Infectious diseases are one of the most important and urgent health problems in the world. According to the World Health Organization (WHO) statistics, infectious and parasitic diseases are a cause of about 16% of all deaths worldwide and over 40% of deaths in Africa. A considerable progress that has been made during last hundred years in the fight against infectious diseases, in particular bacterial infections, can be attributed mainly to three factors: (1) the general improvement of living conditions, in particular sanitation; (2) development of vaccines and (3) development of efficient antibacterial drugs. Although considerable progress in reduction of the number of cases of bacterial infections, especially in lethal cases, has been made, continued cases and outbreaks of these diseases persist, which is caused by different contributing factors. Indeed, during last sixty years antibacterial drugs were used against various infectious diseases caused by bacterial pathogens with an undoubtable success. The most fruitful period for antibiotic development lasted from 40's to 60's of the last century and resulted in the majority of antibiotics currently on the market, which were obtained by screening actinomycetes derived from soil. Although the market for antibacterial drugs is nowadays greater than 25 billion US dollars per year, novel antibacterial drugs are still demanded due to developed resistance of many pathogenic bacteria against current antibiotics. In the last five years, one can observe a dramatic increase in cases of resistant bacteria strains (e.g. Klebsiella pneumoniae and E. coli) which are responsible for difficult to treat pneumonia and infections of urinary tract. The development of resistant bacteria strains is a side effect of antibiotic application for treatment: the infections become untreatable as a result of the existence of antibiotic-tolerant persisters. In this review, we discuss the challenges in antibacterial drug discovery, including the molecular basis of drug resistance, drug targets for novel antibacterial drugs, and new compounds (since year 2010) from different chemical classes with antibacterial activity, focusing on structure-activity relationships.

The ongoing control of virulent bacteria strains is a challenge for today’s medicine. An example of this, is one widely used drug employed in treating less serious external oral and ocular bacterial infections. This is a gel containing both cetalkonium chloride and choline salicylate. However, whether in the era of expanding bacterial resistance this gel is still effective, is not clear. Hence, in our work, its antibacterial effect was studied against 13 strains of Pseudomonas aeruginosa, 6 strains of Staphylococcus spp. and 6 strains of Streptococcus spp. drawn from the collection of the Department of Microbiology, Virology and Immunology, Kazakh National Medical University, as well as against 30 strains of Staphylococcus spp. recently isolated from Kazakh medical students. This work demonstrated that Pseudomonas aeruginosa was insensitive to this preparation in all samples, while the sensitivity of Staphylococcus spp. and Streptococcus spp. was almost halved, compared to untreated samples. An interesting discovery was the greater resistance of strains obtained from student volunteers than from the collection. However, despite the evident resistance of some strains to the combined cetalkonium chloride and choline salicylate gel, we put forward that it can still be used in less serious external bacterial infections.

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The influence of excipients on the disintegration times of tablets and the release of papaverine hydrochloride (PAP) from tablets were studied. Ten different formulations of tablets with PAP were prepared by direct powder compression. Different binders, disintegrants, fillers, and lubricants were used as excipients. The release of PAP was carried out in the paddle apparatus using 0.1 N HCl as a dissolution medium. The results of the disintegration times of tablets showed that six formulations can be classified as fast dissolving tablets (FDT). FDT formulations contained Avicel PH 101, Avicel PH 102, mannitol, (3-lactose, PVP K 10, gelatinized starch (CPharmGel), Prosolv Easy Tab, Prosolv SMCC 90, magnesium stearate, and the addition of disintegrants such as AcDiSol and Kollidon CL. Drug release kinetics were estimated by the zero- and first-order, Higuchi release rate, and Korsmeyer-Peppas models. Two formulations of the tablets containing PVP (K10) (10%), CPharmGel (10% and 25%), and Prosolv Easy Tab (44% and 60%) without the addition of a disintegrant were well-fitted to the kinetics models such as the Higuchi and zero-order, which are suitable for controlled- or sustained-release.

Pain is a symptom of many diseases and significantly affects the quality of life, so researchers are constantly seeking new substances to be used as analgesics. Other, easier way is to combine already known drugs which cause synergistic effects greater than additive, so that probability of drug-specific side effects can be reduced. Researchers showed that caffeine can be an effective analgesic adjuvant enhancing antinociceptive effect of ibuprofen in animals and humans. By using modern drug technology methods tablets containing well-soluble ibuprofen salt and caffeine can be easily prepared. Thanks to that combination, the therapeutic dose of ibuprofen can be lowered and the side effects may be reduced.