Special Issue "Anti-Infective Agents"

Guest Editor
Prof. Dr. Paul Cos
Laboratory of Microbiology, Parasitology and Hygiene (LMPH) Department of Pharmaceutical Sciences Faculty of Pharmaceutical, Biomedical and Veterinary Sciences Antwerp University, campus groenenborger, building V, office 5.23 Groenenborgerlaan 171, B-2020 Antwerp, Belgium
Website: www.ua.ac.be/paul.cos
E-Mail:
Interests: anti-infective agents; biofilm; bacterial virulence; oxidative stress; antibacterial; antifungal; antiparasitic and antiviral

Guest Editor
Prof. Dr. Mark Hamann
Department of Pharmacognosy and The National Center for the Development of Natural Products, University of Mississippi, USA
Website: http://www.pharmacy.olemiss.edu/pharmacognosy/Hamann/Hamannres.html
E-Mail:
Interests: natural products; antiinfectives; anticancer agents; NMR spectroscopy; marine ecology; synthesis of natural products; biosynthesis

Dear Colleagues,

Despite the tremendous progress in human medicine, infectious diseases represent one of the greatest challenges to mankind in the 21st century. According to WHO, infectious diseases account for nearly a third of global deaths. AIDS, malaria, tuberculosis and respiratory infections were among the top eight leading causes of death in 2004. The burden of infectious diseases falls particularly on the less developed countries due to the relative unavailability of medicines and the emergence of widespread drug resistance. In developing countries, a high infectious disease burden commonly co-exists with rapid emergence and spread of microbial resistance. The growing threat of emerging diseases such as SARS and influenza A (H1N1) has served as a wake-up call to public health services, pharmaceutical industry and academia.
Because the evolution of drug resistance is likely to compromise every drug in time, research on new anti-infective agents must be continued and all possible strategies should be explored. Besides small molecules from medicinal chemistry, natural products are still major sources of innovative therapeutic agents for various conditions, including infectious diseases.
This special issue welcomes research articles and comprehensive reviews addressing the discovery and/or development of anti-infective agents.

Prof. Dr. Paul Cos
Guest Editor

Prof. Dr. Mark Hamann
Guest Editor

Related Special Issues in other Journals

Anti-Infective Agents in Pharmaceuticals

Submission

• anti-infectives
• biofilm
• bacterial virulence
• oxidative stress
• antibacterial
• antifungal
• antiparasitic
• antiviral
• screening
• small molecules
• natural products

Manuscript ID: Molecules-antiinfect-20091023-Kim-kr
Type of Paper: Review
Title: Discovery and Development of Anti-HBV Agents and Their Resistance
Author: Kyun-Hwan Kim; E-Mail: khkim10@kku.ac.kr
Abstract: Infection of hepatitis B virus (HBV) is a prime cause of liver diseases such as hepatitis, cirrhosis and hepatocellular carcinoma. The recent drugs available for clinics are nucleot(s)ide analogues inhibiting the activity of viral reverse transcriptase. All drugs are reported to have viral resistance with breakthrough. Recent advances in in silico virtual screening methods and chemical libraries, together with a better understanding of the resistance mechanisms of existing drugs, have accelerated and made easier to discover and develop the novel HBV drugs. This review will summarize the current status and viral resistance of HBV drugs, approaches for the development of novel drugs, as well as new viral and host targets for future drugs.

Manuscript ID: Molecules-antiinfect-20091107-Desmaële-fr
Type of Paper: Review
Title: Chemistry and Structure-Activity Relationships of the Styrylquinoline-Type HIV Integrase Inhibitors
Authors: Didier Desmaële ¹ and Jean-François Mouscadet ²
Affiliations: ¹ Université Paris-Sud, Faculté de Pharmacie, UMR CNRS 8076 Biocis, Châtenay-Malabry, France; E-Mail: didier.desmaele@u-psud.fr
² LBPA, CNRS, Ecole Normale Supérieure de Cachan, France
Abstract: Despite significant progresses in anti-HIV-1 therapy, the current antiviral chemotherapy still suffers from deleterious side effects and emerging drug resistance. Therefore, the development of novel antiviral drugs remains crucial for the fight against AIDS. The HIV-1 integrase is a key enzyme in the replication cycle of the retrovirus since it catalyzes the integration of the reverse transcribed viral DNA into the chromosomal DNA. Efforts to develop anti-integrase drugs started during the early nineties to culminate with the recent approval of Raltegravir. The discovery and the development of the styrylquinoline inhibitor class was an important step in overall the process. In this review we will describe the key synthetic issues and the structure-activity relationships of this family of integrase inhibitors.

Type of Paper: Article
Title: Antifungal Effects of Pinoresinol Isolated from Sambucus Williamsii Hance
Authors: Bomi Hwang ¹, Eun-Rhan Woo ² and Dong Gun Lee ¹
Affiliations: ¹ School of Life Sciences and Biotechnology, College of Natural Sciences, Kyungpook National University, Daegu 702-701, Korea; E-Mail: juneyounglee@knu.ac.kr
² College of Pharmacy, Chosun University, Gwangju 501-759, Korea
Abstract: We investigated antifungal activity and its mechanism of pinoresinol, a biphenolic compound, which was isolated from the herbal Sambucus williamsii Hance. First of all, pinoresinol contained potent antifungal activities without hemolysis on human erythrocytes. To understand the antifungal mechanism(s), we conducted experiments with Candida albicans, a fungal pathogen. Fluorescence analysis using 1,6-diphenyl-1,3,5-hexatriene (DPH) and glucose and trehalose-release testing indicated that pinoresinol disrupted fungal plasma membrane. These results were confirmed by using rhodamine-labeled giant unilamellar vesicle (GUV). In conclusion, pinoresinol possesses antifungal effects by membrane-disruptive mechanism(s) and potential as therapeutic agents for treatment of fungal infectious diseases in human.
Keywords: pinoresinol; antifungal activity; membrane-active mechanism; Sambucus williamsii hance