25870-72-8Relevant academic research and scientific papers
Design, synthesis and bioactivity of chalcones and its analogues
Niu, Chao,Tuerxuntayi, Adila,Li, Gen,Kabas, Madina,Dong, Chang-Zhi,Aisa, Haji Akber
supporting information, p. 1533 - 1538 (2017/07/17)
The Vernohia anthelmintica L.'s extract is one of the most popular Uygur medicines used for vitiligo. It is believed that the chalcone compounds of the plant play an important role in the treatment since they may activate tyrosinase and improve melanin production. In this study, twenty-one chalcones and nine analogues were synthesized in view of three different components of chalcone (A, B ring and α, β-unsaturated carbonyl). After biological evaluation of their activity on tyrosinase in cell-free systems, the result showed that most compounds (except polyhydroxy chalcones) possess activator effect on the tyrosinase, especially for 13a–15a, 20a and 1b, which bearing a comparable activity to the positive control 8-MOP. SAR of these tyrosinase activator was summed up for the first time as well. Finally, compound 13a was found to increase melanin contents and tyrosinase activity 1.75 and 1.3 fold, respectively, compared with that of untreated murine B16 cells at the concentration of 40?μg/mL.
Synthesis of amino chalcones in presence of ionic liquid as soluble support
Pan, Xianhua,Yi, Fengping,Zhang, Xuan,Chen, Shihong
experimental part, p. 3809 - 3813 (2012/09/07)
A microwave-assisted liquid phase synthesis of aminochalcones was developed by using aldehyde-functionalized ionic liquid as soluble support. Ionic liquid bound aminoacetophenone was treated with aromatic aldehyde to give supported chalcone derivatives. After cleavage, the target compounds were obtained in 83-92 % yields and ≥ 95 % purities without column chromatographic purification. The recovered aldehyde-functionalized ionic liquid could be reused for several times without affecting its activity and the yields of desired compounds were between 86-89 %. These results indicated that the presented method could be applied efficiently to the liquid phase combinatorial chemistry based on aldol condensation.
A study of anti-inflammatory and analgesic activity of new 2,4,6-trisubstituted pyrimidines
Yejella, Rajendra Prasad,Atla, Srinivasa Rao
scheme or table, p. 1079 - 1082 (2011/10/05)
Chalcone derivatives (3a - m) were prepared by condensing 4-aminoacetophenone with various substituted aromatic and hetero aromatic aldehydes according to Claisen-Schmidt condensation. These chalcones, on reaction with guanidine hydrochloride under basic alcoholic conditions gave 2,4,6-trisubstituted pyrimidines (5a - m) in quantitative yields. All the newly synthesized pyrimidines were characterized by means of IR, 1H- and 13CNMR, Electron Ionization (EI)-mass and elemental analyses and screened for anti-inflammatory and analgesic activities by in vivo. 2-Amino-4-(4-aminophenyl)-6-(2,4-dichlorophenyl)pyrimidine (5b) and 2-amino-4-(4-aminophenyl)- 6-(3-bromophenyl) pyrimidine (5d) were found to be the most potent anti-inflammatory and analgesic activity compared with ibuprofen, reference standard. And also it was found that compound 5b identified as lead structure among all in both the activities. Pyrimidines which showed good anti-inflammatory activity also displayed better analgesic activity.
Synthesis and antimicrobial activity of some new 2,4,6-trisubstituted pyrimidines
Prasad, Y. Rajendra,Rao, B. Bhaskar,Agarwal,Rao, A. Srinivasa
scheme or table, p. 641 - 644 (2011/12/15)
Chalcone derivatives [3(a-m)] were prepared by condensing 4-aminoacetophenone with various substituted aromatic and hetero aromatic aldehydes in dilute ethanolic potassium hydroxide solution at room temperature according to Claisen-Schmidt condensation. These chalcones react with guanidine hydrochloride in a basic alcoholic media to give 2,4,6-trisubstituted pyrimidines [5(a-m)]. All these pyrimidines were characterized by means of their IR, 1H NMR and elemental analyses and screened for their antimicrobial activity. Some of these compounds showed significant antimicrobial activity.
Synthesis and analgesic activity of some chalcones
Srinivasa Rao
experimental part, p. 4373 - 4376 (2012/02/14)
A series of novel 1-(4′-aminophenyl)-3-(substituted aryl/heteroaryl)-2-propen-1-ones (1-16) have been synthesized by treating 4-amino acetophenone with various substituted aromatic and unsubstituted heterocyclic aldehydes in presence of methanol and aqueous alkaline solution at room temperature. Their structures were confirmed by IR, 1H NMR, 13C NMR, EI-MS spectra and elemental analyses data. The synthesized compounds were investigated for their analgesic activity. Compounds 6 and 15 exhibited maximum analgesic activity. Chalcones with electron releasing substituent like amino, hydroxyl, methyl, halogens etc exhibited good analgesic activity.
