Balancing physicochemical properties of phenylthiazole compounds with antibacterial potency by modifying the lipophilic side chain

A Mancy, NS Abutaleb, MM Elsebaei… - ACS infectious …, 2019 - ACS Publications
Bacterial resistance to antibiotics is presently one of the most pressing healthcare
challenges and necessitates the discovery of new antibacterials with unique chemical …

Naphthylthiazoles: Targeting Multidrug-Resistant and Intracellular Staphylococcus aureus with Biofilm Disruption Activity

M Hagras, NS Abutaleb, AO Ali… - ACS infectious …, 2018 - ACS Publications
Thirty-two new naphthylthiazole derivatives were synthesized with the aim of exploring their
antimicrobial effect on multidrug-resistant Gram-positive bacteria. Compounds 25 and 32 …

Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness

Y Hosny, NS Abutaleb, M Omara, M Alhashimi… - European journal of …, 2020 - Elsevier
Compounds with high lipophilic properties are often associated with bad physicochemical
properties, triggering many off-targets, and less likely to pass clinical trials. Two …

Development of Biphenylthiazoles Exhibiting Improved Pharmacokinetics and Potent Activity Against Intracellular Staphylococcus aureus

M Hagras, NS Abutaleb, NM Elhosseiny… - ACS Infectious …, 2020 - ACS Publications
Exploring the structure–activity relationship (SAR) at the cationic part of arylthiazole
antibiotics revealed hydrazine as an active moiety. The main objective of the study is to …

Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity

A Kotb, NS Abutaleb, MA Seleem, M Hagras… - European journal of …, 2018 - Elsevier
A new series of phenylthiazoles with t-butyl lipophilic component was synthesized and their
antibacterial activity against a panel of multidrug-resistant bacterial pathogens was …

From phenylthiazoles to phenylpyrazoles: broadening the antibacterial spectrum toward carbapenem-resistant bacteria

A Hammad, NS Abutaleb, MM Elsebaei… - Journal of medicinal …, 2019 - ACS Publications
The narrow antibacterial spectrum of phenylthiazole antibiotics was expanded by replacing
central thiazole with a pyrazole ring while maintaining its other pharmacophoric features …

Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA)

MM Elsebaei, H Mohammad, M Abouf… - European journal of …, 2018 - Elsevier
The promising activity of phenylthiazoles against multidrug-resistant bacterial pathogens, in
particular MRSA, has been hampered by their limited systemic applicability, due to their …

Investigating the Antibacterial Activity of Biphenylthiazoles against Methicillin- and Vancomycin-Resistant Staphylococcus aureus (MRSA and VRSA)

M Hagras, H Mohammad, MS Mandour… - Journal of Medicinal …, 2017 - ACS Publications
Phenylthiazoles were reported previously as a new scaffold with antibacterial activity against
an array of multidrug-resistant staphylococci. However, their promising antibacterial activity …

tert-Butylphenylthiazoles with an oxadiazole linker: a novel orally bioavailable class of antibiotics exhibiting antibiofilm activity

A Kotb, NS Abutaleb, M Hagras, A Bayoumi… - RSC …, 2019 - pubs.rsc.org
The structure–activity and structure–kinetic relationships of a new tert-butylphenylthiazole
series with oxadiazole linkers were conducted with the objective of obtaining a new orally …

Alkoxyphenylthiazoles with broad-spectrum activity against multidrug-resistant gram-positive bacterial pathogens

M ElAwamy, H Mohammad, A Hussien… - European Journal of …, 2018 - Elsevier
With the continued rise of antibiotic resistance and reduced susceptibility to almost all front-
line antibiotics, multidrug-resistant Gram-positive bacterial infections represent an incessant …