ABSTRACT
Bacterial biofilm widely exists in all kinds of bacteria, and is related to about 80 percent of bacterial infections. It is one of the main reasons for bacterial tolerance and resistance to existing antibiotics. Therefore, there is unmet clinical need for new anti-biofilm drugs. At present, there are three kinds of anti-biofilm agents under research, including biofilm inhibitors, biofilm dispersal agents and biofilm eradication agents. Among them, the biofilm eradication agent is unique, which can not only kill bacteria in biofilm but also eliminate biofilm as a monotherapy. Based on modifications of natural products with antibacterial activity, a variety of compounds with biofilm eradicating activities have been obtained, such as, acyldepsipeptides, pyrrolomycins, halogenated phenazines and halogenated 8-hydroxyquinolines. In this review, we summarize several major biofilm eradication agents above according to their structures and mechanisms.
ABSTRACT
Thirteen benzopyran derivatives were synthesized and their activity stimulating the differentiation of preadipocytes into adipocytes were evaluated with 3T3-L1 cells. Compound 8 was also tested for its hypoglycemic activity on db diabetes mice model. Results indicated that compounds 3, 8 and 11 exhibited strong differentiation-stimulating activity on 3T3-L1 cells model, and compound 8 can reduce the blood-sugar level of db diabetes mice dramatically.
Subject(s)
Animals , Mice , 3T3-L1 Cells , Adipocytes , Benzopyrans , Chemistry , Pharmacology , Blood Glucose , Metabolism , Cell Differentiation , Diabetes Mellitus, Experimental , Blood , Hypoglycemic Agents , Chemistry , PharmacologyABSTRACT
To design and synthesis a series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates with more potent anti-HBV activity, adefovir dipivoxil was used as lead compound, according to the results of enhanced oral bioavailability and antiviral activities of nucleoside L-amino acid ester prodrugs. Eleven novel L-amino acid ester prodrugs of acyclic nucleoside phosphonates were designed and synthesized, their anti-HBV activities were evaluated in HepG2 2.2.15 cells. Eight compounds exhibited antiviral activity, and compound 11 showed the most potent anti-HBV activity and highest selective index in vitro (EC50 0.0952 micromol x L(-1), SI 69523). Moreover, by analyzing the primary structure and activity relationship of these compounds, it could be suggested that L-amino acid ester strategy has significant potential in the acyclic nucleoside phosphonates prodrug design.
Subject(s)
Humans , Amino Acids , Chemistry , Antiviral Agents , Pharmacology , Cell Line, Tumor , Hepatitis B virus , Liver Neoplasms , Pathology , Virology , Nucleosides , Pharmacology , Organophosphonates , Pharmacology , Prodrugs , PharmacologyABSTRACT
Ten novel compounds were designed and synthesized on the basis of compound 1, their insulin-sensitizing activities were evaluated in 3T3-L1 cells. Results showed that compound 10 exhibited strong differentiation-stimulating activity on 3T3-L1 cells model, which indicated that compound 10 may possess well insulin-sensitizing activity.
Subject(s)
Animals , Mice , 3T3-L1 Cells , Benzopyrans , Pharmacology , Drug Design , Hypoglycemic Agents , Pharmacology , Insulin , PharmacologyABSTRACT
<p><b>AIM</b>To design and synthesize compounds with insulin-sensitizing activity.</p><p><b>METHODS</b>Using association principle of drug design, ten title compounds were designed and synthesized on the basis of known compounds with insulin-sensitizing activity, and their insulin-sensitizing activity were evaluated on 3T3-L1 pre-adipocyte cells.</p><p><b>RESULTS</b>One of the synthesized compounds showed strong insulin-sensitizing activity in vitro.</p><p><b>CONCLUSION</b>This compound may possess good sugar-lowering activity, and will be chosen for further hypoglycemic evaluation in vivo.</p>