Abstract
The modern world has no available drugs for the treatment of enteroviruses (EV), which affect millions of people worldwide each year. The EV71 is a major causative disease for hand, foot, and mouth disease; sometimes it is associated with severe central nervous system diseases. Treatment for enteroviral infection is mainly supportive; treatment for aseptic meningitis caused by enteroviruses is also generally symptomatic. Upon the urgent request of new anti-enterovirus drugs, a series of hinged aromatic compounds with polynulei were synthesized through two different chemical pathways. Among these morpholine–furan/thiophene/pyrrole–benzene–pyrazole conjugates, three new agents exhibited inhibitory activity with EC50 = 2.29–6.16 μM toward EV71 strain BrCr in RD cells. Their selectivity index values were reached as high as 33.4. Their structure–activity relationship was deduced that a thiophene derivative with morpholine and trifluorobenzene rings showed the greatest antiviral activity, with EC50 = 2.29 μM.
Highlights
Millions of people worldwide each year are affected by enteroviruses (EV), which are often found in the respiratory secretions and stools of an infected person [1]
EV71 target, target, the the hinged hingedfuran–benzene–pyrazole furan–benzene–pyrazole conjugate conjugate shown shown of below was found with potency of. We considered it as a hit molecule and, below was found with potency of EC50 = 11.6 μM. We considered it as a hit molecule and, designed and and synthesized synthesizedaaseries seriesofofhinged hingedheterocycle–benzene–pyrazole heterocycle–benzene–pyrazoleconjugated conjugatedcompounds compounds designed
After removal of the silyl group by n-tetrabutylammonium flouride (TBAF), the resultant ester 7 was saponificated with aqueous LiOH in THF to afford heterotricycle 8 in 78% yield
Summary
Millions of people worldwide each year are affected by enteroviruses (EV), which are often found in the respiratory secretions and stools of an infected person [1]. These viruses cause blurred vision, encephalitis, pericarditis, rashes, and summer colds. Enteroviruses are by far the most common causes of aseptic meningitis in children. There are 64 non-polio EV that can cause disease in humans [2]. Infection can result in a wide variety of symptoms, including acute flaccid paralysis, acute hemorrhagic conjunctivitis, aseptic meningitis, hand/foot/mouth disease, myocarditis, neonatal sepsis-like disease, respiratory illness (common cold) [1]. Enterovirus 71 is notorious and associated with severe central nervous system diseases [3]
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