73004-43-0Relevant academic research and scientific papers
Synthesis, characterisation and in vitro cytotoxicity studies of a series of chiral platinum(II) complexes based on the 2-aminomethylpyrrolidine ligand: X-ray crystal structure of [PtCl2(R-dimepyrr)] (R-dimepyrr = N-dimethyl-2(R)-aminomethylpyrrolidine)
Diakos, Connie I.,Zhang, Mei,Beale, Philip J.,Fenton, Ronald R.,Hambley, Trevor W.
scheme or table, p. 2807 - 2814 (2009/10/10)
A series of platinum(II) complexes were synthesised based on the enantiomerically pure amino acid proline. Novel synthetic pathways were developed, adapted from standard peptide chemistry, to produce the 2-aminomethylpyrrolidine (pyrr) ligand and its derivatives with differing arrangements of methyl substituents at the exocyclic amine sites. The crystal structure of [PtCl2(R-dimepyrr)] (R-dimepyrr = N,N-dimethyl-2(R)-aminomethylpyrrolidine) is reported and the five-membered ligand ring has been shown to be in an envelope conformation. Cytotoxicity studies were carried out on the ovarian cancer A2780 tumour cell line and its cisplatin-resistant variant, A2780cisR. Remarkably good activity was seen for several of the drugs when compared to cisplatin despite the addition of substantial steric bulk to the amine groups, and there was a lack of cross-resistance with cisplatin seen for some compounds.
Studies in Potential Filaricides: Part 19 - Synthesis of 1-Methyl-4-substituted Carbonylpiperazines as Diethylcarbamazine Analogs
Sharma, Satyavan,Agarwal, V. K.,Dubey, S. K.,Iyer, R. N.,Anand, Nitya,et al.
, p. 748 - 751 (2007/10/02)
The synthesis and antifilarial activity of a series of 1-methyl-4-substituted carbamoyl- and carbonylpiperazines (6 - 42) against Litomosoides carinii in cotton rats and Dipetalonema viteae in Mastomys natalensis are described.The most potent compound of this series, 1-methyl-4-(pyrrolidin-1-yl)carbonylpiperazine (7) causes 95 - 98 percent reduction of blood microfilarial count in cotton rats infected with L. carinii at an intraperitoneal or oral dose of 1.5 (base) or 3 (citrate) mg/kg given for 6 days.A number of other compounds also exhibit marked microfilaricidal efffect in the dose range of 6 - 30 mg/kg.
