Evaluation of new pregnane derivatives as 5alpha-reductase inhibitor

The objective of this study was to synthesize several new pregnane derivatives and evaluate them as antiandrogens. From the commercially available 16-dehydropregnenolone acetate (7), two new steroidal compounds were synthesized: 17alpha-hydroxy-17beta-methyl-16beta-phenyl-D-homoandrosta-1,4,6-triene-3,20-dione (18) and 17alpha-acetoxy-17beta-methyl-16beta-phenyl-D-homoandrosta-1,4,6-triene-3,20-dione (19). The 5alpha-reductase inhibitory effect of the new compounds 18 and 19 together with the previously synthesized intermediates 7, 8, 13, 16, and 17 was determined in three different models: gonadectomized hamster flank organs diameter size, incorporation of [1,2-(14)C]sodium acetate into lipids in flank organs and conversion of [3H]testosterone (T) to [3H]dihydrotestosterone (DHT) by Penicillium crustosum. The evaluation of these steroids was carried out with three different controls: one group was treated with vehicle, the second with T and the third group with T plus finasteride. The pharmacological results from this work demonstrated that T significantly increases the diameter of the pigmented spot on the flank organs (p<0.05) as well as the incorporation of labeled sodium acetate into lipids in gonadectomized hamster flank organs (from 0.125 to 0.255 nmol per gland). In this study we also observed that broth of Penicillium crustosum converted [3H]T to [3H]DHT in a manner comparable to that of the flank organs. All experiments indicated that finasteride as well as steroids 7, 8, 13, 16-19 reduced significantly the conversion of T to DHT in P. crustosum. These compounds also decrease the size of the pigmented spot in the flank organs as well as reducing the incorporation of radiolabeled sodium acetate into lipids; T and the control sample (treated with vehicle only) were used for comparison. Apparently the presence of the 4,6-diene-3,20-dione moiety and also the C-17 ester group produce a higher inhibitory effect on the parameters used. PPThe data from this study indicated also that the three models used for the pharmacological evaluation exhibited comparable results.     

Synthesis and characterization of stereoregular AABB‐type polymannaramides

The condensation of D ‐mannaro‐1,4:6,3‐dilactone ( 2 ) with even‐numbered alkylenediamines (C₂, C₆–C₁₂) in a methanol solution and in the presence of triethylamine afforded polymannaramides 3 – 7 , which were isolated directly as white solids with various hydrophobic–hydrophilic characters. Because all the stereocenters in 2 possessed an S configuration, the random polymerization led to optically active, stereoregular polyhydroxypolyamides. The polymers were characterized by elemental analysis and IR, ¹H NMR, and ¹³C NMR spectroscopy. Their number‐average molecular weights were estimated by ¹H NMR spectral integration analysis. Thermal and powder X‐ray diffraction studies revealed that compounds 3 – 7 were poorly crystalline. © 2001 John Wiley & Sons, Inc. J Polym Sci A: Polym Chem 39: 1024–1030, 2001     

Aza-substitution,benzo-annulation effects and catalytic activity of <Emphasis Type="Italic">β</Emphasis>-octaphenyl-substituted tetrapyrrolic macroheterocyclic cobalt complexes. I. heterogeneous catalysis

The influence of the size of conjugated π-system on catalytic activity of cobalt complex with β-octaphenylporphyrin and its tetraaza-, tetrabenzo and tetrabenzotetraaza derivatives was studied in present work. It is found that catalytic activity for oxidation of sulfur-containing compounds increases under extension of conjugated macrocycle system according to the following series CoP < CoBP ≤ CoPz < CoPPz ? CoPc.     

Complete hypersurfaces with constant scalar curvature in spheres

To a given immersion ${i:M^n\to \mathbb S^{n+1}}$ with constant scalar curvature R, we associate the supremum of the squared norm of the second fundamental form sup |A|². We prove the existence of a constant C _n (R) depending on R and n so that R ≥ 1 and sup |A|² = C _n (R) imply that the hypersurface is a H(r)-torus ${\mathbb S^1(\sqrt{1-r^2})\times\mathbb S^{n-1} (r)}$ . For R > (n ? 2)/n we use rotation hypersurfaces to show that for each value C > C _n (R) there is a complete hypersurface in ${\mathbb S^{n+1}}$ with constant scalar curvature R and sup |A|² = C, answering questions raised by Q. M. Cheng.     

First stability eigenvalue characterization of Clifford hypersurfaces

The stability operator of a compact oriented minimal hypersurface is given by , where is the norm of the second fundamental form. Let be the first eigenvalue of and define . In 1968 Simons proved that for any non-equatorial minimal hypersurface . In this paper we will show that only for Clifford hypersurfaces. For minimal surfaces in , let denote the area of and let denote the genus of . We will prove that . Moreover, if is embedded, then we will prove that . If in addition to the embeddeness condition we have that , then we will prove that .

     

Solving the Gleason problem on linearly convex domains

Let be a bounded, connected linearly convex set in with boundary. We show that the maximal ideal (both in ) and ) consisting of all functions vanishing at is generated by the coordinate functions . Received: 2 July 2001; in final form: 26 September 2001 / Published online: 28 February 2002     

Quotient normed cones

Given a normed cone (X, p) and a subconeY, we construct and study the quotient normed cone (X/Y,p) generated byY. In particular we characterize the bicompleteness of (X/Y, ‖·‖ ^p ,p) in terms of the bicompleteness of (X, p), and prove that the dual quotient cone ((X/Y)^*, || · ‖·‖^p,p) can be identified as a distinguished subcone of the dual cone (X ^*, || · ||_{p, u}). Furthermore, some parts of the theory are presented in the general setting of the spaceCL(X, Y) of all continuous linear mappings from a normed cone (X, p) to a normed cone (Y, q), extending several well-known results related to open continuous linear mappings between normed linear spaces.