Design of new imidazole derivatives with anti-HCMV activity: QSAR modeling,synthesis and biological testing

Journal of Computer-Aided Molecular Design - The problem of designing new antiviral drugs against Human Cytomegalovirus (HCMV) was addressed using the Online Chemical Modeling Environment (OCHEM)....     

Normals in a Minkowski Plane

In this paper we will establish bounds on the average number of normals through a point in a convex body in a Minkowski plane for certain classes of convex bodies. Also, a related Euler relation is discussed.     

Padé approximations to the logarithm II: Identities, recurrences, and symbolic computation

Combinatorial identities that were needed in [25] are proved, mostly with C. Schneider’s computer algebra package Sigma. The form of the Padé approximation of the logarithm of arbitrary order is stated as a conjecture. 2000 Mathematics Subject Classification Primary—41A21, 05A19, 33F10 Supported by NRF-grant 2047226. Supported by NRF-grant 2053748. Supported by the Austrian Academy of Sciences, by the John Knopfmacher Research Centre for Applicable Analysis and Number Theory, and by the SFB-grant F1305 and the grant P16613-N12 of the Austrian FWF. Supported by NRF-grant 2053756.     

The regular part of sectorial forms

We study the regular part of a densely defined sectorial form, first in the abstract setting and then under mild conditions for a differential sectorial form. The regular part of the latter turns out to be again a differential sectorial form. Moreover, we characterize when taking the real part of a differential sectorial form commutes with taking the regular part. An example shows that these two operations do not commute in general.     

Confocal microscopy of whole mount embryonic cartilage: Intracellular localization of F-actin, chick prolyl hydroxylase and type II collagen mRNA

We show that whole mount preparations of embryonic chick sterna can be analyzed with confocal laser scanning microscopy (CLSM). This technique replaces the traditional sectioning of cartilage or culturing of chondrocytes. Whole ‘chunks’ of cartilage can be stained with dyes, used for immunohistochemistry or in situ hybridization. Although other stains have been used, the stains presented include phalloidin and propidium iodide which stain filamentous actin (F-actin) and the DNA and RNA of cells, respectively. Collagen secreting endoplasmic reticulum (ER) was localized with a primary antibody to chick prolyl hydroxylase (CPH) that was detected with a secondary antibody conjugated to FITC. The intracellular localization of type II collagen mRNA was analyzed using in situ hybridization. The cDNA probe specific for the C-propeptide region of the 1 type (II) collagen mRNA was nick translated and labeled with biotin-16-dUTP. Biotin labeled probes were visualized with avidin-FITC. Depending on the intensity of the stain, we were able to analyze approximately 3–10 layers of chondrocytes. Stains penetrated into the cartilage better than antibodies and biotin-avidin labeled cDNA probes. The F-actin was located as bands of filaments in the superficial layers of the cartilage and was associated with the membranes that marked cell boundaries as deep as 10 layers of chondrocytes. The ER stained with anti-chick prolyl hydroxylase was prominent in perinuclear regions of the cells, but the antibody was only able to penetrate 4–5 cell layers. Single label in situ hybridization studies show that chondrocytes are positive for type II collagen mRNA. Similar to the immunohistochemistry, in situ hybridization probes were only able to penetrate 4–5 cell layers. The type II collagen mRNA appeared perinuclear in the chondrocytes, similar to the ER staining pattern.     

DEVELOPMENT OF A PLAQUE REDUCTION ASSAY AND APPLICATION TO THE STUDY OF PSORALEN-DAMAGED DNA

Abstract— We have developed a procedure called a plaque reduction assay to assess the biological activity of duplex circular DNA modified by covalent adduct formation with psoralen derivatives. The replicating form (RF) of bacteriophage DNA modified by photochemical addition of a psoralen derivative was introduced into bacterial cells using the CaCI₂ transfection method. The transfected cells. plated upon a confluent lawn of cells permissive for the bacteriophage in the inoculum, provided a measure of the reduction in infectivity of the RF DNA which resulted from its covalent modification. Use of this assay is illustrated in studies which screened and compared the activities of several recently synthesized psoralen derivatives. We describe two new compounds. β-(8-psoralenoxy)-ethanol and β-(8-psoralenoxy)ethylamine that are significantly more active than either 8-methoxypsoralen or trioxsalen in the biological assay