Design, synthesis, and antibacterial evaluation of new quinoline-1, 3, 4-oxadiazole and quinoline-1, 2, 4-triazole hybrids as potential inhibitors of DNA gyrase and …

HA Hofny, MFA Mohamed, HAM Gomaa… - Bioorganic …, 2021 - Elsevier
DNA gyrase and topoisomerase IV (topo IV) inhibitors are among the most interesting
antibacterial drug classes without antibacterial pipeline representative. Twenty-four new …

[HTML][HTML] Novel 1, 2, 4-oxadiazole/pyrrolidine hybrids as DNA gyrase and topoisomerase IV inhibitors with potential antibacterial activity

FOA Frejat, Y Cao, H Zhai, SA Abdel-Aziz… - Arabian Journal of …, 2022 - Elsevier
DNA gyrase is a promising target for antibacterial agents. Several classes of small-molecule
inhibitors have been discovered in recent decades, but none of these have reached the …

Synthesis of novel 2-aminobenzothiazole derivatives as potential antimicrobial agents with dual DNA gyrase/topoisomerase IV inhibition

MMF Ismail, HG Abdulwahab, ES Nossier… - Bioorganic …, 2020 - Elsevier
Novel benzothiazole-based compounds were designed and synthesized as potential
antimicrobial agents with dual DNA gyrase/topoisomerase IV inhibitory activity. The …

Structure–activity relationships of 3-aminoquinazolinediones, a new class of bacterial type-2 topoisomerase (DNA gyrase and topo IV) inhibitors

TP Tran, EL Ellsworth, JP Sanchez, BM Watson… - Bioorganic & medicinal …, 2007 - Elsevier
A series of 3-aminoquinazolinediones was synthesized and evaluated for its antibacterial
and DNA gyrase activity. The SAR around the quinazolinedione core was explored and the …

[HTML][HTML] Design, synthesis, and antibacterial screening of some novel heteroaryl-based ciprofloxacin derivatives as DNA gyrase and topoisomerase IV inhibitors

LH Al-Wahaibi, AA Amer, AA Marzouk, HAM Gomaa… - Pharmaceuticals, 2021 - mdpi.com
A novel series of ciprofloxacin hybrids comprising various heterocycle derivatives has been
synthesized and structurally elucidated using 1H NMR, 13C NMR, and elementary analyses …

[HTML][HTML] Synthesis, antimicrobial activity and molecular docking of novel thiourea derivatives tagged with thiadiazole, imidazole and triazine moieties as potential DNA …

HE Hashem, AEGE Amr, ES Nossier, EA Elsayed… - Molecules, 2020 - mdpi.com
To develop new antimicrobial agents, a series of novel thiourea derivatives incorporated
with different moieties 2–13 was designed and synthesized and their biological activities …

Novel 1, 2, 4-oxadiazole-chalcone/oxime hybrids as potential antibacterial DNA gyrase inhibitors: Design, synthesis, ADMET prediction and molecular docking study

TS Ibrahim, AJ Almalki, AH Moustafa, RM Allam… - Bioorganic …, 2021 - Elsevier
New antibacterial drugs are urgently needed to tackle the rapid rise in multi-drug resistant
bacteria. DNA gyrase is a validated target for the development of new antibacterial drugs …

Synthesis and antibacterial activity of novel and potent DNA gyrase inhibitors with azole ring

A Tanitame, Y Oyamada, K Ofuji, M Fujimoto… - Bioorganic & medicinal …, 2004 - Elsevier
The 4-piperidyl moiety and the pyrazole ring in 1-(3-chlorophenyl)-5-(4-phenoxyphenyl)-3-(4-
piperidyl) pyrazole 2, which has previously shown improved DNA gyrase inhibition and …

Discovery of benzothiazole scaffold-based DNA gyrase B inhibitors

M Gjorgjieva, T Tomasic, M Barancokova… - Journal of medicinal …, 2016 - ACS Publications
Bacterial DNA gyrase and topoisomerase IV control the topological state of DNA during
replication and are validated targets for antibacterial drug discovery. Starting from our …

Discovery of substituted oxadiazoles as a novel scaffold for DNA gyrase inhibitors

Ž Jakopin, J Ilaš, M Barančoková, M Brvar… - European Journal of …, 2017 - Elsevier
DNA gyrase and topoisomerase IV are type IIa topoisomerases that are essential bacterial
enzymes required to oversee the topological state of DNA during transcription and …