3gw5 › Citations

Design and optimization of renin inhibitors: Orally bioavailable alkyl amines.

Tice CM, Xu Z, Yuan J, Simpson RD, Cacatian ST, Flaherty PT, Zhao W, Guo J, Ishchenko A, Singh SB, Wu Z, Scott BB, Bukhtiyarov Y, Berbaum J, Mason J, Panemangalore R, Cappiello MG, Müller D, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA
Bioorg Med Chem Lett 19 3541-5 (2009)
Cited: 9 times
EuropePMC logo PMID: 19457666

Abstract

Structure-based drug design led to the identification of a novel class of potent, low MW alkylamine renin inhibitors. Oral administration of lead compound 21l, with MW of 508 and IC(50) of 0.47nM, caused a sustained reduction in mean arterial blood pressure in a double transgenic rat model of hypertension.

Articles - 3gw5 mentioned but not cited (1)

  1. Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility. Jia L, Simpson RD, Yuan J, Xu Z, Zhao W, Cacatian S, Tice CM, Guo J, Ishchenko A, Singh SB, Wu Z, McKeever BM, Bukhtiyarov Y, Johnson JA, Doe CP, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA. ACS Med Chem Lett 2 747-751 (2011)


Reviews citing this publication (3)

  1. A current evaluation of the safety of angiotensin receptor blockers and direct renin inhibitors. Siragy HM. Vasc Health Risk Manag 7 297-313 (2011)
  2. Recent progress on the discovery of non-peptidic direct renin inhibitors for the clinical management of hypertension. Yokokawa F. Expert Opin Drug Discov 8 673-690 (2013)
  3. The role of direct renin inhibition in clinical practice: focus on combination therapy. Rashid HU, Mende C. Am J Cardiovasc Drugs 11 303-315 (2011)

Articles citing this publication (5)

  1. Optimization of orally bioavailable alkyl amine renin inhibitors. Xu Z, Cacatian S, Yuan J, Simpson RD, Jia L, Zhao W, Tice CM, Flaherty PT, Guo J, Ishchenko A, Singh SB, Wu Z, McKeever BM, Scott BB, Bukhtiyarov Y, Berbaum J, Mason J, Panemangalore R, Cappiello MG, Bentley R, Doe CP, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA. Bioorg Med Chem Lett 20 694-699 (2010)
  2. Discovery of new renin inhibitory leads via sequential pharmacophore modeling, QSAR analysis, in silico screening and in vitro evaluation. Al-Nadaf AH, Taha MO. J Mol Graph Model 29 843-864 (2011)
  3. An integrated computational workflow for efficient and quantitative modeling of renin inhibitors. Subramanian G, Rao SN. Bioorg Med Chem 20 851-858 (2012)
  4. An electronic environment and contact direction sensitive scoring function for predicting affinities of protein-ligand complexes in Contour(®). Lindblom PR, Wu G, Liu Z, Jim KC, Baldwin JJ, Gregg RE, Claremon DA, Singh SB. J Mol Graph Model 53 118-127 (2014)
  5. Computational modeling and design of renin inhibitors. Subramanian G. Bioorg Med Chem Lett 23 460-465 (2013)


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