Antimicrobials

Broad-spectrum antibiotic; bacterial cell wall biogenesis inhibitor

Ceftriaxone is a broad-spectrum cephalosporin antibiotic that is used for the treatment of bacterial infections in different locations such as the skin, soft tissue and respiratory tract. This drug works by inhibiting mucopeptide synthesis in the bacterial cell wall. As a result, bacteria will produce defective cell walls leading to cell death.

Chlorpropham-4-hydroxy-o-sulfonic acid is a herbicide metabolite with action on plant growth regulation and is used for environmental and agricultural research.

Pirazinecarboxamide (Pyrazinamide) is an antitubercular agent with action on Mycobacterium tuberculosis by disrupting membrane energetics and is used for treating tuberculosis in combination with other drugs.

Posaconazole is a triazole antifungal agent that inhibits the 14-alpha demethylase enzyme. This drug prevents the formation of fungal cell walls thus leading to fungal cell lysis. Posaconazole is shown to inflict its inhibitory activity against common pathogenic fungus such as Candida and Aspergillus species in severely immunocompromised patients.

Streptomycin sulfate is an antibiotic that inhibits the growth of bacteria by binding to the ribosomal subunit and interfering with protein synthesis. It is used in culture media for the production of human antibodies as well as in drug therapy for methicillin-resistant staphylococcus. Streptomycin sulfate has a high specific activity and low sensitivity, but it also has a low solubility in water. The active form of streptomycin sulfate is streptomycin A, which is produced by the addition of a phenyl ring to neomycin sulfate. In plant roots, streptomycin sulfate inhibits cyanogenic glycosides from being hydrolyzed into hydrogen cyanide (HCN) and benzaldehyde.

Dasabuvir is a non-nucleoside NS5B polymerase inhibitor with action on hepatitis C virus RNA replication and is used for treating hepatitis C in combination therapies.

Tenofovir diphosphate triethylamine (mixture of diastereomers) is an antiviral compound, which is a synthetic chemical product derived from the parent compound, tenofovir. This formulation includes a mixture of diastereomers to enhance its solubility and bioavailability. The compound primarily functions as a nucleotide reverse transcriptase inhibitor (NRTI). It targets viral reverse transcriptase enzymes, inhibiting DNA synthesis and subsequent viral replication by causing premature chain termination.

Protein synthesis inhibitor; tetracycline class

Tilmicosin is a macrolide antibiotic with action on bacterial protein synthesis inhibition and is used for treating respiratory infections in cattle and sheep.

Cefuroxime is a second-generation cephalosporin antibiotic with action on bacterial cell wall synthesis and is used for treating respiratory tract infections, urinary tract infections, and Lyme disease.

Erythromycin thiocyanate is a macrolide antibiotic derivative with action on bacterial protein synthesis inhibition and is used for research and pharmaceutical applications.

Enrofloxacin is a rapidly bactericidal antibiotic, that inhibits bacterial growth by binding to the 50S ribosomal subunit and blocking protein synthesis, thereby preventing the bacteria from making new proteins. Enrofloxacin also has strong activity against gram-positive bacteria, including Clostridium perfringens which is an anaerobic bacterium that causes food-borne illness. This antibiotic is used for the treatment of acute bacterial infections in humans, such as, skin or soft tissue infections, urinary tract infections (UTIs) and septicemia (bloodstream infection). Enrofloxacin has shown excellent bioavailability with high serum protein binding capacity. Additionally, it has good efficacy against clinical isolates of Escherichia coli and Klebsiella pneumoniae. Enrofloxacin can be used effective in treatments for Pseudomonas aeruginosa and Enterobacter species.

Amphotericin B is a macrocycle antibiotic first isolated from Streptomyces nodosus. Its antifungal activity is exerted by interacting with the fungal membrane, mainly ergosterol, and inducing pore formation. The increase in membrane permeability causes loss of ions and cell death. The C-2’ hydroxyl residue of the mycosamine carbohydrate moiety in the structure seems to have a major role in binding to ergosterol. It is used in cell culture to prevent growth of microbial contaminants, such as yeast and fungi. It is recommended by the WHO and CDC as an antifungal component for VTM at a concentration of 250ug/ml.

Cefadroxil monohydrate is a hydrated form of cefadroxil with similar action and applications as cefadroxil.

Anthracycline antibiotic with potent anti-tumoral activity. The compound interferes with DNA replication and RNA transcription since it intercalates between the base pairs of nucleic acids. It also inhibits the topoisomerase II, proteasome and generates free radicals, which leads to cell death of treated cells. Moreover, daunorubicin triggers apoptosis trough the stimulation of ceramide synthesis. It has been used as chemotherapy agent for the treatment of myeloid leukaemia (AML) and acute lymphocytic leukaemia (ALL).