Recent Patents on Anti-Infective Drug Discovery - Volume 6, Issue 2, 2011

Resurgence of tuberculosis (TB) worldwide, coupled to increasing frequency of TB infections that are multi-drug (MDR TB) and extensive drug resistant (XDR TB), infections that are problematic to treat, extol high human and financial costs. At the present time there are no new drugs that are effective against these antibiotic resistant infections. Therefore, there is an urgent need for effective agents that are safe and within Read More

Drug resistance is a major hurdle in the global battle against tuberculosis (TB). In tackling this problem it is important to understand both how resistance emerges as well as the ways in which multi-drug and extensively drugresistant TB (M/XDR-TB) may be successfully treated. The biggest problem with treatment is the lack of effective drugs. Exciting developments have been made in this area over recent years with useful Read More

New and active infections of tuberculosis continue to increase globally. Although antibiotic susceptible infections can be readily cured with isoniazide and rifampicin, infections resistant to these two antibiotics, named Multi- Drug Resistant TB (MDR TB), are problematic for therapy, extol high costs in terms of human suffering and finances, and when these MDR infections progress to Extensive Drug Resistant TB (XDR TB) status, they Read More

New drugs are desperately needed to combat XDR-TB as effective treatment involves at least four drugs to which the patient is sensitive or has never received in the past. Most Indian patients have received almost all second line drugs and have amplified resistance to most of the available drugs. Thioridazine has proven anti tuberculous effects in vitro and in vivo mouse models and we used this drug as salvage therapy in 4 I Read More

Thioridazine is a phenothiazine drug which has previously been extensively used for its antipsychotic properties as it is associated with a low risk of extra-pyramidal side-effects. There is good evidence to suggest that, in common with other phenothiazine drugs, thioridazine has important anti-microbial activity and is a potential candidate for development as an anti-microbial drug against multi-resistant organisms, including dru Read More

Current evidence shows that thioridazine (THZ) is ready for global clinical evaluation, while some of its derivatives and other efflux pump inhibitors reach the end stage of preclinical evaluation. In this paper, a clinical trial plan is described that investigates the antituberculosis potency, the safety profile and the role of THZ and/or its derivatives in the treatment of TB in humans, both in patients infected with drug sensitive strains a Read More

The phenothiazines are neuroleptic drugs that have long been known to have antimycobacterial activity, in vitro. Of the various commercially available phenothiazines, thioridazine, chlorpromazine and trifluoperazine are most active against mycobacteria, in vitro. Their MICs for Mycobacterium tuberculosis are in the 8-16 μg/ml range and MICs for Mycobacterium avium in the 10-32 μg/ml range, depending on me Read More

The emergence of resistance in Tuberculosis has become a serious problem for the control of this disease. For that reason, new therapeutic strategies that can be implemented in the clinical setting are urgently needed. The design of new compounds active against mycobacteria must take into account that Tuberculosis is mainly an intracellular infection of the alveolar macrophage and therefore must maintain activity Read More

Mycobacteria are responsible for some of the oldest diseases known to man, usually associated with high morbility and mortality rates. An example is tuberculosis (TB), a major public health problem that accounts for eight million new cases each year. Furthermore, the increase of multidrug and extremely-drug resistance seriously threatens the success of the TB control programmes. Resistance to anti-mycobacterial drugs is ofte Read More

Use of the old antipsychotic phenothiazine thioridazine (THZ) for therapy of multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis (TB) infection is now being seriously considered. It is reported that THZ primarily acts on enzymes involved in fatty acid metabolism and membrane proteins, particularly efflux pumps, as well as oxidoreductases and proteins involved in aerobic respiration that overlap Read More

Approximately 1/3 of the world's population is infected with Mycobacterium tuberculosis. In the vast majority of cases this results in latent not active disease. Latent disease is defined as a positive reaction to tuberculin antigens but without any further clinical symptoms. Models have been developed to study latent tuberculosis with the two most prominent being the in vivo Murine model and the in vitro Wayne model. In bot Read More

Whereas exposure of combinations of a phenothiazine and bacterium to incoherent UV increases the activity of the phenothiazine, exposure of the phenothiazine alone does not yield an increase of its activity. Because the laser beam energy is greater than that produced by the incoherent UV sources, exposure of phenothiazines to specific lasers may yield molecules with altered activities over that of the unexposed parent. Chl Read More

Viral infections leading to carcinogenesis tops the risk factors list for the development of human cancer. The decades of research has provided ample scientific evidence that directly links 10-15% of the worldwide incidence of human cancers to the infections with seven human viruses. Moreover, the insights gained into the molecular pathogenetic and immune mechanisms of hepatitis B virus (HBV) and human papilloma Read More

Lantibiotics are an interesting group of antimicrobial peptides. There are a number of reviews that describe the potential application of lantibiotics for controlling foodborne illnesses and their potential to treat Gram positive infections caused by organisms like Staphylococcus aureus. In this review, commercial potential for the producing organism for promoting health and their potential for protein chemistry applications are Read More

The patents annotated in this section have been selected from various patent databases. These recent patents are relevant to the articles published in this journal issue, categorized by therapeutic areas/targets and therapeutic agents related to antiinfective drug discovery.