromanone molecular scaffold functionalized primarily at the C-6 position were prepared by chemical synthesis and evaluated as inhibitors of cathepsins L and...