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Design, synthesis, and antibacterial evaluation of PFK-158 derivatives as potent agents against drug-resistant bacteria

期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021; 41 ()

Infections caused by antibiotic resistant bacteria are a major health concern throughout the world. It is well known that PFK-158 can enhance the anti......

Enantiomeric profiling of a chiral benzothiazole necroptosis inhibitor

期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021; 43 ()

Necroptosis is a form of programmed cell death that contributes to the pathophysiology of multiple diseases. Development of small-molecule anti-necrop......

Design and synthesis of novel diosgenin-triazole hybrids targeting inflammation as potential neuroprotective agents

期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021; 43 ()

Alzheimer's disease is a progressive neurodegenerative disease, and its incidence is expected to increase as the global population ages. Recent studie......

Penpolonin A-E, cytotoxic alpha-pyrone derivatives from Penicillium polonicum

期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021; 40 ()

Five new alpha -pyrone derivatives, named penpolonin A-E (1-5), together with two known compounds (6-7) were acquired from the endophytic fungus Penic......

Insecticidal activity of twin compounds from podophyllotoxin and cytisine

期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021; 43 ()

To explore natural-product-based insecticide candidates, and high value-added application of natural plants in agriculture, a series of twin compounds......

Synthesis, crystal structure, and biological evaluation of a novel eight-membered dinitration neonicotinoid analogues

期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021; 43 ()

In the studies on dihydroxy intermediate synthesis, a serendipitous reaction of introducing nitro group from nitromethylene has been observed. Instead......

Discovery and characterization of a novel glucose-6-phosphate dehydrogenase (G6PD) inhibitor via high-throughput screening

期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021; 40 ()

Altered glucose-6-phosphate dehydrogenase (G6PD) status is influential in many cellular pathophysiological processes and diseases, making G6PD a poten......

The optimization and characterization of functionalized sulfonamides derived from sulfaphenazole against Mycobacterium tuberculosis with reduced CYP 2C9 inhibition

期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021; 40 ()

In this study, a series of sulfonamide compounds was designed and synthesized through the systematic optimization of the antibacterial agent sulfaphen......

Discovery of novel reversible monoacylglycerol lipase inhibitors via docking-based virtual screening

期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021; 41 ()

Monoacylglycerol lipase (MAGL) is the major enzyme that catalyzes the hydrolysis of monoacylglycerols (MAGs). MAGL is responsible for degrading 2-arac......

Design and development of 1,3,5-triazine derivatives as protective agent against spinal cord injury in rat via inhibition of NF-KB

期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021; 41 ()

Spinal cord injury (SCI) is a chronic disease causing motor and sensory loss in the affected individuals. The SCI has a huge impact on the lives of pa......

Synergistic hepatoprotective effect of combined administration of Lachnum polysaccharide with silymarin

期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021; 46 ()

In recent years, combination therapy has gradually become one of the hot spots. As a new therapy strategy, we investigated the combination treatment o......

Design, synthesis and antiproliferative activity of novel 2,4-diamino-5--methyleneaminopyrimidine derivatives as potential anticancer agents

期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021; 47 ()

In order to discover new anticancer agents, 25 novel 2,4-diamino-5-methyleneaminopyrimidine derivatives were designed and synthesized based on our pre......

Design and synthesis of a series of OFF-ON near infrared fluorescent probes for nucleic acid in aqueous solution

期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021; 48 ()

Five cyanine dyes (6a-e) with aza units were prepared by the reaction of pyridinum or quinolinium with suitable aldehydes. They present several remark......

Small molecule approaches to treat autoimmune and inflammatory diseases (Part II): Nucleic acid sensing antagonists and inhibitors

期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021; 44 ()

Nucleic acid sensing pathways play an important role in the innate immune system, protecting hosts against infections. However, a large body of eviden......

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