Sulfamate-tethered aza-Wacker approach towards analogs of Bactobolin A [0.03%]
用于合成巴克波林A类似物的亚胺键固硫氨改性的aza-沃卡反应方法学研究
Someshwar Nagamalla,David K Johnson,Shyam Sathyamoorthi
Someshwar Nagamalla
Here, we describe an approach towards analogs of the potent antibiotic Bactobolin A. Sulfamate-tethered aza-Wacker cyclization reactions furnish key synthons, which we envision can be elaborated into analogs of Bactobolin A. Docking studies...
Development of convenient crystallization inhibition assays for structure-activity relationship studies in the discovery of crystallization inhibitors [0.03%]
结晶抑制剂发现中的构效关系研究的便捷结晶抑制分析法的发展
Jeffrey Yang,Haifa Albanyan,Yiling Wang et al.
Jeffrey Yang et al.
Kidney stone diseases are increasing globally in prevalence and recurrence rates, indicating an urgent medical need for developing new therapies that can prevent stone formation. One approach we have been working on is to develop small mole...
Successes in antiviral drug discovery: a tribute to Nick Meanwell [0.03%]
抗病毒药物发现的成功案例——致敬Nick Meanwell教授
David P Rotella
David P Rotella
Drug discovery is a difficult task, and is even more challenging when the target evolves during therapy. Antiviral drug therapy is an excellent example, exemplified by the evolution of therapeutic approaches for treatment of hepatitis C and...
Discovery of pyrrolo[2,1- f][1,2,4]triazine-based inhibitors of adaptor protein 2-associated kinase 1 for the treatment of pain [0.03%]
用于治疗疼痛的适应型蛋白2相关激酶1抑制剂类吡咯并[2,1- f][1,2,4]三嗪衍生物的研究发现
Carolyn D Dzierba,Bireshwar Dasgupta,George Karageorge et al.
Carolyn D Dzierba et al.
Adaptor protein 2-associated kinase 1 (AAK1) is a member of the Ark1/Prk1 family of serine/threonine kinases and plays a role in modulating receptor endocytosis. AAK1 was identified as a potential therapeutic target for the treatment of neu...
Nicholas A Meanwell
Nicholas A Meanwell
The pyridazine ring is endowed with unique physicochemical properties, characterized by weak basicity, a high dipole moment that subtends π-π stacking interactions and robust, dual hydrogen-bonding capacity that can be of importance in dr...
Amide- and bis-amide-linked highly potent and broadly active antifungal agents for the treatment of invasive fungal infections- towards the discovery of pre-clinical development candidate FC12406 [0.03%]
高效广谱抗真菌剂用于侵袭性真菌感染的治疗—迈向临床前开发候选物FC12406的研究
Simon D P Baugh,Anna Chaly,Damian G Weaver et al.
Simon D P Baugh et al.
Most fungal infections are common, localized to skin or mucosal surfaces and can be treated effectively with topical antifungal agents. However, while invasive fungal infections (IFIs) are uncommon, they are very difficult to control medica...
Recent insights into antibacterial potential of benzothiazole derivatives [0.03%]
苯并噻唑衍生物抗菌活性的最新研究进展
Priyanka Kashyap,Sangeeta Verma,Pankaj Gupta et al.
Priyanka Kashyap et al.
Antimicrobial resistance (AMR) is a worldwide concern among infectious diseases due to increased mortality, morbidity and treatment cost. According to WHO 2019 report, among the 32 antibiotics in the clinical trials, only six were classifie...
An update on the discovery and development of reversible covalent inhibitors [0.03%]
可逆共价抑制剂的发现和开发进展
Faridoon,Raymond Ng,Guiping Zhang et al.
Faridoon et al.
Small molecule drugs that covalently bind irreversibly to their target proteins have several advantages over conventional reversible inhibitors. They include increased duration of action, less-frequent drug dosing, reduced pharmacokinetic s...
Shikha Kaushik,Sarvesh Kumar Paliwal,Malliga R Iyer et al.
Shikha Kaushik et al.
Emerging and re-emerging illnesses will probably present a new hazard of infectious diseases and have fostered the urge to research new antiviral agents. Most of the antiviral agents are analogs of nucleosides and only a few are non-nucleos...
Design, synthesis, biochemical and in silico characterization of novel naphthalene-thiourea conjugates as potential and selective inhibitors of alkaline phosphatase [0.03%]
设计、合成、生化和计算机表征新型菲噻二唑共轭物作为碱性磷酸酶的潜在及选择性抑制剂
Aamer Saeed,Saba Ashraf,Mubashir Aziz et al.
Aamer Saeed et al.
Naphthalene ring is present in a number of FDA-approved, commercially available medications, including naphyrone, terbinafine, propranolol, naproxen, duloxetine, lasofoxetine, and bedaquiline. By reacting newly obtained 1-naphthoyl isothioc...