Synthesis of lupeol derivatives and their antileishmanial and antitrypanosomal activities

The natural product lupeol 1 was isolated from aerial parts of Vernonia scorpioides with satisfactory yield, which made it viable to be used as starting material in semisynthetic approach. Ten lupeol derivatives 2–11 were prepared by classical procedures. Including, five new esters derivatives 7–11, which were obtained by structural modifications in the isopropylidene fragment. All semisynthetic compounds and lupeol 1–11 were confirmed by ¹H NMR, ¹³C NMR and HRMS. Their antiprotozoal activity was evaluated in vitro against L. amazonensis and T. cruzi. Derivative 6 showed the best antitrypanosomal activity (IC₅₀ = 12.48 μg/mL) and the lowest cytotoxic derivative (CC₅₀ = 161.50 μg/mL). The mechanism of action of the most active derivatives (4, 6 and 11) is not dependent from the enzyme trypanothione reductase.     

Sui principi variazionali nella meccanica dei continui classici

In this paper, along with the well established lines of the analytical mechanics, we aim to show an autonomous formulation of the fundamental principle of Lagrange-d'Alembert and of the subsequent Hamilton principle in classical mechanics of deformable continua in the sense that the afore—mentioned principles do not turn out to be a reformulation of the well known undefined equations of motion.     

cos πρ theorems for δ-subharmonic functions

For ϕ a δ-subharmonic function, sharp results are obtained that connectA(r, ϕ), B(r, ϕ) andT(r, ϕ), whereA(r, ϕ)=inf_|z|=r ϕ(z),B(r, ϕ)=sup_|z|=r ϕ(z), andT(r, ϕ) is the Nevanlinna characteristics.     

Palladium-catalyzed pseudo-domino cyclizations: An easy entry toward polycondensed pyrrolidone derivatives

A new type I palladium-catalyzed pseudo-domino process is developed, in which a single Pd-based catalytic system promotes two mechanistically unrelated, sequential catalytic cycles in chronologically distinct order. Suitable precursors undergo an allylic alkylation and a Heck coupling in sequence, affording polycondensed pyrrolidone derivatives. Depending on the starting precursors, intra/inter or doubly intramolecular processes can be obtained. The allylic alkylation process takes place always very smoothly. On the other hand, the Heck coupling turns out to be rather difficult either when the process is intermolecular, or when an intramolecular process generates polycondensed structures featuring three fused bonds connected to a common carbon atom. In such difficult cases, use of the Herrmann-Beller phosphapalladacycle allowed to catalyze the coupling. This study demonstrates also that allylic alkylations can be catalyzed by the Herrmann-Beller phosphapalladacycle.     

Necessary conditions and non-existence results for autonomous nonconvex variational problems

Classical one-dimensional, autonomous Lagrange problems are considered. In absence of any smoothness, convexity or coercivity condition on the energy density, we prove a DuBois-Reymond type necessary condition, expressed as a differential inclusion involving the subdifferential of convex analysis. As a consequence, a non-existence result is obtained.     

Approche non paramétrique du filtrage de système non linéaire à temps discret et à paramètres inconnus

Particle filters are presently among the most powerful tools for filtering discrete time non linear systems. However the presence of unknown parameters in the system equations makes their use more complex and can even impair their convergence properties. This Note shows how an on-line consistent estimation of these parameters can be obtained simultaneously to that of the state variables to be filtered. This approach relies upon a kernel-based non parametric estimation of conditional probability densities from successive Monte Carlo generations of system particles. To cite this article: V. Rossi, J.-P. Vila, C. R. Acad. Sci. Paris, Ser. I 340 (2005).     

Groups in which every non-abelian subgroup is permutable

A subgroupH of a groupG is said to bepermutable ifHX=XH for every subgroupX ofG. In this paper the structure of groups in which every subgroup either is abelian or permutable is investigated. This work was done while the last author was visiting the University of Napoli Federico II. He thanks the “Dipartimento di Matematica e Applicazioni” for its financial support.     

Novel intramolecular cyclization of N-alkynyl heterocycles containing proximate nucleophiles

Intramolecular cyclization of 2-acyl-1-propargyl-1H-indoles in the presence of ammonia provides an easy entry to pyrazino[1,2-a]indole nucleus.     

Crossing of shears bands in196Pb

High-spin states in¹⁹⁶Pb have been populated using the reaction¹⁷⁰Er(³⁰Si,4n). The previously observed shears bands in this nucleus have been extended and some of their transitions have been reordered. They now form regular bands with band crossings. One of the bands splits into two pathways at high spin.