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Volumn 46, Issue 4, 2005, Pages 695-698

Derivatives of pentamidine designed to target the Leishmania lipophosphoglycan

Author keywords

Boronate drug targeting; Leishmania; Pentamidine

Indexed keywords

LIPOPHOSPHOGLYCAN; PENTAMIDINE DERIVATIVE;

EID: 11144321488     PISSN: 00404039     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.tetlet.2004.11.112     Document Type: Article
Times cited : (16)

References (32)
  • 27
    • 11144295659 scopus 로고    scopus 로고
    • note
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    • 11144292011 scopus 로고    scopus 로고
    • note
    • Compounds 2-7 were tested for leishmanicidal activity against the L. chagasi strain as follows. A 10 mM stock solution for each of the eight trials (six compounds in DMSO, pentamidine (1) in DMSO, and a DMSO control) were prepared. Each drug was diluted to a concentration of 400 μM with modified HOMEM buffer system. Addition of 40 μL DMSO in 460 μL HOMEM served as a solvent control. Initially, 100 μL of HOMEM was placed in all 12 rows of 8 columns of an 8 × 12 sterile cell well plate (FALCON 3872). Duplicate serial dilutions of each drug were made as follows: 100 μL of the 400 μM drug solution was pipetted into wells 1 and 2 (rows 1 and 2), 100 μL of the solution in well 1 was pipetted into well 3, and 100 μL of the solution in well 2 was pipetted into well 4. This procedure was repeated until 100 μL was removed from wells 11 and 12 at the end. To each well 100 μL of L. chagasi promastigotes at approximately 5 × 106 parasites/mL was added, and the cell well plate was placed in an incubator at 25°C overnight. The parasites were counted after 24 and 48 h incubation time by pipetting 10 μL of solution from each well under the cover slip of a hemacytometer with a 5 × 5 major grid divided into 4 × 4 minor grids. The number of parasites in two major grids was counted (viewed at 400× magnification), averaged, and converted to parasites/mg by multiplying by 25 × 104. The average parasite counts were converted into percent parasite fatality as shown in Table 1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.