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19-Nor-10-azasteroids, a New Class of Steroid 5α-Reductase Inhibitors. 2. X-ray Structure, Molecular Modeling, Conformational Analysis of 19-Nor-10-azasteroids and Comparison with 4-Azasteroids and 6-Azasteroids [PDF]
Journal of Medicinal Chemistry, 1997 19-Nor-10-azasteroids are a new class of 5 alpha-reductase inhibitors whose activity depends on the presence of the bridgehead N-10 atom conjugated with the 4-en-3-one moiety in the A ring. The X-ray structure of 19-nor-10-azasteroid 1 has been determined and it is compared with the X-ray structure of testosterone. A complete conformational analysis of
Antonio Guarna +2 more
exaly +9 more sources
Design and synthesis of novel Azasteroids and Pseudoazulenyl nitrones
, 2016 Steroids are one of the essential classes of bioactive compounds and are involved in many biological functions which include their role as signaling compounds, the alteration of membrane fluidity and the regulation of a variety of metabolic processes. In
Nagaraju Birudukota
semanticscholar +6 more sources
Synthetic approaches to 9-azasteroids [PDF]
, 1968 An account is given of total syntheses of azasteroids, syntheses of 4-piperidones, and also syntheses of 2-quinolizidones. \ud l,2,3,4,5,6-Hexahydro-3-oxo-4aH-benzo[c]quinolizine was prepared and methylation shown to occur in the 2-position which was of no further synthetic value.
Colin Moore
core +4 more sources
ChemInform, 2005 AbstractFor Abstract see ChemInform Abstract in Full Text.
H. Surya Prakash Rao, S. P. Senthilkumar
openaire +2 more sources
Linear Relationships between the Ligand Binding Energy and the Activation Energy of Time-dependent Inhibition of Steroid 5α-Reductase by Δ1-4-Azasteroids [PDF]
Journal of Biological Chemistry, 2001 The inhibition of steroid 5α-reductase (5AR) by Δ1-4-azasteroids is characterized by a two-step time-dependent kinetic mechanism where inhibitor combines with enzyme in a fast equilibrium, defined by the inhibition constant K i , to form an initial ...
Gaochao Tian, Curt D. Haffner
openalex +2 more sources
14-azasteroids via heterocycloaddition
Tetrahedron, 1978 Abstract Benzo[f]quinoline alcohol 1 has been converted into azasteroids 14 and 15 via a standard procedure and via application of the newly discovered 1.4 aryl radical rearrangement of α-halomethyl-N-arylsutfonylpiperidioes. An intramolecular accelerating effect of an OH group on LAH reductions of N-tosylamides is described.
R.P. Loven, W.N. Speckamp
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The syntheses of 9-azasteroids—I
Tetrahedron, 1965 Abstract 4-Oxobenzo [c] quinolizidines have been examined as possible precursors of 9-azasteroids. 4-Oxo- and 3-methyl-4-oxobenzo [c] quinolizinium salts have been prepared and reduced to 4-hydroxy-benzo [c] quinolizidines, but attempts at oxidation of these alcohols have failed.
G. Jones, J. Wood
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Synthetic routes to 9-azasteroids [PDF]
, 1975 Syntheses of azasteroids both from natural steroids and from precursors bearing a nitrogen atom are reviewed.\ud The present research was directed towards the preparation of suitable tricyclic compounds possessing the future A-,B- and D-rings of a 9-azasteroid system which were suitably substituted for the construction of ring C of the azasteroid ...
Easom, John MM
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