Antiproliferative, antiangiogenic and apoptotic effect of new hybrids of quinazoline-4 (3H)-ones and sulfachloropyridazine

SS Zahran, FA Ragab, MG El-Gazzar… - European Journal of …, 2023 - Elsevier
Three new sets of quinazolinones bearing sulfachloropyridazine 4a-f, 6a-i and 8a-i were
designed and synthesized. All the synthesized compounds were screened for their in vitro …

Antibacterial activity evaluation of pleuromutilin derivatives with 4 (3H)-quinazolinone scaffold against methicillin-resistant Staphylococcus aureus

Y Deng, Y Zhang, XH Chen, CH Li - European Journal of Medicinal …, 2023 - Elsevier
Growing antibiotic resistance is causing a health care crisis, leading to an urgent need for
new antibiotics to tackle serious hospital and community infections. Pleuromutilin, a naturally …

Design, synthesis, anticancer, and antibacterial evaluation of some quinazolinone‐based derivatives as DHFR inhibitors

EO Osman, SH Emam, A Sonousi… - Drug Development …, 2023 - Wiley Online Library
Two series of quinazolinone derivatives were designed and synthesized as dihydrofolate
reductase (DHFR) inhibitors. All compounds were evaluated for their antibacterial and …

Novel quinazolinone disulfide analogues as pqs quorum sensing inhibitors against Pseudomonas aeruginosa

S Sabir, T Das, R Kuppusamy, TT Yu, MDP Willcox… - Bioorganic …, 2023 - Elsevier
It is well established that the quorum sensing (QS) in Pseudomonas aeruginosa is primarily
responsible for the synthesis and the release of several virulence factors including …

Design and synthesis of novel quinazolinone-based derivatives as EGFR inhibitors with antitumor activity

A Sonousi, RA Hassan, EO Osman… - Journal of Enzyme …, 2022 - Taylor & Francis
Abstract Nineteen new quinazolin-4 (3 H)-one derivatives 3a–g and 6a–l were designed
and synthesised to inhibit EGFR. The antiproliferative activity of the synthesised compounds …

Design, Synthesis, Pharmacological Evaluation of Quinazolin-4(3H)-Ones Bearing Urea Functionality as Potential VEGFR-2 Inhibitors

MM Al-Sanea, HM Hafez, AAB Mohamed… - Drug Design …, 2024 - Taylor & Francis
Background In response to the urgent need for continuous discovery of new anti-proliferative
agents, a new series of quinazoline compounds 5a-r was prepared. Methods As a reference …

Efficacy of a brain-penetrant antiviral in lethal Venezuelan and eastern equine encephalitis mouse models

X Cao, D Yang, J Parvathareddy, Y Chu… - Science Translational …, 2023 - science.org
Venezuelan and eastern equine encephalitis viruses (VEEV and EEEV, respectively) are
mosquito-borne, neuroinvasive human pathogens for which no FDA-approved therapeutic …

Cobalt(II)-Catalyzed Directed C–H Functionalization/[3+2] Annulation of N-Arylguanidines with Alkynes

H Parihar, N Thirupathi - Organic Letters, 2022 - ACS Publications
A family of N, N′-diaryl-N ″-(quinolin-8-yl) guanidines were prepared by two methods, and
these guanidines were subjected to Co (II)-catalyzed C–H functionalization/annulation with …

Copper and In Situ-Generated Triflic Acid Relay-Promoted Four-Component Cascade Reaction for the Construction of Polysubstituted Cycloguanidines

Y Zhao, R Yang, C Wu, S Wang, X Liu… - The Journal of Organic …, 2023 - ACS Publications
An unprecedented copper and in situ-generated triflic acid relay-promoted four-component
cascade reaction of cyanamides, diaryliodonium triflates, propargylic amines, and H2O was …

Direct synthesis of N 2-unprotected five-membered cyclic guanidines by regioselective [3+ 2] annulation of aziridines and cyanamides

CC Wang, XL Wang, QL Zhang, J Liu, ZW Ma… - Organic Chemistry …, 2022 - pubs.rsc.org
A novel and efficient [3+ 2] annulation of 2-substituted aziridines and N-tosyl cyanamides via
a domino regioselective ring-opening/5-exo-dig cyclization procedure has been developed …