Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives
In order to prepare, at low cost, new compounds active against <i>Plasmodium falciparum</i>, and with a less side-effects, we have designed and synthesized a library of 1,4-disubstituted piperidine derivatives from 4-aminopiperidine derivatives <b>6</b>. The resulting compoun...
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-01-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/25/2/299 |
| _version_ | 1828453028796039168 |
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| author | Rokhyatou Seck Abdoulaye Gassama Sandrine Cojean Christian Cavé |
| author_facet | Rokhyatou Seck Abdoulaye Gassama Sandrine Cojean Christian Cavé |
| author_sort | Rokhyatou Seck |
| collection | DOAJ |
| description | In order to prepare, at low cost, new compounds active against <i>Plasmodium falciparum</i>, and with a less side-effects, we have designed and synthesized a library of 1,4-disubstituted piperidine derivatives from 4-aminopiperidine derivatives <b>6</b>. The resulting compound library has been evaluated against chloroquine-sensitive (3D7) and chloroquine-resistant (W2) strains of <i>P. falciparum.</i> The most active molecules—compounds <b>12d</b> (13.64 nM (3D7)), <b>13b</b> (4.19 nM (3D7) and 13.30 nM (W2)), and <b>12a</b> (11.6 nM (W2))—were comparable to chloroquine (22.38 nM (3D7) and 134.12 nM (W2)). |
| first_indexed | 2024-12-11T00:01:31Z |
| format | Article |
| id | doaj.art-cc65d6acefb247ab80de775db2bc47bb |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-11T00:01:31Z |
| publishDate | 2020-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-cc65d6acefb247ab80de775db2bc47bb2022-12-22T01:28:27ZengMDPI AGMolecules1420-30492020-01-0125229910.3390/molecules25020299molecules25020299Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine DerivativesRokhyatou Seck0Abdoulaye Gassama1Sandrine Cojean2Christian Cavé3Laboratoire de Chimie et Physique des Matériaux (LCPM), Université Assane SECK de Ziguinchor, Ziguinchor BP 523, SenegalLaboratoire de Chimie et Physique des Matériaux (LCPM), Université Assane SECK de Ziguinchor, Ziguinchor BP 523, SenegalCentre National de Référence du Paludisme, Hôpital Bichat-Claude Bernard, APHP, 75018 Paris, FranceUniversité Paris-Saclay, CNRS BioCIS, 92290 Châtenay-Malabry, FranceIn order to prepare, at low cost, new compounds active against <i>Plasmodium falciparum</i>, and with a less side-effects, we have designed and synthesized a library of 1,4-disubstituted piperidine derivatives from 4-aminopiperidine derivatives <b>6</b>. The resulting compound library has been evaluated against chloroquine-sensitive (3D7) and chloroquine-resistant (W2) strains of <i>P. falciparum.</i> The most active molecules—compounds <b>12d</b> (13.64 nM (3D7)), <b>13b</b> (4.19 nM (3D7) and 13.30 nM (W2)), and <b>12a</b> (11.6 nM (W2))—were comparable to chloroquine (22.38 nM (3D7) and 134.12 nM (W2)).https://www.mdpi.com/1420-3049/25/2/299piperidinereductive aminationreagent-based diversityantimalarialdrug lead |
| spellingShingle | Rokhyatou Seck Abdoulaye Gassama Sandrine Cojean Christian Cavé Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives Molecules piperidine reductive amination reagent-based diversity antimalarial drug lead |
| title | Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives |
| title_full | Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives |
| title_fullStr | Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives |
| title_full_unstemmed | Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives |
| title_short | Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives |
| title_sort | synthesis and antimalarial activity of 1 4 disubstituted piperidine derivatives |
| topic | piperidine reductive amination reagent-based diversity antimalarial drug lead |
| url | https://www.mdpi.com/1420-3049/25/2/299 |
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