Antifungal agents: their diversity and increasing sophistication
نویسنده
چکیده
Since the 1950s, antifungal drug discovery has identified three classes of natural products (griseofulvin, polyenes and echinocandins) and four classes of synthetic chemicals (allylamines, azoles, flucytosine and phenylmorpholines) with clinical value against fungal infections. For life threatening fungal disease, the polyene amphotericin B is still a common choice despite toxic side-effects. The azoles remain the most widely used group of anti fungals active against a wide range of mycoses, benefiting from creative chemistry to boost their effectiveness. More recently, the echinocandins show great promise, with caspofungin licensed for clinical use in 2002 and two other molecules close to registration. New advances in molecular genetics afford the promise of revealing new antifungal targets, together with new agents to inhibit those targets specifically.
منابع مشابه
Antifungal agents: Polyene, azole, antimetabolite, other and future agents
Antifungals have always been considered as one of the astonishing discoveries of the 20th century. This is correct, but the real marvel is the development of antifungal resistance in hospitals, communities, and the environment concomitant with their use. Fungal infections have emerged as an important clinical threat, with significant associated morbidity and mortality. This study is desig...
متن کاملStudying Performance and Learning With ABIR The Effects of Knowledge, Mobilizing Agents, and Predictability
This study uses the Agent-Based Identity Repertoire model to investigate the ability of populations to adapt and learn in an unpredictable environment. The authors’ findings highlight the trade-off between adaptation and diversity in the pursuit of performance but also show that this trade-off is far from straightforward. Increasing sophistication improves the ability to adapt but reduces diver...
متن کاملSynthesis and Biological Evaluation of Novel Quinoline Derivatives as Antibacterial and Antifungal Agents
Vilsmeier Several diamide derivatives containing 2-chloroquinoline scaffolds were synthesized via Ugi reaction of 2-chloroquinoline-3-carboxaldehydes, amines, carboxylic acids and isocyanides. The diversity of these quinolinyl Ugi-adducts was increased by using 2-chloroquinoline-3-carboxylic acids as a source of acid. Among them, compounds 2d, 2n, 2p, 4a, 4c and<strong...
متن کاملMicrowave assisted synthesis, antifungal activity, DFT and SAR study of 1,2,4-triazolo[4,3-a]pyridine derivatives containing hydrazone moieties
BACKGROUND The increasing prevalence of multi-drug resistant fungal infections has encouraged the search for new antifungal agents. Hydrazone derivatives always exhibited diversity activities, including antifungal, anti-inflammatory, anti-oxidation, anti-cancer activity. Regarding the heterocyclic moiety, 1,2,4-triazolo[4,3-a]pyridine derivatives also display broad activities, such as antifunga...
متن کاملسنتز مشتقات جدید 2-متیل- 3-تریازولیل کرومانون اکسیم اتر به عنوان ترکیبات بالقوه ضد قارچ
Background and purpose: Despite growing list of antifungal agents, their clinical value has been limited by their relatively high risk of toxicity, the emergence of drug resistance, and insufficiencies in their antifungal activity. This situation has led to an ongoing search for potent broad spectrum antifungal agents with low side effects, which can be administered both orally and parenteral...
متن کامل