- A beta-tryptase inhibitor with a tropanylamide scaffold to improve in vitro stability and to lower hERG channel binding affinity
[作者:Liang, GY; Choi-Sledeski, YM; Shum, P; Chen, X; Poli, GB; Kumar, V; Minnich, A; Wang, QP; Tsay, J; Sides, K; Kang, JS; Zhang, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1606-1610 , 文章类型: Article,,卷期:2012年22-4]
- Tropanylamide was investigated as a possible scaffold for beta-tryptase inhibitors with a basic benzylamine P1 group and a substituted thiophene P4 group. Comparing to piperidinylamide, the tropanylamide scaffold is much...
- Imidazopyridines as selective CYP3A4 inhibitors
[作者:Song, XY; Li, XH; Ruiz, CH; Yin, Y; Feng, YB; Kamenecka, TM; Cameron, MD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1611-1614 , 文章类型: Article,,卷期:2012年22-4]
- Cytochrome P450s are the major family of enzymes responsible for the oxidative metabolism of pharmaceuticals and xenobiotics. CYP3A4 and CYP3A5 have been shown to have overlapping substrate and inhibitor profiles and the...
- Microbial transformation of deoxyandrographolide and their inhibitory activity on LPS-induced NO production in RAW 264.7 macrophages
[作者:Deng, S; Zhang, BJ; Wang, CY; Tian, Y; Yao, JH; An, L; Huang, SS; Peng, JY; Liu, KX; Ma, XC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1615-1618 , 文章类型: Article,,卷期:2012年22-4]
- A series of analogues of deoxyandrographolide (1) transformed by Cunninghamella blakesleana AS 3.2004 were isolated and identified by spectral methods including 2D NMR. Among them, 3-oxo-17,19-dihydroxy-7,13-ent-labdadie...
- gamma-Carbolines: A novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration
[作者:Cheng, YX; Pourashraf, M; Luo, XH; Srivastava, S; Walpole, C; Salois, D; St-Onge, S; Payza, K; Lessard, E; Yu, XH; Tomaszewski, MJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1619-1624 , 文章类型: Article,,卷期:2012年22-4]
- An oral, peripherally restricted CB1/CB2 agonist could provide an interesting approach to treat chronic pain by harnessing the analgesic properties of cannabinoids but without the well-known central side effects. gamma-C...
- Synthesis of novel brassinosteroid biosynthesis inhibitors based on the ketoconazole scaffold
[作者:Oh, K; Yamada, K; Asami, T; Yoshizawa, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1625-1628 , 文章类型: Article,,卷期:2012年22-4]
- Brassinosteroids (BRs) are steroidal plant hormones that control several important agronomic traits such as plant architecture, seed yield, and stress tolerance. Inhibitors that target BR biosynthesis are candidate plant...
- SAR of alpha 7 nicotinic receptor agonists derived from tilorone: Exploration of a novel nicotinic pharmacophore
[作者:Schrimpf, MR; Sippy, KB; Briggs, CA; Anderson, DJ; Li, T; Ji, JG; Frost, JM; Surowy, CS; Bunnelle, WH; Gopalakrishnan, M; Meyer, MD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1633-1638 , 文章类型: Article,,卷期:2012年22-4]
- The well-known interferon-inducer tilorone was found to possess potent affinity for the agonist site of the alpha 7 neuronal nicotinic receptor (K-i = 56 nM). SAR investigations determined that both basic sidechains are ...
- Synthesis and antihypertensive activity of pyrimidin-4(3H)-one derivatives as losartan analogue for new angiotensin II receptor type 1 (AT(1)) antagonists
[作者:Kim, TW; Yoo, BW; Lee, JK; Kim, JH; Lee, KT; Chi, YH; Lee, JY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1649-1654 , 文章类型: Article,,卷期:2012年22-4]
- The discovery, in vitro and in vivo studies of the highly potent AT(1) antagonist 12a (BR-A-657, Fimasartan) are presented. A series of pyrimidin-4(3H)-one derivatives as losartan analogue were synthesized and evaluated ...
- Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis
[作者:Cumming, JG; Tucker, H; Oldfield, J; Fielding, C; Highton, A; Faull, A; Wild, M; Brown, D; Wells, S; Shaw, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1655-1659 , 文章类型: Article,,卷期:2012年22-4]
- Modifications to a series of potent and selective substituted 1-(3,3-diphenylpropyl)-piperidine phenylacetamide CCR5 antagonists were explored with the aim of reducing affinity at the hERG cardiac ion channel. Replacemen...
- Inhibitory activity of eudesmane sesquiterpenes from Alpinia oxyphylla on production of nitric oxide
[作者:Xu, JJ; Ji, CJ; Zhang, YM; Su, J; Li, Y; Tan, NH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1660-1663 , 文章类型: Article,,卷期:2012年22-4]
- Sixteen eudesmane-type sesquiterpenes including seven new compounds oxyphyllanene A-G (1-2 and 5-9) were isolated from the fruits of Alpinia oxyphylla. Among them, compounds 1-2 are novel trinoreudesmane sesquiterpenes, ...
- Synthesis, characterization and biological activity of a niobium-substituted-heteropolytungstate on hepatitis B virus
[作者:Zhang, H; Qi, YF; Ding, YH; Wang, J; Li, QM; Zhang, JZ; Jiang, YF; Chi, XM; Li, J; Niu, JQ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1664-1669 , 文章类型: Article,,卷期:2012年22-4]
- To synthesise and characterize the polyoxometalate Cs2K4Na[SiW9Nb3O40]center dot H2O 1 for its anti-hepatitis B virus (HBV) properties by using the HepG2.2.15 cell. The methylthiazol tetrazolium assay was used to evaluat...
- Targeting the estrogen receptor with metal-carbonyl derivatives of estradiol
[作者:Hanson, RN; Kirss, R; McCaskill, E; Hua, E; Tongcharoensirikul, P; Olmsted, SL; Labaree, D; Hochberg, RB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1670-1673 , 文章类型: Article,,卷期:2012年22-4]
- As part of our program to develop new probes for the estrogen receptor binding domain, we prepared and evaluated a novel 17 alpha-(rhenium tricarbonyl bipyridyl) vinyl estradiol complex. Preparation of the final compound...
- Synthesis and biological evaluation of [6]-gingerol analogues as transient receptor potential channel TRPV1 and TRPA1 modulators
[作者:Morera, E; De Petrocellis, L; Morera, L; Moriello, AS; Nalli, M; Di Marzo, V; Ortar, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1674-1677 , 文章类型: Article,,卷期:2012年22-4]
- In order to explore the structural determinants for the TRPV1 and TRPA1 agonist properties of gingerols, a series of nineteen analogues (1b-5) of racemic [6]-gingerol (1a) was synthesized and tested on TRPV1 and TRPA1 ch...
|