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10.1016/j.bbamem.2015.01.004 http://scihub22266oqcxt.onion/10.1016/j.bbamem.2015.01.004 C4364388!4364388!25613743     free     free     free Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       Biochim+Biophys+Acta 2015 ; 1848 (5): 1075-80 Nephropedia Template TP {{tp|p=25613743|t=2015. Structure-activity analysis of thiourea analogs as inhibitors of UT-A and UT-B urea transporters |pdf=|usr=}}{{25613743}} gab.com Text Structure-activity analysis of thiourea analogs as inhibitors of UT-A and UT-B urea transporters JO: Biochim Biophys Acta http://www.kidney.de/pget.php?&tw=1&pmid=25613743 #FOAvip Small-molecule inhibitors of urea transporter (UT) proteins in kidney have potential application as novel salt-sparing diuretics. The urea analog dimethylthiourea (DMTU) was recently found to inhibit the UT isoforms UT-A1 (expressed in kidney tubule epithelium) and UT-B (expressed in kidney vasa recta endothelium) with IC50 of 2-3 mM, and was shown to have diuretic action when administered to rats. Here, we measured UT-A1 and UT-B inhibition activity of 36 thiourea analogs, with the goal of identifying more potent and isoform-selective inhibitors, and establishing structure-activity relationships. The analog set systematically explored modifications of substituents on the thiourea including alkyl, heterocycles and phenyl rings, with different steric and electronic features. The analogs had a wide range of inhibition activities and selectivities. The most potent inhibitor, 3-nitrophenyl-thiourea, had an IC50 of ?0.2 mM for inhibition of both UT-A1 and UT-B. Some analogs such as 4-nitrophenyl-thiourea were relatively UT-A1 selective (IC50 1.3 vs. 10 mM), and others such as thioisonicotinamide were UT-B selective (IC50 >15 vs. 2.8 mM). Twit Text FOAVip Structure-activity analysis of thiourea analogs as inhibitors of UT-A and UT-B urea transporters ????Biochim Biophys Acta http://www.kidney.de/pget.php?&tw=1&pmid=25613743 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=25613743 #FOAvip English Wikipedia <ref>{{Cite pmid|25613743}}</ref> Structure-activity analysis of thiourea analogs as inhibitors of UT-A and UT-B urea transporters #MMPMID25613743 Esteva-Font C; Phuan PW; Lee S; Su T; Anderson MO; Verkman AS Biochim Biophys Acta 2015[May]; 1848 (5): 1075-80 PMID25613743show ga Small-molecule inhibitors of urea transporter (UT) proteins in kidney have potential application as novel salt-sparing diuretics. The urea analog dimethylthiourea (DMTU) was recently found to inhibit the UT isoforms UT-A1 (expressed in kidney tubule epithelium) and UT-B (expressed in kidney vasa recta endothelium) with IC50 of 2-3 mM, and was shown to have diuretic action when administered to rats. Here, we measured UT-A1 and UT-B inhibition activity of 36 thiourea analogs, with the goal of identifying more potent and isoform-selective inhibitors, and establishing structure-activity relationships. The analog set systematically explored modifications of substituents on the thiourea including alkyl, heterocycles and phenyl rings, with different steric and electronic features. The analogs had a wide range of inhibition activities and selectivities. The most potent inhibitor, 3-nitrophenyl-thiourea, had an IC50 of ?0.2 mM for inhibition of both UT-A1 and UT-B. Some analogs such as 4-nitrophenyl-thiourea were relatively UT-A1 selective (IC50 1.3 vs. 10 mM), and others such as thioisonicotinamide were UT-B selective (IC50 >15 vs. 2.8 mM). äStructure-activity analysis of thiourea analogs as inhibitors of UT-A (epmc).pdf DeepDyve Pubget Overpricing