Dengue (DENV) and Zika (ZIKV) viruses are important human pathogens, causing ∼100 million symptomatic infections each year. These infections carry a 20-fold increased incidence of serious neurological diseases, such as microcephaly in newborns (for ZIKV) and Guillain-Barré syndrome. Moreover, DENV can develop serious and possibly life-threatening dengue hemorrhagic fever in certain patients. Patients recovered from one of the four serotypes of DENV are still susceptible to other serotypes with a higher likelihood of serious disease because of antibody-dependent enhancement. Except for mosquito control, there have been no antiviral drugs to prevent and treat ZIKV/DENV infections. Phenotypic screening found that 2,3,6-trisubstituted quinazolinone compounds are novel inhibitors of ZIKV replication. Fifty-four analogues were synthesized, and their structure-activity relationships are discussed. Additional testing shows that compounds 22, 27, and 47 exhibited broad and potent activities against ZIKV and DENV with EC₅₀ values as low as 86 nM with no significant cytotoxicity to mammalian cells.

Journal of Medicinal Chemistry

Quinazolinone Compounds Have Potent Antiviral Activity against Zika and Dengue Virus

Author: Song, Yongcheng ; Yao, Yuan ; Moku, Bala Krishna ; Li, Xin ; Ashraf-Uz-Zaman, Md ; Mishra, Chandra Bhushan

Dengue (DENV) and Zika (ZIKV) viruses are important human pathogens, causing ~100 million symptomatic infections each year.These infections carry a 20-fold increased incidence of serious neurol. diseases, such as microcephaly in newborns (for ZIKV) and Guillain-Barre syndrome.Moreover, DENV can develop serious and possibly life-threatening dengue hemorrhagic fever in certain patients.Patients recovered from one of the four serotypes of DENV are still susceptible to other serotypes with a higher likelihood of serious disease because of antibody-dependent enhancement.Except for mosquito control, there have been no antiviral drugs to prevent and treat ZIKV/DENV infections.Phenotypic screening found that 2,3,6-trisubstituted quinazolinone compounds are novel inhibitors of ZIKV replication.Fifty-four analogs were synthesized, and their structure-activity relationships are discussed.Addnl. testing shows that compounds 22, 27, and 47 exhibited broad and potent activities against ZIKV and DENV with EC₅₀ values as low as 86 nM with no significant cytotoxicity to mammalian cells.

100 Deals associated with Virus replication inhibitors(Baylor College of Medicine)

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Indication	Highest Phase	Country/Location	Organization	Date
Dengue	Preclinical	United States	Baylor College of Medicine	28 Jul 2023
Zika Virus Infection	Preclinical	United States	Baylor College of Medicine	28 Jul 2023

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Virus replication inhibitors(Baylor College of Medicine)

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