27 research outputs found
Giant cell arteritis presenting with bilateral orbital inflammatory disease and enhancing superficial temporal arteries
Morphine and HIV-1 gp120 cooperatively promote pathogenesis in the spinal pain neural circuit
Pharmacologic and non-pharmacologic treatments for chronic pain in individuals with HIV: a systematic review
Evaluation of the interaction of levothyroxine with bovine serum albumin using spectroscopic and molecular docking studies
Retrospective Assessment of Transcription-Mediated Amplification-Based Screening for Trichomonas vaginalis in Male Sexually Transmitted Infection Clinic Patients
Expanded therapeutic potential in activity space of next-generation 5-nitroimidazole antimicrobials with broad structural diversity
Metronidazole and other 5-nitroimidazoles (5-NI) are among the most effective antimicrobials available against many important anaerobic pathogens, but evolving resistance is threatening their long-term clinical utility. The common 5-NIs were developed decades ago, yet little 5-NI drug development has since taken place, leaving the true potential of this important drug class unexplored. Here we report on a unique approach to the modular synthesis of diversified 5-NIs for broad exploration of their antimicrobial potential. Many of the more than 650 synthesized compounds, carrying structurally diverse functional groups, have vastly improved activity against a range of microbes, including the pathogenic protozoa Giardia lamblia and Trichomonas vaginalis, and the bacterial pathogens Helicobacter pylori, Clostridium difficile, and Bacteroides fragilis. Furthermore, they can overcome different forms of drug resistance, and are active and nontoxic in animal infection models. These findings provide impetus to the development of structurally diverse, next-generation 5-NI drugs as agents in the antimicrobial armamentarium, thus ensuring their future viability as primary therapeutic agents against many clinically important infections