Synthesis, Antimicrobial, Antiquorum‐Sensing, and Cytotoxic Activities of New Series of Isoindoline‐1,3‐dione, Pyrazolo[5,1‐a]isoindole, and Pyridine Derivatives

Abstract

New series of isoindoline-1,3-diones 2-9, pyrazolo[5,1-a]isoindoles 10-14, and pyridines 16-18 were synthesized. Twenty of the synthesized compounds were screened for their antibacterial activity against S. aureus, B. cereus, and E. coli. Compound 5 was proved to be the most active member in this study, showing the highest antibacterial activity against the three selected microorganisms. The antifungal activity of these compounds was also tested against C. albicans and A. flavus 3375. Compounds 4, 5, 8, and 17a exhibited the best antifungal activity against A. flavus 3375. The same compounds were examined for their antiquorum-sensing activity against Ch. violacium ATCC 12472, whereas compound 5 displayed strong antiquorum-sensing activity. The in vitro cytotoxicity testing of compounds 4-9 and 17a against human normal lung fibroblast (W138) cell line revealed that compounds 4, 5, and 8 are the least cytotoxic analogs in this study. In vivo acute toxicity testing of compounds 4, 5, and 8 was performed. The DNA-binding affinity of compounds 4-9 and 17a was also tested and the obtained results showed that all tested compounds have moderate DNA-binding affinity.

Design, synthesis, biological evaluations, molecular docking, and in vivo studies of novel phthalimide analogs

“…It has been reported that the phthalimide moiety is a very important biologically active pharmacophore . Antimicrobial properties of phthalimide derivatives were reported . Compounds IV and V (Figure ) exhibited high antimicrobial activities against the tested microorganisms .…”

“…Antimicrobial properties of phthalimide derivatives were reported . Compounds IV and V (Figure ) exhibited high antimicrobial activities against the tested microorganisms . Isoindole‐1,3‐dione is a building unit in antitumor, antiangiogenic as well as immunomodulatory drug candidates .…”

Antimicrobial, Antiquorum-sensing and Ex-vivo Antispasmodic Activity of Adhatoda vasica

“…In addition to the antimicrobial screening of the compounds and extracts, their anti-pathogenic potential was checked by examining their antiquorum-sensing activity against Chromobacterium violaceum in LB agar medium as described previously (El-Gohary and Shaaban [12].…”

Microwave‐Assisted Multicomponent Reaction: A Green and Catalyst‐Free Method for the Synthesis of Poly‐Functionalized 1,4‐Dihydropyridines

“…A widespread and diversity of nitrogen heterocyclic molecules have been prepared and applied in the fields of medicinal, agro and combinatorial chemistry . Pyridines and their derivatives are a significant class of heterocyclic molecules which reveals a wide variety of promising biological activities such as anticancer, anti‐Inflammatory, antimalarial, anti‐oxidant, anti‐mycobacterial, antiviral, anti‐leishmanial, anti‐microbial, anti‐tubercular, anti‐proliferative and anti‐ulcer agents . Due to their feasible and scientific importance, various methods have been described in the literature for the preparation of several pyridine moieties.…”