Antimicrobials

CCR-5 chemokine receptor antagonist; inhibits HIV entry via gp120 protein

Clotrimazole is an azole antifungal medication with action on fungal cell membrane disruption and is used for treating fungal infections like athlete's foot, ringworm, and vaginal yeast infections.

Daptomycin is a cyclic lipopeptide that disrupts cell membrane potential and causes leakage from the cell. The antibacterial effects are limited to gram-positive bacteria since daptomycin can’t reach the outer membrane of gram-negative species. It is often used for infections cause by vancomycin-resistant enterococci and staphylococci.

Selective and potent inhibitor of sialidases (neuraminidases) in influenza A and B viruses. The compound binds tightly to the viral neuraminidase active site in late stages of viral life-cycle. It inhibits shedding sialic acids from host cell surface glycans, which interact with viral hemagglutinin, and consequently prevents release of new viral particles from the host cell surface.

Impurity of Micafungin; anti-fungal

Darunavir is a HIV-1 protease inhibitor used orally in the treatment of patients with multi-drug resistant HIV-1 infection (Ghosh, 2007). It has also been shown to be effective against other infectious diseases such as hepatitis C virus and SARS coronavirus. Metabolized by cytochrome P450 3A (CYP3A) isoenzymes, darunavir is often administered together with ritonavir that prolongs its bioavaiability, giving a terminal elimination half-life (t1/2) of 15 hours (Back, 2008). The effect of darunavir on natural compounds such as matrix proteins and toll-like receptor activity has also been studied via high performance liquid chromatography (HPLC) experiments.

Inhibitor of protein synthesis; aminoglycoside

Antibiotic of fluoroquinolone class; DNA replication inhibitor

Posaconazole is an antifungal agent that inhibits the 14-alpha demethylase enzyme which is responsible for the synthesis of the fungal cell wall component, ergosterol. This demethylase enzyme synthesizes ergosterol through converting lanosterol to ergosterol. Therefore Posaconazole prevents the formation of fungal cell walls with the appropriate membrane permeability thus leading to fungal cell lysis. Posaconazole can be used as an antifungal drug to treat opportunistic fungal infections in immunocompromised individuals such as HIV patients. Moreover it is shown to inflict its inhibitory activity against common pathogenic fungus such as Candida and Aspergillus species but also Mucorales and some Fusarium species, which are less common.

Cefsulodin sodium salt is a beta lactam antibiotic in the third-generation cephalosporin family that inhibits penicillin-binding proteins (PBPs) to disrupt bacterial cell wall synthesis.

Filociclovir is a novel antiviral agent, which is synthesized from small-molecule pharmaceutical compounds. It functions primarily by inhibiting viral DNA polymerase, thereby halting viral replication within infected host cells. This mechanism of action is particularly effective against certain herpesviruses, as it targets the polymerase enzyme that is critical for viral DNA synthesis and proliferation.

Inhibitor of protein synthesis; steroid antibiotic

Dihydrostreptomycin sesquisulfate, EP is an aminoglycoside antibiotic, structurally derived from Streptomyces griseus. This compound originates from microbial biosynthesis, a method which harnesses the natural antibiotic-producing capabilities of microbial cultures. The mode of action of dihydrostreptomycin sesquisulfate involves binding to the 30S subunit of bacterial ribosomes, which interrupts the process of protein synthesis, ultimately leading to bacterial cell death.