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A New Class of ?-Pyrrolidino-1,2,3-Triazole Derivatives as ?-Adrenergic Receptor Inhibitors: Synthesis, Pharmacological, and Docking Studies.

ABSTRACT: New 1,4-disubstituted ?-pyrrolidino-1,2,3-triazoles were synthesized using a reusable copper-iodide-doped neutral alumina catalyst. Synthesis of diversely substituted triazoles and recyclability of CuI catalyst explains the broad scope of this protocol. The synthesized compounds were screened for their antimicrobial and anticancer properties. Most of the compounds showed significant antimicrobial activities against all the tested microorganisms compared to standard drugs. Furthermore, compounds 5a, 5e, 5g, 5h, 5i, and 5j showed moderate to potent activities against A549 and HepG-2 cells. In addition, compounds 5g and 5h displayed potential cytotoxicity activity against A549 cells with IC50 values of 72 ± 3.21 and 58 ± 2.31 µM, respectively. The molecular docking study revealed that some of the synthesized compounds exhibited comparable binding as co-crystalized ligands with the DNA topoisomerase IV and anaplastic lymphoma kinase receptors.

SUBMITTER: Easwaramoorthi K 

PROVIDER: S-EPMC6803965 | biostudies-literature | 2019 Sep

REPOSITORIES: biostudies-literature

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A New Class of β-Pyrrolidino-1,2,3-Triazole Derivatives as β-Adrenergic Receptor Inhibitors: Synthesis, Pharmacological, and Docking Studies.

Easwaramoorthi Kaliyappan K   Rajendran Jeya A JA   Rao Kella Chennakesava KC   Balachandran Chandrasekar C   Arun Yuvaraj Y   Mahalingam Sakkarapalayam M SM   Arumugam Natarajan N   Almansour Abdulrahman I AI   Kumar Raju Suresh RS   Al-Thamili Dhaifallah M DM   Aoki Shin S  

Molecules (Basel, Switzerland) 20190926 19

New 1,4-disubstituted β-pyrrolidino-1,2,3-triazoles were synthesized using a reusable copper-iodide-doped neutral alumina catalyst. Synthesis of diversely substituted triazoles and recyclability of CuI catalyst explains the broad scope of this protocol. The synthesized compounds were screened for their antimicrobial and anticancer properties. Most of the compounds showed significant antimicrobial activities against all the tested microorganisms compared to standard drugs. Furthermore, compounds  ...[more]

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