Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Vaibhav, Varkhedkar"'
Autor:
David L. Linemeyer, M Venkat Reddy, Zhili Sun, James M. Fujitaki, David B. Olsen, Mark D. Erion, Serge H. Boyer, Vaibhav Varkhedkar, Kenneth A Koeplinger, Scott J. Hecker, Paul D. van Poelje, K. Raja Reddy, Malcolm Maccoss, Wenjian Huang
Publikováno v:
Journal of Medicinal Chemistry. 50:3891-3896
2'-C-Methyladenosine exhibits impressive inhibitory activity in the cell-based hepatitis C virus (HCV) subgenomic replicon assay, by virtue of intracellular conversion to the corresponding nucleoside triphosphate (NTP) and inhibition of NS5B RNA-depe
Autor:
Venkata Palle, Dewan Zeng, Arthur Gimbel, Xiaofen Li, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Rao Kalla, Jeff Zablocki, Tennig Maa
Publikováno v:
Journal of Medicinal Chemistry. 49:3682-3692
Adenosine has been suggested to induce bronchial hyperresponsiveness in asthmatics, which is believed to be an A(2B) adenosine receptor (AdoR) mediated pathway. We hypothesize that a selective, high-affinity A(2B) AdoR antagonist may provide therapeu
Autor:
Irving Fong, Elfatih Elzein, Prabha Ibrahim, Lin Wu, Jeff Zablocki, Timothy A. Marquart, Yuzhi Wu, David Lustig, Dewan Zeng, Christopher Morrison, Tenning Maa, Bob Jiang, Kevin D. Shenk, Kwan Leung, Venkata Palle, Vaibhav Varkhedkar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:3793-3797
Atrial fibrillation (AF) is the most commonly encountered sustained clinical arrhythmia with an estimated 2.3 million cases in the US (2001). A(1) adenosine receptor agonists can slow the electrical impulse propagation through the atrioventricular (A
Publikováno v:
Journal of Medicinal Chemistry. 43:4694-4700
The synthesis and biological evaluation of three classes of chain-modified derivatives of (+)-EHNA are described. Among the 5', 6'-unsaturated derivatives, the Z-isomer was the most potent inhibitor of adenosine deaminase (ADA) but 3-fold less active
Autor:
Kara A. Loiacono, Ian A. MacNeil, Berkley A. Lynch, Taylor Merry, Chi B. Vu, Ukti Mani, Vaibhav Varkhedkar, John L. Buchanan, Dennis A. Holt, Selvaluxmi G. Pradeepan, Hilary R. Plake, Michael Yang, Evelyn G. Corpuz, Choi Lai Tiong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:2359-2364
The structure-activity relationships (SAR) of a novel class of Src SH2 inhibitors are described. Variation at the pY+1 and pY+3 side chain positions using 2,4- and 2,5-substituted thiazoles and 1,2,4-oxadiazoles as scaffolds resulted in inhibitors th
Autor:
Taylor Merry, Selvi Pradeepan, Raji Sundaramoorthi, Virginia A. Jacobsen, Mayumi Uesugi, Vaibhav Varkhedkar, Chi B. Vu, Chester A. Metcalf, Jeremy Green, Dennis A. Holt, Edgardo Laborde, Karina J. Macek, Yinka Green
Publikováno v:
Tetrahedron Letters. 39:3435-3438
An efficient method for the preparation of protected phosphate ester-linked resins in high yield and purity is presented. Variation in tether length/functionality and substitution pattern of the phenol precursors, as well as mild deprotection conditi
Publikováno v:
ChemInform. 29
Several 9-aralkyladenines have been prepared and their ADA inhibitory activity was determined. A minimum of two carbon atoms separating the aromatic ring from the adenine-bearing carbon (C3′) was found essential for potent activity.
Autor:
Rao V, Kalla, Elfatih, Elzein, Thao, Perry, Xiaofen, Li, Venkata, Palle, Vaibhav, Varkhedkar, Arthur, Gimbel, Tennig, Maa, Dewan, Zeng, Jeff, Zablocki
Publikováno v:
Journal of medicinal chemistry. 49(12)
Adenosine has been suggested to induce bronchial hyperresponsiveness in asthmatics, which is believed to be an A(2B) adenosine receptor (AdoR) mediated pathway. We hypothesize that a selective, high-affinity A(2B) AdoR antagonist may provide therapeu
Autor:
Dengming Xiao, Jia Hao, Piscopio Anthony D, Art Gimbel, Thao Perry, Venkata Palle, Jeff Zablocki, Dewan Zeng, Vaibhav Varkhedkar, Kwan Leung, Rao Kalla, Nancy Chu, Tenning Maa
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(3)
Adenosine has been suggested to play a role in asthma, possibly via activation of A2B adenosine receptors on mast cells and other pulmonary cells. We describe our initial efforts to discover a xanthine based selective A2B AdoR antagonist that resulte
Autor:
Venkata P. Palle, Prabha Ibrahim, Yuzhi Wu, Dewan Zeng, Nancy Chu, Kwan Leung, Zhihe Li, Hiba Ahmed, Vaibhav Varkhedkar, Zhenhai Gao, Mark Ozeck, Lin Wu, Jeff Zablocki
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(2)
The SAR for the affinity to the A(1) adenosine receptor and relative intrinsic efficacy (IE, [(35)S]-GTPgammaS binding) of a series of 5'-carbamate and 5'-thionocarbamate derivatives of tecadenoson is described. Based on this SAR, selected compounds