Synthesis and antimicrobial evaluation of 3-(4-arylthieno[2,3-d]pyrimidin-2-yl)- 2H-chromen-2-ones

Author:

Vlasov Sergiy V.1,Kovalenko Sergiy M.2,Shynkarenko Pavlo E.3,Krolenko Konstantin Yu.4,Vlasov Vitaliy S.5

Affiliation:

1. Organic Chemistry Department, National University of Pharmacy, 53, Pushkinska str., Kharkiv 61002, Ukraine

2. Organic Chemistry Department, V. N. Karazin Kharkiv National University, 4, Svobody Sq., Kharkiv 61022, Ukraine

3. Enamine Ltd., 78, Chervonotkatska str., Kiev 02094, Ukraine

4. Medicinal Chemistry Department, National University of Pharmacy, 53, Pushkinska str., Kharkiv 61002, Ukraine

5. Pharmacoinformatics Department, National University of Pharmacy, 53, Pushkinska str., Kharkiv 61002, Ukraine

Abstract

AbstractSyntheses of 3-(4-arylthieno[2,3-d]pyrimidin-2-yl)-2H-chromen-2-ones 5 by the reaction of 2-iminocoumarin-3-carboxamides 1 with (2-aminothiophen-3-yl)(aryl)methanones 2 and by the alternative Suzuki coupling of 4-chlorothieno[2,3-d]pyrimidin-2-yl-2H-chromen-2-one 7 with arylboronic acids were developed. Compound 5d showed higher antimicrobial activity against Staphylococcus aureus than the reference drug streptomycin.

Publisher

Walter de Gruyter GmbH

Subject

Organic Chemistry

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