- In vitro and in vivo antifilarial activity evaluation of 3,6-epoxy [1,5]dioxocines: A new class of antifilarial agents
[作者:Sashidhara, KV; Kumar, A; Rao, KB; Kushwaha, V; Saxena, K; Murthy, PK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1527-1532 , 文章类型: Article,,卷期:2012年22-4]
- A series of 3,6-epoxy [1,5] dioxocines were synthesized and evaluated for their antifilarial activity against adult parasites of human lymphatic filarial parasite Brugia malayi (sub-periodic strain) in vitro. Out of thes...
- Concise synthesis of (+)-conduritol F and inositol analogues from naturally available (+)-proto-quercitol and their glucosidase inhibitory activity
[作者:Worawalai, W; Rattanangkool, E; Vanitcha, A; Phuwapraisirisan, P; Wacharasindhu, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1538-1540 , 文章类型: Article,,卷期:2012年22-4]
- An effective synthesis of (+)-conduritol F, (+)-chiro-and (+)-epi-inositols from naturally available (+)proto- quercitol is described. This synthetic method provides a concise synthesis of cyclitols in enantiomerically p...
- Novel morpholine ketone analogs as potent histamine H-3 receptor inverse agonists with wake activity
[作者:Sundar, BG; Bailey, TR; Dunn, D; Hostetler, GA; Chatterjee, S; Bacon, ER; Yue, C; Schweizer, D; Aimone, LD; Gruner, JA; Lyons, J; Raddatz, R; Lesur, B,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1546-1549 , 文章类型: Article,,卷期:2012年22-4]
- Structure-activity relationship on a novel ketone class of H3R antagonists/inverse agonists is disclosed. Compound 4 showed excellent target potency, selectivity and brain penetration. Evaluation of antagonist 4 in the r...
- Discovery of benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitors
[作者:Shen, HC; Ding, FX; Jiang, JL; Verras, A; Chabin, RM; Xu, SY; Tong, XC; Chen, Q; Xie, D; Lassman, ME; Bhatt, UR; Garcia-Calvo, MM; Geissler, W; Shen, Z; Murphy, BA; Gorski, JN; Wiltsie, J; SinhaRoy, R; Hale, JJ; Pinto, S; Shen, DM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1550-1556 , 文章类型: Article,,卷期:2012年22-4]
- A series of benzodihydroisofurans were discovered as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase (PrCP) inhibitors. The structure-activity relationship (SAR) is focused on improving PrCP activi...
- Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors
[作者:Truppo, E; Supuran, CT; Sandomenico, A; Vullo, D; Innocenti, A; Di Fiore, A; Alterio, V; De Simone, G; Monti, SM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1560-1564 , 文章类型: Article,,卷期:2012年22-4]
- Human carbonic anhydrase (CA, EC 4.2.1.1) VII is a cytosolic enzyme with high carbon dioxide hydration activity. Here we report an unexpected S-glutathionylation of hCA VII which has also been observed earlier in vivo fo...
- Discovery of dimeric inhibitors by extension into the entrance channel of HIV-1 reverse transcriptase
[作者:Ekkati, AR; Bollini, M; Domaoal, RA; Spasov, KA; Anderson, KS; Jorgensen, WL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1565-1568 , 文章类型: Article,,卷期:2012年22-4]
- Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase is being pursued with computational guidance. Extension of azine-containing inhibitors into the entrance channel between Lys103 and Glu138 has led to the...
- [C-11]GSK2126458 and [F-18]GSK2126458, the first radiosynthesis of new potential PET agents for imaging of PI3K and mTOR in cancers
[作者:Wang, M; Gao, MZ; Miller, KD; Sledge, GW; Zheng, QH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1569-1574 , 文章类型: Article,,卷期:2012年22-4]
- GSK2126458 is a highly potent inhibitor of phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) with low picomolar to subnanomolar activity. [C-11]GSK2126458 and [F-18]GSK212 6458, new potential PET ...
- Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain
[作者:Bennett, CE; Burnett, DA; Greenlee, WJ; Knutson, CE; Korakas, P; Li, C; Tulshian, D; Wu, WL; Bertorelli, R; Fredduzzi, S; Grilli, M; Lozza, G; Reggiani, A; Veltri, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1575-1578 , 文章类型: Article,,卷期:2012年22-4]
- A series of fused tricyclic mGluR1 antagonists containing a pyridone ring were synthesized. In vitro, these antagonists were potent against both human and rat isozymes, as well as selective for inhibiting mGluR1 over mGl...
- Design and synthesis of novel inhibitors of human kynurenine aminotransferase-I
[作者:Akladios, FN; Nadvi, NA; Park, J; Hanrahan, JR; Kapoor, V; Gorrell, MD; Church, WB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1579-1581 , 文章类型: Article,,卷期:2012年22-4]
- Herein we report 6-ethoxy-6-oxo-5-(2-phenylhydrazono) hexanoic acid and 3-(2-carboxyethyl)-1H-indole- 2-carboxylic acid derivatives as synthetically accessible leads for human kynurenine aminotransferase-I (KAT-I) inhibi...
- Praziquantel derivatives exhibit activity against both juvenile and adult Schistosoma japonicum
[作者:Duan, WW; Qiu, SJ; Zhao, Y; Sun, HA; Qiao, CH; Xia, CM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1587-1590 , 文章类型: Article,,卷期:2012年22-4]
- A praziquantel analog 10-hydroxy praziquantel and eight praziquantel/peroxide conjugates were synthesized. The biological activity of these compounds was evaluated against juvenile and adult stages of Schistosoma japonic...
- Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors
[作者:Pastor, J; Oyarzabal, J; Saluste, G; Alvarez, RM; Rivero, V; Ramos, F; Cendon, E; Blanco-Aparicio, C; Ajenjo, N; Cebria, A; Albarran, MI; Cebrian, D; Corrionero, A; Fominaya, J; Montoya, G; Mazzorana, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1591-1597 , 文章类型: Article,,卷期:2012年22-4]
- PIM kinases have become targets of interest due to their association with biochemical mechanisms affecting survival, proliferation and cytokine production. 1,2,3-Triazolo[4,5-b]pyridines were identified as PIM inhibitors...
- Synthesis and antimycobacterial evaluation of N-substituted 3-aminopyrazine-2,5-dicarbonitriles
[作者:Zitko, J; Jampilek, J; Dobrovolny, L; Svobodova, M; Kunes, J; Dolezal, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1598-1601 , 文章类型: Article,,卷期:2012年22-4]
- A series of 14 new compounds related to pyrazinamide were synthesized, characterized with analytical data and screened for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii an...
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