New therapies on the horizon: Targeted protein degradation in neuroscience

Gregory, James A.; Hickey, Christopher M.; Chavez, Juan; Cacace, Angela M.

doi:10.1016/j.chembiol.2024.08.010

Cell Chemical Biology

2024

DOI: 10.1016/j.chembiol.2024.08.010

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New therapies on the horizon: Targeted protein degradation in neuroscience

James A. Gregory,

Christopher M. Hickey,

Juan Chavez

et al.

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Cited by 1 publication

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Synthesis and Antimicrobial Evaluation of New 1,2,4-Triazolo[1,5-a]pyrimidine-Based Derivatives as Dual Inhibitors of Bacterial DNA Gyrase and DHFR

Al-Wahaibi,

Rabea,

Mahmoud

et al. 2024

ACS Omega

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A series of 1,2,4-triazolo [1,5-a]pyrimidine-based derivatives were developed and prepared by reacting chalcones 8a−p with 3-phenyl-1,2,4-triazole-5-amine (5). The novel compounds were analyzed using several spectroscopic techniques, and their antimicrobial efficacies against six pathogens (Gramnegative, Gram-positive, and fungi) were tested. Most of the tested compounds exhibited significant antimicrobial activity compared to ciprofloxacin and fluconazole. Four compounds (9d, 9n, 9o, and 9p) showed promising results. Their minimal inhibitory concentration (MIC) values were between 16 and 102 μM, similar to ciprofloxacin's 10−90 μM values. MIC values against the tested fungal species were between 15.50 and 26.30 μM, higher than fluconazole's 11.50−17.50 μM values. Compounds 9n and 9o, in particular, showed excellent bactericidal activity. Compounds 9n and 9o, the most effective antibacterial agents, were further evaluated for their inhibitory effects on bacterial DNA gyrase and DHFR enzymes as possible molecular targets. The results indicated that 9n and 9o demonstrated a similar level of activity against DNA gyrase and DHFR when compared to the reference drugs ciprofloxacin and trimethoprim. We conducted molecular docking to investigate the binding mechanism and evaluate the reactivity of the intriguing compounds. Compounds 9n and 9o demonstrated favorable binding interactions with the essential amino acids necessary for the inhibition of E. coli DNA gyrase and DHFR enzymes.

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Synthesis and Antimicrobial Evaluation of New 1,2,4-Triazolo[1,5-a]pyrimidine-Based Derivatives as Dual Inhibitors of Bacterial DNA Gyrase and DHFR

Al-Wahaibi,

Rabea,

Mahmoud

et al. 2024

ACS Omega

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New therapies on the horizon: Targeted protein degradation in neuroscience

Cited by 1 publication

References 88 publications

Synthesis and Antimicrobial Evaluation of New 1,2,4-Triazolo[1,5-a]pyrimidine-Based Derivatives as Dual Inhibitors of Bacterial DNA Gyrase and DHFR

Synthesis and Antimicrobial Evaluation of New 1,2,4-Triazolo[1,5-a]pyrimidine-Based Derivatives as Dual Inhibitors of Bacterial DNA Gyrase and DHFR

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