99552-32-6Relevant academic research and scientific papers
Synthesis, Characterization and Biological Evaluation of Some Novel Regioisomers of Ropivacaine Analogues: An Anaesthetic Drug
Sharavanan,Venkatesan,Bhaskara Suresh Raju,Kabilan
, p. 2180 - 2186 (2020/09/16)
A series of ropivacaine analogues were synthesized by altering the methyl group substituent in the aromatic ring. The synthesized compounds (2a-f and 3a-f) were characterized by using IR, NMR and HRMS analysis and then compounds 3a-3f were screened in vitro anticancer (MTT assay) activity against breast cancer cell line (MCF-7), antibacterial and antioxidant (DPPH scavenging assay) studies. The biological studies revealed that the compounds 3c and 3f have shown a good inhibitory activity against MCF-7 cell line. Compounds 3e, 3b, 3c and 3f showed moderate antioxidant activity. There was no inhibition observed against both Gram-positive and Gram-negative bacteria.
Synthesis of 2-piperidinecarboxylic acid derivatives as potential anticonvulsants
Ho, Bin,Venkatarangan, Prabha M.,Cruse, Sharon F.,Hinko, Christine N.,Andersen, Peter H.,Crider, Albert M.,Adloo, Ahmad A.,Roane, David S.,Stables, James P.
, p. 23 - 31 (2007/10/03)
A variety of 2-piperidinecarboxamides were synthesized and evaluated for anticonvulsant activity using the MES and sc PTZ tests in mice and rats. Neurotoxicity was determined by the rotorod test. Several N-(benzyl)-2- piperidinecarboxamides exhibited potent MES activity in mice [2-CF3 14, ED50 = 29 mg/kg; 3-F 16, ED50 = 31 mg/kg; and 3-CF3 17, ED50 = 24 mg/kg]. The most active compounds in the MES test in mice were the 2,6- dimethylanilides [(R,S)-34, ED50 = 5.8 mg/kg; (R)-35, ED50 = 5.7 mg/kg; and (S)-36, ED50 = 14.8 mg/kg]. The enantiomer (S)-36 was about two-fold less potent in the MES test than (R)-35 and also was less neurotoxic. Acylation of the piperidine ring nitrogen of 12 anal 34 led to a decrease in the MES activity. In the N-(α-methylbenzyl)-2-piperidine-carboxamides, the stereochemistry at either the 2-position of the piperidine ring or at the α- position of the N-(α-methylbenzyl) group does not significantly affect MES activity.
