104236-80-8Relevant articles and documents
Flavonoid glycosides with a triazole moiety for marine antifouling applications: Synthesis and biological activity evaluation
Pereira, Daniela,Gon?alves, Catarina,Martins, Beatriz T.,Palmeira, Andreia,Vasconcelos, Vitor,Pinto, Madalena,Almeida, Joana R.,Correia-Da-silva, Marta,Cidade, Honorina
, (2021/07/28)
Over the last decades, antifouling coatings containing biocidal compounds as active ingre-dients were used to prevent biofouling, and eco-friendly alternatives are needed. Previous research from our group showed that polymethoxylated chalcones and glycosy
Potentiation of Δf508- and G551D-CFTR-mediated Cl- current by novel hydroxypyrazolines
Park, Jinhong,Khloya, Poonam,Seo, Yohan,Kumar, Satish,Lee, Ho K.,Jeon, Dong-Kyu,Jo, Sungwoo,Sharma, Pawan K.,Namkung, Wan
, (2016/03/08)
The most common mutation of CFTR, affecting approximately 90% of CF patients, is a deletion of phenylalanine at position 508 (F508del, ΔF508). Misfolding of ΔF508-CFTR impairs both its trafficking to the plasma membrane and its chloride channel activity. To identify small molecules that can restore channel activity of ΔF508-CFTR, we synthesized and evaluated eighteen novel hydroxypyrazoline analogues as CFTR potentiators. To elucidate potentiation activities of hydroxypyrazolines for ΔF508-CFTR, CFTR activity was measured using a halide-sensitive YFP assay, Ussing chamber assay and patch-clamp technique. Compounds 7p, 7q and 7r exhibited excellent potentiation with EC50 value 50 values of 0.88 ± 0.11 and 4.45 ± 0.31 μM for wild-type and ΔF508-CFTR, respectively. In addition, CP7q significantly potentiated chloride conductance of G551DCFTR, a CFTR gating mutant; its maximal potentiation activity was 1.9 fold higher than the well-known CFTR potentiator genistein. Combination treatment with CP7q and VX-809, a corrector of ΔF508-CFTR, significantly enhanced functional rescue of ΔF508-CFTR compared with VX-809 alone. CP7q did not alter the cytosolic cAMP level and showed no cytotoxicity at the concentration showing maximum efficacy. The hydroxypyrazolines may be potential development candidates for drug therapy of cystic fibrosis.
Synthesis, docking studies and antioxidant activity of some chalcone and aurone derivatives
Narsinghani, Tamanna,Sharma, Mukesh C.,Bhargav, Sakshi
, p. 4059 - 4068 (2013/09/02)
Chalcones and aurones are found to possess high antioxidant activity. They are known to inhibit tyrosinase enzyme involved in synthesis of melanin. A series of substituted chalcones and aurones have been synthesized and tested for their antioxidant activi