Synthesis and in Vitro Evaluation of Novel Highly Potent Coumarin Inhibitors of Gyrase B

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 1999 Aug 18

PMID 10450985

Citations 15

Authors

P Laurin

D Ferroud

M Klich

P Mauvais

P Lassaigne

A Bonnefoy

B Musicki

Affiliations

Soon will be listed here.

Abstract

The design, synthesis, and in vitro biological activity of a series of novel coumarin inhibitors of gyrase B is presented. Replacement of the 3-acylamino residue (3-NHCOR) of coumarin drugs with reversed isosteres C(=O)R, C(=N-OR)R', COOR, CONHR and CONHOR leads to highly potent analogues which displayed excellent inhibition of the negative supercoiling of the relaxed DNA and antibacterial activity.

Citing Articles

The Synthesis and Evaluation of Aminocoumarin Peptidomimetics as Cytotoxic Agents on Model Bacterial Strains.

Kowalczyk P, Wilk M, Parul P, Szymczak M, Kramkowski K, Raj S Materials (Basel). 2021; 14(19).

PMID: 34640121 PMC: 8510199. DOI: 10.3390/ma14195725.

Coumarin Derivatives as New Toxic Compounds to Selected K12, R1-R4 Strains.

Kowalczyk P, Madej A, Paprocki D, Szymczak M, Ostaszewski R Materials (Basel). 2020; 13(11).

PMID: 32486298 PMC: 7321437. DOI: 10.3390/ma13112499.

Coumarin-benzimidazole hybrids as a potent antimicrobial agent: synthesis and biological elevation.

Singh L, Avula S, Raj S, Srivastava A, Palnati G, Tripathi C J Antibiot (Tokyo). 2017; 70(9):954-961.

PMID: 28634338 DOI: 10.1038/ja.2017.70.

Cytotoxic Properties of Three Isolated Coumarin-hemiterpene Ether Derivatives from Lam.

Mojarrab M, Emami S, Delazar A, Tayarani-Najaran Z Iran J Pharm Res. 2017; 16(1):221-229.

PMID: 28496477 PMC: 5423249.

Antifungal and antioxidant activities of Coleonema album and C. pulchellum against skin diseases.

Fajinmi O, Gruz J, Tarkowski P, Kulkarni M, Finnie J, van Staden J Pharm Biol. 2017; 55(1):1249-1255.

PMID: 28262031 PMC: 6130550. DOI: 10.1080/13880209.2017.1296470.