Brindoxime is an organic compound with antimalarial and anti-RNA-virus activity

Filibuvir (PF-868554), being developed by Pfizer, is an orally administered, non-nucleoside inhibitor of the HCV NS5B RNA-dependent RNA polymerase for the potential treatment of chronic hepatitis C (HCV) infection. Filibuvir is a potent and specific inhibitor of the virally encoded NS5B polymerase, and inhibited genotype 1 sub genomic HCV replication in the cell-based replicon system. In phase I and a IIa clinical trial in treatment-naïve patients infected with genotype 1 HCV, filibuvir monotherapy or in combination with pegylated IFNα2a/ribavirin (the standard of care [SoC] for HCV infection) for up to 4 weeks significantly reduced HCV RNA levels compared with placebo or SoC alone. However, company stopped development of the drug and the decision to halt development of the non-nucleoside polymerase inhibitor, which was in mid-stage testing, was not related to any safety issues.

Etisazole was studied as a veterinary fungicide, possessed skin sensitizing properties in man. Information about the current use of this compound is not available.

Dexelvucitabine is a cytidine analogue, which has been shown to be active in both naive and HIV-experienced individuals and has in vitro activity against a variety of NRTI-resistant strains. Dexelvucitabine belongs to a class of HIV drugs called nucleoside reverse transcriptaseinhibitors (NRTIs). In the Phase IIb study most side effects were generally mild and included headache, fatigue, and gastrointestinal disorders. However, some participants developed severe hyperlipasemia and pancreatitis. Drug development is discontinued due to 40% incidence of grade 4 hyperlipasemia including one case of pancreatitis.

N-(4-Chloro-3-((3-Methyl-2-Butenyl)Oxy)Phenyl)-2-Methyl-3-Furancarbothioamide (also known as UC-781) is a thiocarboxanilide non-nucleoside reverse transcriptase inhibitor patented by Uniroyal Chemical Company, Inc. for prevention of HIV transmission. UC-781 is a potent inhibitor of reverse transcriptase-dependent pyrophosphorolysis, and purportedly restores the chain-terminating activity of zidovudine (AZT) against AZT-resistant virus. In clinical trials single and 7-day topical rectal exposure of UC-781 was safe with no significant adverse events, no detected UC-781 plasma drug levels, no significant mucosal changes, and high participant acceptability. Ex vivo biopsy infections demonstrated marked suppression of HIV infectibility, identifying a potential early biomarker of efficacy.

Pirazmonam is a potent anti-gram-negative monobactam that is differentiated from aztreonam by its high intrinsic activity against Ps. aeruginosa and good activity against Pseudomonas species. Pirazmonam has generally poor activity against gram-positive aerobic bacteria and anaerobic bacteria. Pirazmonam is a Trojan Horse molecule containing a b-lactam antibiotic that has been developed based on bacterial iron uptake systems. It features high structural similarity to aztreonam attached to a 3-hydroxy-4-pyridinone iron chelating group. Pirazmonam exhibited strong affinity to penicillin-binding protein 3 (PBP3) of Escherichia coli and moderate to negligible affinity to the other E. coli PBPs.

Quinacillin is semisynthetic penicillase-resistant penicillin patented by Boots Pure Drug Co. Ltd. For the treatment of bacterial infection. Quinacillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall, eventually causing cell lysis. In clinical trials Staph. aureus was eradicated from all but two patients during treatment but recurred in 4 after withdrawal. The antibiotic was especially useful in the treatment of staphylococcal respiratory infections, as it has little effect on the normal bacterial flora of the chest.

Etamocycline is a broad-spectrum antibiotic. It was studied in the treatment of bronchopulmonary and gastrointestinal infectious diseases.

Dichloroxylenol is a bactericide, preservative and deodorant. It is often used in the preparation of antiseptic and deodorant lotions and bath preparations. Dichloroxylenol also showed slightly greater activity against S. aureus Oxoid 701/1 Lot 610254 than against Escherichia coli and Salmonella typhi, indicating a probable role for cell wall in the susceptibility of bacteria to dichloroxylenol. The efficacy of either povidone-iodine (Betadine) or dichloroxylenol (Septocid) intrauterine infusions on the treatment of endometritis and/or cervicitis in cows was examined. The recovery and conception rates obtained after Betadine treatment were better than those obtained after Septocid. Moreover, healthy cows and those inseminated before post-partum day 180, having no more than 4-7 previous services, responded well to either Betadine or Septocid treatment.

Aplaviroc (GW873140) is a small-molecule noncompetitive allosteric CCR5 antagonist or HIV entry inhibitor (EI) that binds specifically to human CCR5 and exhibits potent anti-HIV activity in vitro in the nanomolar or subnanomolar range. Aplaviroc has exhibited potent in vivo antiviral activity (1.66 log decrease in viral load at nadir) following 10 days of monotherapy. In vitro studies of antiviral activity demonstrate that aplaviroc is active against HIV isolates from a variety of clades as well as those resistant to current HIV therapies targeting RT, PR, and gp41. However, GlaxoSmithKline has decided to terminate Phase III trials of aplaviroc after encountering additional cases of liver damage in patients taking the drug.