Abstract
In the present work, the syntheses of new 4-amino-7-chloroquinoline N-derivatives were performed by selective modification of the side chain amino group of N-(7-chloroquinoline-4-yl) alkyldiamines, basis framework of chloroquine (CQ) drug through the incorporation of heterocyclic 2-imino-thiazolidine-4-one and {sup 1}H-pyrrol-2,5-dione systems. These potential activity modulators were selected thanks to their characteristic properties, and evaluated by virtual screening employing the OSIRIS and Molinspirations platforms. Designed and synthesized quinolinic derivatives could increase the antimalarial activity of CQ analogues without affecting the lipophilicity as described in literature, suggesting them as candidates for further biological assessments. (author)
Rojas, Fernando A;
Kouznetsov, Vladimir V., E-mail: kouznet@uis.edu.co
[1]
- Laboratorio de Quimica Organica y Biomolecular, Escuela de Quimica, Universidad Industrial de Santander, Bucaramanga (Colombia)
Citation Formats
Rojas, Fernando A, and Kouznetsov, Vladimir V., E-mail: kouznet@uis.edu.co.
Property-based design and synthesis of new chloroquine hybrids via simple incorporation of 2-imino-thiazolidine-4-one or 1h-pyrrol-2, 5-dione fragments on the 4-amino-7-chloroquinoline side chain.
Brazil: N. p.,
2011.
Web.
doi:10.1590/S0103-50532011000900021.
Rojas, Fernando A, & Kouznetsov, Vladimir V., E-mail: kouznet@uis.edu.co.
Property-based design and synthesis of new chloroquine hybrids via simple incorporation of 2-imino-thiazolidine-4-one or 1h-pyrrol-2, 5-dione fragments on the 4-amino-7-chloroquinoline side chain.
Brazil.
https://doi.org/10.1590/S0103-50532011000900021
Rojas, Fernando A, and Kouznetsov, Vladimir V., E-mail: kouznet@uis.edu.co.
2011.
"Property-based design and synthesis of new chloroquine hybrids via simple incorporation of 2-imino-thiazolidine-4-one or 1h-pyrrol-2, 5-dione fragments on the 4-amino-7-chloroquinoline side chain."
Brazil.
https://doi.org/10.1590/S0103-50532011000900021.
@misc{etde_21565692,
title = {Property-based design and synthesis of new chloroquine hybrids via simple incorporation of 2-imino-thiazolidine-4-one or 1h-pyrrol-2, 5-dione fragments on the 4-amino-7-chloroquinoline side chain}
author = {Rojas, Fernando A, and Kouznetsov, Vladimir V., E-mail: kouznet@uis.edu.co}
abstractNote = {In the present work, the syntheses of new 4-amino-7-chloroquinoline N-derivatives were performed by selective modification of the side chain amino group of N-(7-chloroquinoline-4-yl) alkyldiamines, basis framework of chloroquine (CQ) drug through the incorporation of heterocyclic 2-imino-thiazolidine-4-one and {sup 1}H-pyrrol-2,5-dione systems. These potential activity modulators were selected thanks to their characteristic properties, and evaluated by virtual screening employing the OSIRIS and Molinspirations platforms. Designed and synthesized quinolinic derivatives could increase the antimalarial activity of CQ analogues without affecting the lipophilicity as described in literature, suggesting them as candidates for further biological assessments. (author)}
doi = {10.1590/S0103-50532011000900021}
journal = []
issue = {9}
volume = {22}
place = {Brazil}
year = {2011}
month = {Sep}
}
title = {Property-based design and synthesis of new chloroquine hybrids via simple incorporation of 2-imino-thiazolidine-4-one or 1h-pyrrol-2, 5-dione fragments on the 4-amino-7-chloroquinoline side chain}
author = {Rojas, Fernando A, and Kouznetsov, Vladimir V., E-mail: kouznet@uis.edu.co}
abstractNote = {In the present work, the syntheses of new 4-amino-7-chloroquinoline N-derivatives were performed by selective modification of the side chain amino group of N-(7-chloroquinoline-4-yl) alkyldiamines, basis framework of chloroquine (CQ) drug through the incorporation of heterocyclic 2-imino-thiazolidine-4-one and {sup 1}H-pyrrol-2,5-dione systems. These potential activity modulators were selected thanks to their characteristic properties, and evaluated by virtual screening employing the OSIRIS and Molinspirations platforms. Designed and synthesized quinolinic derivatives could increase the antimalarial activity of CQ analogues without affecting the lipophilicity as described in literature, suggesting them as candidates for further biological assessments. (author)}
doi = {10.1590/S0103-50532011000900021}
journal = []
issue = {9}
volume = {22}
place = {Brazil}
year = {2011}
month = {Sep}
}