13129-69-6Relevant academic research and scientific papers
Inhibitory effects of isatin Mannich bases on carbonic anhydrases, acetylcholinesterase, and butyrylcholinesterase
Ozgun, Dilan Ozmen,Yamali, Cem,Gul, Halise Inci,Taslimi, Parham,Gulcin, Ilhami,Yanik, Telat,Supuran, Claudiu T.
, p. 1498 - 1501 (2016)
The effects of isatin Mannich bases incorporating (1-[piperidin-1-yl (P1)/morpholin-4-yl (P2)/N-methylpiperazin-1-yl (P3)]methyl)-1H-indole-2,3-dione) moieties against human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoenzymes hCA I and hCA II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzymes were evaluated. P1–P3 demonstrated impressive inhibition profiles against AChE and BChE and also inhibited both CAs at nanomolar level. These inhibitory effects were more powerful in all cases than the reference compounds used for all these enzymes. This study suggests that isatin Mannich bases P1–P3 are good candidate compounds especially for the development of new cholinesterase inhibitors since they were 2.2–5.9 times better inhibitors than clinically used drug Tacrine.
Synthesis, characterization and antibacterial activity of carbamate derivatives of isatin
Jabbar, Sarrah Sattar
, p. 2026 - 2030 (2018)
In search of novel antibacterial agent, a series of new isatin derivatives(3a-d)have been synthesized by condensation isatin(2,3-indolinendione) with piperidine(hexahydropyridine), hydrazine hydrate and Boc-amino acids respectively. Compounds synthesized have been characterized by IR spectroscopy and elemental analysis. In addition, the in vitro antibacterial properties have been tested against E. coli, P. aeruginosa, and Bacillus cereus, S. aureus by employing the well diffusion technique. A majority of the synthesized compounds were showing good antibacterial activity and from comparisons of the compounds, where 3d has been determined to be the most active compound.
Synthesis of novel isatin-thiazoline and isatin-benzimidazole conjugates as anti-breast cancer agents
Taher, Azza T.,Khalil, Nadia A.,Ahmed, Eman M.
experimental part, p. 1615 - 1621 (2012/03/12)
A series of new isatin-thiazoline 3a-h and isatin-benzimidazole 4a-h derivatives were synthesized via condensation of isatin Mannich bases 2a-h with either 2-aminothiazoline or 2-aminobenzimidazole. The structures of the newly synthesized compounds were c
Hybrid pharmacophore design and synthesis of isatin-benzothiazole analogs for their anti-breast cancer activity
Solomon, V. Raja,Hu, Changkun,Lee, Hoyun
experimental part, p. 7585 - 7592 (2011/02/23)
A hybrid pharmacophore approach was used to design and synthesize isatin-benzothiazole analogs to examine their anti-breast cancer activity. The cytotoxicity of these compounds were determined using three different human breast tumor cell lines, MDA-MB231, MDA-MB468, MCF7, and two non-cancer breast epithelial cell lines, 184B5 and MCF10A. Although all compounds examined were quite effective on all the cancer cell lines examined, the compounds 4-bromo-1-diethylaminomethyl-1H-indole-2,3-dione (21) and 4-chloro-1- dimethylaminomethyl-3-(6-methyl-benzothiazol-2-ylimino)-1,3-dihydroindol-2-one (5e) emerged as the most active compounds of this series. Importantly, the cytotoxic effect of 21 was 10-15-fold higher on cancer than non-cancer cells, suggesting that this compound can be very effective for the control of breast cancer with low side effects. Since 21 showed effective cytotoxicity on MCF7 cells and arrested the cells at G2/M at a similar concentration, these two phenomena may be closely correlated. We conclude that the isatin-linked benzothiazole analog can serve as a prototype molecule for further development of a new class of anti-breast cancer agents.
