104236-76-2Relevant academic research and scientific papers
Inhibitory effects of 2'-hydroxychalcones on rat lens aldose reductase and rat platelet aggregation
Lim, Soon Sung,Jung, Sang Hoon,Ji, Jun,Shin, Kuk Hyun,Keum, Sam Rok
, p. 1786 - 1789 (2000)
Inhibitory effects of synthetic 2'-hydroxychalcone derivatives on rat lens aldose reductase (RLAR) and on platelet aggregation were investigated for the prevention or the treatment of chronic diabetic complications. 5'-chloro-4,2'-dihydroxychalcone (8) and 5'-chloro-3,2'-dihydroxychalcone (27) exhibited a potent inhibitory effect on rat platelet aggregation induced by ADP (IC50=0.10 and 0.06 mg/ml, respectively) and collagen (IC50=44 and 16 μg/ml, respectively) but showed relatively weak inhibitory activities on RLAR.
Design and synthesis of chalcone derivatives as potent tyrosinase inhibitors and their structural activity relationship
Akhtar, Muhammad Nadeem,Sakeh, Nurshafika M.,Zareen, Seema,Gul, Sana,Lo, Kong Mun,Ul-Haq, Zaheer,Shah, Syed Adnan Ali,Ahmad, Syahida
, p. 97 - 103 (2015)
Browning of fruits and vegetables is a serious issue in the food industry, as it damages the organoleptic properties of the final products. Overproduction of melanin causes aesthetic problems such as melisma, freckles and lentigo. In this study, a series of chalcones (1-10) have been synthesized and examined for their tryrosinase inhibitory activity. The results showed that flavokawain B (1), flavokawain A (2) and compound 3 were found to be potential tyrosinase inhibitors, indicating IC50 14.20-14.38 μM values. This demonstrates that 4-substituted phenolic compound especially at ring A exhibited significant tyrosinase inhibition. Additionally, molecular docking results showed a strong binding affinity for compounds 1-3 through chelation between copper metal and ligands. The detailed molecular docking and SARs studies correlate well with the tyrosinase inhibition studies in vitro. The structures of these compounds were elucidated by the 1D and 2D NMR spectroscopy, mass spectrometry and single X-ray crystallographic techniques. These findings could lead to design and discover of new tyrosinase inhibitors to control the melanine overproduction and overcome the economic loss of food industry.
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 of chromones and pyrazolines as antimicrobial & antifungal agents
Ghotekar,Mandhane,Joshi,Bhagat,Gill
experimental part, p. 341 - 344 (2012/01/02)
A series of chromones and pyrazolines have been synthesized and evaluated for their antimicrobial and antifungal activity against Gram+ve and Gram-ve microorganisms. 2-Hydroxy acetophenone on treatment with substituted aldehydes gave the corresponding cha
Synthesis of some biologically important fluorinated 3-chlorochromones and 1,5 - Benzothiazepines as antimicrobial and antifungal agents
Ghotekarab,Joshia,Mandhane,Bhagata,Gill
scheme or table, p. 1267 - 1270 (2010/12/25)
A series of synthetic 3-chlorochromones and 1,5-benzo-thiazepines have been synthesized and evaluated for their antimicrobial and antifungal activity against Gram +ve and Gram -ve microorganisms. In these series the chemical transformation of chalcones to
