Synthesis and antileishmanial activity of novel 2,4,6-trisubstituted pyrimidines and 1,3,5-triazines
IR@CDRI: CSIR-Central Drug Research Institute, Lucknow
View Archive Info| Field | Value | |
| Creator |
Sunduru, Naresh
Nishi Palne, Shraddha Chauhan, P M S Gupta, Suman |
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| Date |
2010-08-27T05:46:09Z
2010-08-27T05:46:09Z 2009 |
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| Identifier |
European Journal of Medicinal Chemistry, 44, I6, 2009, 2473-2481
http://hdl.handle.net/123456789/573 |
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| Description |
A series of 2,4,6-trisubstituted pyrimidines and 1,3,5-triazines have been synthesized and screened for their in vitro and in vivo antileishmanial activity against L. donovani. Among all, 14 compounds have shown promising inhibition of 80-100% at 10 µg/ml against promastigotes and IC50 in the range of 0.89-9.68 µg/ml against amastigotes. Three compounds 13, 32 and 33 with good selectivity index (S.I) were screened for their in vivo activity in golden hamsters (Mesocricetus auretus) infected with MHOM/IN/80/Dd8 strain of L. donovani and have shown moderate in vivo inhibition of 48-56 % at a dose of 50 mg/Kgx5, I.P route for 5 days.
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| Format |
185610 bytes
application/pdf |
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| Language |
en
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| Subject |
Leishmaniasis
pyrimidine 1,3,5-triazine |
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| Title |
Synthesis and antileishmanial activity of novel 2,4,6-trisubstituted pyrimidines and 1,3,5-triazines
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| Type |
Article
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