Adane, Legesse ; Bhagat, Shweta ; Arfeen, Minhajul ; Bhatia, Sonam ; Sirawaraporn, Rachada ; Sirawaraporn, Worachart ; Chakraborti, Asit K. ; Bharatam, Prasad V. (2014) Design and synthesis of guanylthiourea derivatives as potential inhibitors of Plasmodium falciparum dihydrofolate reductase enzyme Bioorganic & Medicinal Chemistry Letters, 24 (2). pp. 613-617. ISSN 0960-894X
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Official URL: http://doi.org/10.1016/j.bmcl.2013.12.009
Related URL: http://dx.doi.org/10.1016/j.bmcl.2013.12.009
Abstract
A new class of compounds based on S-benzylated guanylthiourea has been designed as potential PfDHFR inhibitors using computer aided methods (molecular electrostatic potential, molecular docking). Several compounds in this class have been synthesized starting from guanylthiourea and alkyl bromides. In vitro studies showed that two compounds from this class are active with the IC50 value of 100 μM and 400 nM.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier B.V. |
| Keywords: | Antimalaria; Guanylthiourea; PfDHFR; MESP; Molecular Docking. |
| ID Code: | 116451 |
| Deposited On: | 12 Apr 2021 09:44 |
| Last Modified: | 12 Apr 2021 09:44 |
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