72512-24-4Relevant academic research and scientific papers
Synthesis and biological evaluation of new 2,4,6-trisubstituted pyrimidines and their N-alkyl derivatives
Kahriman, Nuran,Serdaro?lu, Vildan,Peker, K?van?,Ayd?n, Ali,Usta, Asu,Fandakl?, Seda,Yayl?, Nurettin
, p. 580 - 594 (2018/11/25)
A series of new 2,4,6-trisubstituted pyrimidines and their N-alkyl bromide derivatives were prepared based upon methoxy substituted azachalcones as the starting materials. All newly synthesized compounds were screened for their anti-proliferative, cytotoxic, antibacterial activities and DNA/protein binding affinity. In vitro cell proliferation inhibitory and cell cytotoxic effects of 2,4,6-trisubstituted pyrimidines (1–9) and their N-alkyl bromide derivatives (2a-c, 3a-c, 5a-c, 6a-c, 8a-c, 9a-c) were obtained with the help of the 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) cell proliferation, LDH cytotoxicity detection, and microdilution assays. The antimicrobial activity for these compounds was also evaluated following the European Pharmacopoeia 8.0 protocol. The interactions of these compounds with DNA or bovine serum albumin were investigated by the spectrophotometric titration method. When the cytotoxic analysis and anticancer properties of the compounds were examined, most of the compounds significantly exhibited an anti-proliferative potency on cancer cells (IC50 ～ 2–10 μg/mL) and caused a cytotoxic effect as low as control drugs, 5-fluorouracil, and cisplatin (～7–15%). Because the compound-DNA adducts are hyperchromic or hypochromic, they caused variations in their spectra. This situation shows they can be linked to DNA by the groove binding mode at a binding constant range of 2.0 × 104 and 2.4 × 105 M?1. The antimicrobial screening results revealed that our new compounds for some human Gram(+) and Gram(?) pathogen bacteria showed remarkable activity with MIC values between 7.81 and 125 μg/mL. Overall, incorporation of alkyl chain to pyrimidines in the generation of N-alkyl bromides has resulted in showing differences in DNA/protein binding affinity, along with anti-proliferative and cytotoxic activity in favor of new compounds.
A Convenient Synthesis of Bipyrido-Fused Coumarins and Their Biological Evaluation
Giri, Rakesh R.,Brahmbhatt, Dinkar I.
, p. 2630 - 2636 (2019/08/21)
A convenient and efficient strategy has been devised for the synthesis of bipyrido-fused coumarins employing Kr?hnke's pyridine synthesis approach. In the present work, 4-hydroxycoumarins 1a–d were reacted with appropriate chalcones 2a–c to afford desired
Synthesis and antifungal activity of chalcone derivatives
Zheng, Yuanyuan,Wang, Xuesong,Gao, Sumei,Ma, Min,Ren, Guiming,Liu, Huabing,Chen, Xiaohong
, p. 1804 - 1810 (2015/03/04)
In the present study, using chalcone as a lead compound, a series of its derivatives (compounds 1-30) were designed and synthesised. Their activity of anti-pathogenic fungi of plants has been evaluated. It is found that these compounds have good antifunga
An efficient synthesis of some new 3-bipyridinyl substituted coumarins as potent antimicrobial agents
Lad, Hemali B.,Giri, Rakesh R.,Brahmbhatt
supporting information, p. 227 - 229 (2013/06/26)
As a part of the ongoing studies in developing new antimicrobials, a series of structurally novel 3-bipyridinyl substituted coumarin derivatives 4a-f and 5a-f were synthesized by a single-step reaction protocol under Krohnke's reaction conditions. 1
NEUE WEGE ZU 1H-UND 2H-PYRROLEN
Pfoertner, Karl-Heinz,Foricher, Joseph
, p. 658 - 663 (2007/10/02)
A synthesis of 1H-pyrroles is described starting with pyridine analogues of chalcones and involving the reacxtion of acetic anhydride with 1-pyrroline-1-oxides.Another route leads from 1-pyrrolines to 2H-pyrroles via bromination with N-bromosuccinimide and subsequent dehydrobromination in dimethylformamide.
