120014-30-4Relevant articles and documents
Synthesis, molecular docking studies, and antimicrobial evaluation of new structurally diverse ureas
Patil, Mahadev,Poyil, Anurag Noonikara,Joshi, Shrinivas D.,Patil, Shivaputra A.,Patil, Siddappa A.,Bugarin, Alejandro
, p. 302 - 311 (2019)
A series of new urea derivatives (3a-p) have been synthesized from readily available isocyanates and amines in good to high yields. All synthesized compounds were fully characterized using 1H NMR, 13C NMR, IR, and mass spectrometry. Additionally, the structure of the compound (3n) was confirmed by single-crystal X-ray diffraction. Furthermore, all compounds were evaluated for antimicrobial activity against five bacteria and two fungi. Last but not the least, molecular docking studies with Candida albicans dihydropteroate synthetase were performed and the results are presented herein.
Two novel donepezil-lipoic acid hybrids: Synthesis, anticholinesterase and antioxidant activities and theoretical studies
Terra, Bruna S.,Da Silva, Pedro H. C.,Tramarin, Anna,Franco, Lucas L.,Da Cunha, Elaine F. F.,Macedo, Fernando,Ramalho, Teodorico C.,Bartolini, Manuela,Bolognesi, Maria L.,De Fátima, ?ngelo
, p. 738 - 747 (2018)
Alzheimer disease (AD) is a complex disease related to multiple pathogenic mechanisms. A strategy to develop effective drugs is based on the so-called multi-Target directed ligands (MTDL) by using hybrid compounds. So, in the present study, we have designed and synthesized two hybrids, containing the indanone-piperidine moiety of donepezil, a drug approved for the treatment of AD, and the lipoic acid scaffold, an antioxidant compound endowed with neuroprotective effects. One hybrid was synthesized in four steps with 42percent global yield, and the other hybrid in six steps with 19percent global yield. The latter hybrid displayed moderate inhibitory activity against human acetylcholinesterase (hAChE) and greater activity against human butyrylcholinesterases (hBuChE). The selectivity for hBuChE was further rationalized by theoretical study. Importantly, the second hybrid showed a good antioxidant activity, exhibiting better ability in scavenging 2,2-diphenyl- 1 picrylhydrazyl (DPPH) radicals than lipoic acid.
Chemoselective Alkylation of Aminoacetophenones with Alcohols by Using a Palladacycle-Phosphine Catalyst
Mamidala, Ramesh,Subramani, M. Siva,Samser, Shaikh,Biswal, Priyabrata,Venkatasubbaiah, Krishnan
, p. 6286 - 6296 (2018/11/23)
The development of efficient and environmentally benign palladacycle-phosphine catalyzed process to enable the formation of chemoselective C-alkylated or N-alkylated aminoacetophenones with alcohols is described. This methodology proved to be tunable by variation of the base and the temperature, which allows for the isolation of structurally diverse C-alkylated and N-alkylated aminoacetophenones. Moreover, this methodology has been applied to the synthesis of biologically and industrially important donepezil.
