4406-05-7Relevant academic research and scientific papers
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
Studies on ruthenium(III) chalconate complexes containing PPh 3/AsPh3
Muthukumar,Viswanathamurthi,Karvembu
experimental part, p. 2201 - 2211 (2011/01/12)
The reactions of [RuX3(EPh3)3] (X = Cl or Br; E = P or As) with 2′-hydroxychalcones in benzene under reflux led to the formation of [RuX2(EPh3)2(L)] (X = Cl or Br; E = P or As; L = chalcona
Synthesis and biological evaluation of flavan-3-ol derivatives as positive modulators of GABAA receptors
Mewett, Kenneth N.,Fernandez, Sebastian P.,Pasricha, Anmol K.,Pong, Alice,Devenish, Steven O.,Hibbs, David E.,Chebib, Mary,Johnston, Graham A.R.,Hanrahan, Jane R.
experimental part, p. 7156 - 7173 (2010/03/04)
We herein describe the synthesis and positive modulatory activities of a small library of flavan-3-ol derivatives on α1β2γ2L GABAA receptors. Structure-activity relationships of various substituents on the A, B
A Convenient Synthesis of 4-Styrylcoumarins
Joshi, U. K.,Kelkar, R. M.,Paradkar, M. V.
, p. 1151 - 1152 (2007/10/02)
The title-compounds (IIa-m) have been prepared by condensing 2'-hydroxychalcones (Ia-m) with the easily accessible Wittig reagent Ph3P=CHCOOEt.
