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Synthesis of Pyrrolo[1,2-b]isoquinolines through Carbopalladation Initiated Domino Reactions. Evaluation as New Antileishmanial Agents
Iratxe Barbolla
* 1 ,
Leidi Hernández-Suárez
1 ,
Viviana Quevedo-Tumailli
1, 2, 3 ,
Deyani Nocedo-Mena
1 ,
Sonia Arrasate
1 ,
María Auxiliadora Dea-Ayuela
4 ,
Nuria Sotomayor
1 ,
Esther Lete
1
1  Departamento de Química Orgánica e Inorgánica, Facultad de Ciencia y Tecnología, Universidad del País Vasco / Euskal Herriko Unibertsitatea UPV/EHU, Apdo. 644, 48080, Bilbao, Spain.
2  RNASA-IMEDIR, Computer Science Faculty, University of A Coruña, 15071, A Coruña, Spain.
3  Universidad Estatal Amazónica UEA, Puyo, 160150, Pastaza, Ecuador.
4  Departamento de Farmacia, Facultad de Ciencias de la Salud, Universidad CEU Cardenal Herrera, Edificio Seminario s/n, 46113, Moncada, Valencia, Spain.
Published: 15 January 2021 by MDPI in MOL2NET'20, Conference on Molecular, Biomed., Comput. & Network Science and Engineering, 6th ed. congress CHEMBIOMOL-06: Chem. Biol. & Med. Chem. Workshop, Bilbao-Rostock, Germany-Galveston, Texas, USA, 2020
https://doi.org/10.3390/mol2net-06-09174 (registering DOI)
Abstract:

A series of C-10 substituted pyrrolo[1,2-b]isoquinolines have been synthesized via palladium-catalyzed Heck/Suzuki and Heck/anion capture cascade reactions. These compounds have shown antileishmanial activity against cutaneous (L. amazonensis) leishmaniasis, being even 10-fold more potent and selective than the drug of reference, Miltefosine. A Perturbation Theory Machine Learning (PTML) model has also been developed for the prediction of the probability with which a query compound reaches a desired level for multiple parameters vs. different Leishmania species and target proteins.

Keywords: pyrrolo[1,2-b]isoquinolines; antileishmanial; PTML model
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