New Renin Inhibitors Containing Pseudodipeptidic Units in P3-P2 and P1-P1' Positions
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Design and Synthesis of Novel Arylketo-containing P1-P3 Linked Macro-cyclic BACE-1 Inhibitors
A series of arylketo-containing P1-P3 linked macrocyclic BACE-1 inhibitors were designed, synthesized, and compared with compounds with a previously known and extensively studied corresponding P2 isophthalamide moiety with the aim to improve on permeability whilst retaining the enzyme- and cell-based activities. Several inhibitors displayed substantial increases in Caco-2 cell-based permeabilit...
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In recent years, parallel computers have changed techniques to solve problems in various kinds of fields. In parallel computers of distributed memory type, data can be shared by communication procedures called message-passing, whose speed is slower than that of computations in a processor. From a practical point of view, it is important to reduce the amount of message-passing. Domain-decomposit...
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G. D. HUNTER AND G. POPJAK I95I James, A. T. & Martin, A. J. P. (1951). Biochem. J. 48, vii. Kao, C. H. & Ma, S. (1931). J. chem. Soc. p. 2046. Kon, G. A. R., Linstead, R. P. & Maclennan, G. W. G. (1932). J. chem. Soc. p. 2454. Lane, J. F. & Wallis, E. S. (1941). J. Amer. chem. Soc. 63, 1674. Oldham, J. W. H. (1950). J. chem. Soc. p. 100. Organic Syntheses (1925). 4, 9. Ponzio, G. (1905). Gazz....
متن کاملChem. Pharm. Bull. 53(10) 1305—1309 (2005)
hypertension and heart failure, especially because of their high specificity for angiotensinogen. In the past a large number of peptidic renin inhibitors were designed and synthesized. Unfortunately, a majority of them showed poor oral absorption and rapid biliary uptake. The above limitations may result from the substrate-like structure of the synthesized inhibitors. Therefore, other structure...
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We consider the two-electron position and momentum dot products, α = r1·r2 and β = p1·p2, and present a method for extracting their distributions, A(α) and B(β), from molecular wave functions built on Gaussian basis functions. The characteristics of the Hartree-Fock AHF(α) and BHF(β) for He and the first-row atoms are investigated, with particular attention to the effects of Pauli exchange. The...
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ژورنال
عنوان ژورنال: Chemical and Pharmaceutical Bulletin
سال: 2005
ISSN: 0009-2363,1347-5223
DOI: 10.1248/cpb.53.1305