- Vasodilatation effect of farnesylacetones, active constituents of Sargassum siliquastrum, on the basilar and carotid arteries of rabbits
[作者:Park, BG; Kwon, SC; Park, GM; Ham, J; Shin, WS; Lee, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6324-6326 , 文章类型: Article,,卷期:2008年18-24]
- Two farnesylacetones, 311 and 312, major active constituents of Sargassum siliquastrum collected from the coast of the East Sea in Korea, showed a moderate vasodilatation effect on the basilar arteries of rabbits. Theref...
- Carbonic anhydrase inhibitors. Inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with anions
[作者:Isik, S; Kockar, F; Arslan, O; Guler, OO; Innocenti, A; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6327-6331 , 文章类型: Article,,卷期:2008年18-24]
- The protein encoded by the Nce103 gene of Saccharomyces cerevisiae, a beta-carbonic anhydrase (CA, EC 4.2.1.1) designated as scCA, has been cloned, purified, characterized kinetically, and investigated for its inhibition...
- Carbonic anhydrase inhibitors: 2-Substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV
[作者:Smaine, FZ; Pacchiano, F; Rami, M; Barragan-Montero, V; Vullo, D; Scozzafava, A; Winum, JY; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6332-6335 , 文章类型: Article,,卷期:2008年18-24]
- A series of 2-substituted-1,3,4-thiadiazole-5-sulfamides was prepared and assayed as inhibitors of several carbonic anhydrase (CA, EC 4.2.1.1) isoforms, the cytosolic CA I and II, the membrane-associated CA IV and the mi...
- Synthesis of BODIPY-labeled alkylphosphocholines with leishmanicidal activity, as fluorescent analogues of miltefosine
[作者:Hornillos, V; Carrillo, E; Rivas, L; Amat-Guerri, F; Acuna, AU,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6336-6339 , 文章类型: Article,,卷期:2008年18-24]
- Two general synthetic methods are described, by which the highly fluorescent and photostable BODIPY group can be inserted in and aligned with the alkyl backbone of linear lipids. These methods have been used to prepare s...
- Structure-activity relationships of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the treatment of cough
[作者:Yang, SW; Ho, G; Tulshian, D; Greenlee, WJ; Fernandez, X; McLeod, RL; Eckel, S; Anthes, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6340-6343 , 文章类型: Article,,卷期:2008年18-24]
- A series of 3-axial-aminomethyl-N-benzhydryl-nortropane analogs have been synthesized and identified to bind to the nociceptin receptor with high affinity. Many of these analogs showed high binding selectivity over class...
- Orally bioavailable prodrugs of a BCS class 2 molecule, an inhibitor of HIV-1 reverse transcriptase
[作者:Elworthy, TR; Dunn, JP; Hogg, JH; Lam, G; Saito, YD; Silva, TMPC; Stefanidis, D; Woroniecki, W; Zhornisky, E; Zhou, AS; Klumpp, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6344-6347 , 文章类型: Article,,卷期:2008年18-24]
- The N-2 position of pyridazinone 1, a potent HIV-1 NNRTI that has limited aqueous solubility, was derivatized into a series of hydroxymethyl esters and carbonates as well as one phosphate. The derivatives served as prodr...
- Identification and optimization of N-3,N-6-diaryl-1H-pyrazolo[3,4-d] pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors
[作者:Kopecky, DJ; Hao, XL; Chen, Y; Fu, JS; Jiao, XY; Jaen, JC; Cardozo, MG; Liu, JS; Wang, ZL; Walker, NPC; Wesche, H; Li, S; Farrelly, E; Xiao, SH; Kayser, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6352-6356 , 文章类型: Article,,卷期:2008年18-24]
- A new series of pyrazolo[3,4-d] pyrimidine-3,6-diamines was designed and synthesized as potent and selective inhibitors of the nonreceptor tyrosine kinase, ACK1. These compounds arose from efforts to rigidify an earlier ...
- Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists
[作者:Bharate, SB; Rodge, A; Joshi, RK; Kaur, J; Srinivasan, S; Kumar, SS; Kulkarni-Almeida, A; Balachandran, S; Balakrishnan, A; Vishwakarma, RA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6357-6361 , 文章类型: Article,,卷期:2008年18-24]
- In this letter, we report discovery of diacylphloroglucinol compounds as a new class of GPR40 (FFAR1) agonists. Several diacylphloroglucinols with varying length of acyl functionality and substitution on aromatic hydroxy...
- Synthesis and cytotoxic activities of 1-benzylidine substituted beta-carboline derivatives
[作者:Cao, RH; Yi, W; Wu, QF; Guan, XD; Feng, MX; Ma, CM; Chen, ZY; Song, HC; Peng, WL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6558-6561 , 文章类型: Article,,卷期:2008年18-24]
- A series of new beta-carboline derivatives, bearing a benzylidine substituent at position-1, has been prepared and evaluated in vitro against a panel of human cell lines. The N-2-benzylated beta-carbolinium bromates repr...
- Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: Design, synthesis, and evaluation as topically applied, dermal anti-scarring agents
[作者:Bailey, S; Fish, PV; Billotte, S; Bordner, J; Greiling, D; James, K; McElroy, A; Mills, JE; Reed, C; Webster, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6562-6567 , 文章类型: Article,,卷期:2008年18-24]
- Succinyl hydroxamates 1 and 2 are disclosed as novel series of potent and selective inhibitors of procollagen C-proteinase (PCP) which may have potential as anti-fibrotic agents. Carboxamide 7 demonstrated good PCP inhib...
- Peptide deformylase inhibitors of Mycobacterium tuberculosis: Synthesis, structural investigations, and biological results
[作者:Pichota, A; Duraiswamy, J; Yin, Z; Keller, TH; Alam, J; Liung, S; Lee, G; Ding, M; Wang, G; Chan, WL; Schreiber, M; Ma, I; Beer, D; Ngew, X; Mukherjee, K; Nanjundappa, M; Teo, JWP; Thayalan, P; Yap, A; Dick, T; Meng, W; Xu, M; Koehn, J; Pan, SH; Clark, K; Xie, X; Shoen, C; Cynamon, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6568-6572 , 文章类型: Article,,卷期:2008年18-24]
- Bacterial peptide deformylase (PDF) belongs to a subfamily of metalloproteases catalyzing the removal of the N-terminal formyl group from newly synthesized proteins. We report the synthesis and biological activity of hig...
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