In Vitro and In Vivo Studies of the Biological Activity of Novel Arylimidamides against Trypanosoma cruzi

被引：12

作者：

De Araujo, J. S. ^{[1
]}

Da Silva, C. F. ^{[1
]}

Batista, D. G. J. ^{[1
]}

Da Silva, P. B. ^{[1
]}

Meuser, M. B. ^{[1
]}

Aiub, C. A. F. ^{[2
]}

da Silva, M. F. V. ^{[2
]}

Araujo-Lima, C. F. ^{[3
]}

Banerjee, M. ^{[4
]}

Farahat, A. A. ^{[4
,5
]}

Stephens, C. E. ^{[6
]}

Kumar, A. ^{[4
]}

Boykin, D. W. ^{[4
]}

Soeiro, M. N. C. ^{[1
]}

机构：

[1] Fundacao Oswaldo Cruz, Inst Oswaldo Cruz, Lab Biol Celular, Rio De Janeiro, Brazil

[2] Univ Estado Rio de Janeiro, Dept Genet & Biol Mol, BR-20550011 Rio De Janeiro, Brazil

[3] Univ Estado Rio de Janeiro, Dept Biofis & Biometria, BR-20550011 Rio De Janeiro, Brazil

[4] Georgia State Univ, Dept Chem, Atlanta, GA 30303 USA

[5] Mansoura Univ, Fac Pharm, Dept Organ Pharmaceut Chem, Mansoura, Egypt

[6] Georgia Regents Univ, Dept Chem & Phys, Augusta, GA USA

来源：

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 2014年 / 58卷 / 07期

关键词：

CHAGAS-DISEASE; TRYPANOCIDAL ACTIVITY; DIAMIDINES; AMIDINES; ANALOGS; AGENTS; DB766;

D O I：

10.1128/AAC.01403-13

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

Fifteen novel arylimidamides (AIAs) (6 bis-amidino and 9 mono-amidino analogues) were assayed against Trypanosoma cruzi in vitro and in vivo. All the bis-AIAs were more effective than the mono-AIAs, and two analogues, DB1967 and DB1989, were further evaluated in vivo. Although both of them reduced parasitemia, protection against mortality was not achieved. Our results show that the number of amidino-terminal units affects the efficacy of arylimidamides against T. cruzi.

引用

页码：4191 / 4195

页数：5

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