Discovery of Triazines Mimetics as potent antileishmanial agents
IR@CDRI: CSIR-Central Drug Research Institute, Lucknow
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| Creator |
Chauhan, Kuldeep
Sharma, Moni Shivahare, Rahul Debnath, Utsab Gupta, Suman Prabhakar, Y S Chauhan, P M S |
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| Date |
2014-04-25T10:13:33Z
2014-04-25T10:13:33Z 2013 |
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| Identifier |
ACS Medicinal Chemistry Letters, 2013, 4 (11), 1108–1113
http://hdl.handle.net/123456789/1215 |
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| Description |
The World Health Organization has classified the leishmaniasis as a major tropical disease. The discovery of new compounds for leishmaniasis is therefore a pressing concern for the anti-infective research program. We have synthesized 19 compounds of triazine dimers as novel antileishmanial agents. Most of the synthesized derivatives exhibited better activity against intracellular amastigotes (IC50 ranging from 0.77 to 10.32 μM) than the control, pentamidine (IC50 = 13.68 μM) and not toxic to vero cells. Compounds 14 and 15 showed significant in vivo inhibition of 74.41% and 62.64% respectively in L. donovani/hamster model. Moreover, expansion of Th1-type and suppression of Th2-type immune responses proved that compound 14 stimulate mouse macrophages to prevent the progression of leishmania parasite. The molecular docking studies involving PTR1 protein PDB further validated the concepts involved the design of these compounds. Among the investigated analogues, compound 14 has emerged as potential one to enlarge the scope of the study.
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450373 bytes
application/pdf |
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| Language |
en
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| Relation |
CSIR-CDRI Communication No. 8549
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| Subject |
L. donovani
Triazine Pentamidine In vitro/in vivo Pteridine reductase 1 |
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| Title |
Discovery of Triazines Mimetics as potent antileishmanial agents
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| Type |
Article
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