Home
Resources
Publications
Synthesis and Antiprotozoal Activity of Dicationic M-Terphenyl and 1,3-dipyridylbenzene Derivatives

Synthesis and Antiprotozoal Activity of Dicationic M-Terphenyl and 1,3-dipyridylbenzene Derivatives

Donald A Patrick, Mohamed A Ismail, Reem K Arafa, Tanja Wenzler, Xiaohua Zhu, Trupti Pandharkar, Susan Kilgore Jones, Karl A Werbovetz, Reto Brun, David W Boykin, Richard R Tidwell

J Med Chem. 2013 Jul 11;56(13):5473-94.

PMID: 23795673

Abstract:

4,4″-Diamidino-m-terphenyl (1) and 36 analogues were prepared and assayed in vitro against T rypanosoma brucei rhodesiense , Trypanosoma cruzi , Plasmodium falciparum , and Leishmania amazonensis . Twenty-three compounds were highly active against T. b. rhodesiense or P. falciparum. Most noteworthy were amidines 1, 10, and 11 with IC50 of 4 nM against T. b. rhodesiense, and dimethyltetrahydropyrimidinyl analogues 4 and 9 with IC50 values of ≤ 3 nM against P. falciparum. Bis-pyridylimidamide derivative 31 was 25 times more potent than benznidazole against T. cruzi and slightly more potent than amphotericin B against L. amazonensis. Terphenyldiamidine 1 and dipyridylbenzene analogues 23 and 25 each cured 4/4 mice infected with T. b. rhodesiense STIB900 with four daily 5 mg/kg intraperitoneal doses, as well as with single doses of ≤ 10 mg/kg. Derivatives 5 and 28 (prodrugs of 1 and 25) each cured 3/4 mice with four daily 25 mg/kg oral doses.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP92068	m-Terphenyl		92-06-8	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: