Publications

PAN-NUCLEOSIDE AND NONNUCLEOSIDE RESISTANT STRAINS AFTER SEQUENTIAL THERAPY WITH NRTIS AND NNRTI

CCDC 600017: Experimental Crystal Structure Determination

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.

On-line monitoring and process control in selective laser melting and laser cutting

No abstract is provided for this article.

Therapeutic potential of PMEA as an antiviral drug

Mechanism of inhibitory effect of glycyrrhizin on replication of human immunodeficiency virus (HIV)

Comparative inhibitory effects of suramin and other selected compounds on the infectivity and replication of human T‐cell lymphotropic virus (HTLV‐III)/lymphadenopathy‐associated virus (LAV)

Suramin and various other selected compounds were evaluated for their in vitro inhibitory effects on the infectivity and replication of human T-cell lymphotropic virus (HTLV/III)/lymphadenopathy-associated virus (LAV). As parameters for infectivity and replication, respectively, we followed the cytopathic effect of HTLV-III/LAV on ATH 8 cells, a T-cell clone with high susceptibility to HTLV-III/LAV, and the expression of HTLV-III/LAV p24 gag protein in H9 cells infected with HTLV-III/LAV. As the most effective inhibitors of HTLV-III/LAV the following substances emerged (in order of decreasing activity): Evans Blue approximately equal to suramin greater than phosphonoformic acid greater than Direct Yellow 50. Several purine nucleoside analogues including vidarabine, tubercidin, neplanocin A, dihydroxypropyladenine, pyrazofurin and ribavirin were not inhibitory to HTLV-III/LAV. In our test systems, involving a high multiplicity of infection, HPA-23, previously reported to be effective against LAV reverse transcriptase, showed no inhibitory effect on HTLV-III/LAV infectivity for ATH 8 cells and proved only weakly inhibitory to HTLV-III/LAV replication in H9 cells. Thus, among the anionic dyes that are structurally related to suramin, compounds were found which were as active as suramin itself, if not more so.

Nitroimidazoles. Part 4. Synthesis and anti‐HIV Activity of New 5‐Alkylsulfanyl and 5‐(4′‐Arylsulfonyl)piperazinyl‐4‐nitroimidazole Derivatives.

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.

Antiviral drug sensitivity in ocular herpes simplex virus infection.

Thirty-nine herpes simplex virus (HSV) isolates were assayed for their sensitivity to 10 different antiviral agents. Of these 39 HSV isolates 10 were cultured from recipient buttons obtained at penetrating keratoplasty in patients with inactive stromal scarring due to recurrent herpetic keratitis, 25 were cultured from patients with conjunctival and ulcerative ocular infections, and the remaining four were laboratory strains with known drug sensitivity patterns, thus providing controls for the experiment. All but one of the 35 clinical isolates of HSV were type 1 and all were sensitive to the 10 antiviral agents. A single type 2 isolate from a young man with recurrent conjunctivitis proved to be resistant to a number of the antiviral agents. Since many of the clinical isolates had been exposed to multiple and protracted antiviral drug treatment, it is suggested that antiviral drug resistance in type 1 HSV ocular infection is not a significant problem.

Flow cytometric method for the detection of gpI antigens of varicella zoster virus and evaluation of anti-VZV agents

Cytotoxic 1,3-diarylidene-2-tetralones and related compounds

The discovery of antiviral agents: Ten different compounds, ten different stories

This review article, while autobiographical to some extent, describes the discovery of ten (classes of) antiviral compounds that have made (or just did not make) it to the market for the therapy of viral infections, but each in its own way influenced the landscape of our dealing with virus infections: (i) valaciclovir, (ii) BVDU, (iii) DHPA, (iv) cidofovir, (v) adefovir, (vi) tenofovir, (vii) stavudine, (viii) HEPT, (ix) TIBO, and (x) AMD3100. Successful drug development, as is certainly true for antiviral drugs and exemplified for the acyclic nucleoside phosphonates cidofovir, adefovir and tenofovir, requires patience and perseverance, and a close continuous and dedicated interaction between Chemistry, Biology/Medicine and Industry.

Handbook of viral bioterrorism and biodefense

An overview on the use of a viral pathogen as a bioterrorism agent: why smallpox? (B. Mahy). Smallpox: a potential agent of bioterrorism (R.J. Whitley). Potential antiviral therapeutics for smallpox, monkeypox and other orthopoxvirus infections (R.O. Baker, M. Bray, J.W. Huggins). Smallpox: a potential agent of bioterrorism (R.J. Whitley). Therapy and short-term prophylaxis of poxvirus infections: historical background and perspectives (J. Neyts, E. de Clercq). In vitro activity of potential anti-poxvirus agents (E.R. Kern). A review of compounds exhibiting anti-orthopoxvirus activity in animal models (D.F. Smee, R.W. Sidwell). Defense against filoviruses as biological weapons (M. Bray). Molecular diagnostics of viral hemorrhagic fevers (including Lassa fever, Yellow fever and Crimean-Congo hemorrhagic fever) (C. Drosten, B.M. Kummerer et al.). Arenaviruses other than Lassa virus (R.N. Charrel, X. de Lamballerie). Viruses of the bunya- and togaviridae families: potential as bioterrorism agents and means of control (R.W. Sidwell, D.F. Smee). Nipah virus - a potential agent of bioterrorism? (Sai-Kit Lam). Hantavirus - a potential agent of bioterrorism? (J.P. Clement). Tick-borne encephalitis (T.S. Gritsun, V.A. Lashkevich, E.A. Gould). The potential use of influenza virus as an agent for bioterrorism (R.M. Krug).

Design and production of bone scaffolds with selective laser melting

No abstract is provided for this article.

Crystallographic Study of a Novel Subnanomolar Inhibitor Provides Insight on the Binding Interactions of Alkenyldiarylmethanes with Human Immunodeficiency Virus-1 Reverse Transcriptase

Two crystal structures have been solved for separate complexes of alkenyldiarylmethane (ADAM) nonnucleoside reverse transcriptase inhibitors (NNRTI) 3 and 4 with HIV-1 reverse transcriptase (RT). The structures reveal inhibitor binding is exclusively hydrophobic in nature and the shape of the inhibitor-bound NNRTI binding pocket is unique among other reported inhibitor-RT crystal structures. Primarily, ADAMs 3 and 4 protrude from a large gap in the back side of the binding pocket, placing portions of the inhibitors unusually close to the polymerase active site and allowing 3 to form a weak hydrogen bond with Lys223. The lack of additional stabilizing interactions, beyond the observed hydrophobic surface contacts, between 4 and RT is quite perplexing given the extreme potency of the compound (IC(50) </= 1 nM). ADAM 4 was designed to be hydrolytically stable in blood plasma, and an investigation of its hydrolysis in rat plasma demonstrated it has a significantly prolonged half-life in comparison to ADAM lead compounds 1 and 2.

Effect of (E)-5-(2-Bromovinyl)-2′-deoxyuridine on replication of Epstein-Barr Virus in human lymphoblastoid cell lines

Fuchsin acid selectively inhibits human immunodeficiency virus (HIV) replication invitro

What can be Expected from Non‐nucleoside Reverse Transcriptase Inhibitors (NNRTIs) in the Treatment of Human Immunodeficiency Virus Type 1 (HIV‐1) Infections?

Mutation of Gln125 to Asn Selectively Abolishes the Thymidylate Kinase Activity of Herpes Simplex Virus Type 1 Thymidine Kinase