Indolylquinoline derivatives are cytotoxic to Leishmania donovani promastigotes and amastigotes in vitro and are effective in treating murine visceral leishmaniasis
IR@IICB: CSIR-Indian Institute of Chemical Biology, Kolkata
View Archive Info| Field | Value | |
| Title |
Indolylquinoline derivatives are cytotoxic to Leishmania donovani
promastigotes and amastigotes in vitro and are effective in treating
murine visceral leishmaniasis
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| Creator |
Chakrabarti, Ganes
Basu, Anirban Manna, Partha Pratim Mahato, Shashi B Mondal, Nirup B Bandyopadhyay, Santu |
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| Subject |
Chemistry
Infectious Diseases and Immunology |
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| Description |
A wide variety of biologically active compounds contain indole and quinoline nuclei. Some
novel indolylquinoline derivatives were synthesized from indole by Friedel-Crafts acylation
reaction. Out of the four derivatives tested, 2-(20-acetamidobenzyl)-3-(39-indolylquinoline) (C)
had no effect on the promastigotes or amastigotes of Leishmania donovani in vitro. The
remaining three analogues, 2-(20-dichloroacetamidobenzyl)-3-(39-indolylquinoline) (A), 2-(20-
chloroacetamidobenzyl)-3-(39-indolylquinoline) (B), and 2-(20-aminobenzyl)-3-(39-indolylquinoline)
(D), inhibited the growth of L. donovani promastigotes in vitro and were cytotoxic to both
the promastigote and amastigote forms of the parasite. These three derivatives were also
effective in eliminating L. donovani amastigotes from BALB/c mouse peritoneal macrophages
in vitro. One indolylquinoline derivative [A] was used to treat established visceral leishmaniasis
in BALB/c mice. This compound was significantly more effective than sodium
antimony gluconate (SAG) in reducing the splenic parasite load at a much lower concentration
(5% of SAG). Our results suggest that indolylquinoline derivatives may be exploited as
antileishmanial agents.
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| Publisher |
Oxford University Press
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| Date |
1999
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| Type |
Article
PeerReviewed |
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| Format |
application/pdf
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| Identifier |
http://www.eprints.iicb.res.in/676/1/JOURNAL_OF_ANTIMICROBIAL_CHEMOTHERAPY_43_(3)_359%2D366;1999[68].pdf
Chakrabarti, Ganes and Basu, Anirban and Manna, Partha Pratim and Mahato, Shashi B and Mondal, Nirup B and Bandyopadhyay, Santu (1999) Indolylquinoline derivatives are cytotoxic to Leishmania donovani promastigotes and amastigotes in vitro and are effective in treating murine visceral leishmaniasis. Journal of Antimicrobial Chemotherapy, 43 (3). pp. 359-366. |
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| Relation |
http://dx.doi.org/10.1093/jac/43.3.359
http://www.eprints.iicb.res.in/676/ |
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