European journal of medicinal chemistry · 2026
Discovery and evaluation of a 4-(benzothiazol-2-yl)-N-substituted aniline scaffold as MERS-CoV inhibitors.
СтатьяНазвание и аннотация: Перевод в очереди
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Dai Kaili, Zhang Xiaomeng, Dai Jun, Hu Minqi, Ren Jinjin, Hu Dandan, Tang Jie, Feng Chunlan, Wang Fan, Liu Yi, Li Suxiang, Liu Ting, Hong Ye, Yu Lifang, Yang Fan, Tang Wei
Аннотация
Highly pathogenic coronaviruses pose a serious health threat. However, currently available small-molecule inhibitors (SMIs) targeting the Middle East Respiratory Syndrome Coronavirus (MERS-CoV) spike (S) protein generally lack potency. Here, we design and synthesize a novel class of 4-(benzothiazol-2-yl)-N-substituted aniline derivatives. Distinct from most SMIs targeting viral enzymes, compound 22 potently inhibited both MERS-CoV pseudotyped and live viruses in vitro, with surface plasmon resonance (SPR) providing evidence for a direct interaction with the S protein. Alongside good solubility and metabolic stability, compound 22 exhibited in vivo proof-of-concept efficacy in hDPP4-transgenic mice by significantly reducing pulmonary viral loads. Overall, this study validates the 4-(benzothiazol-2-yl)-N-substituted aniline scaffold as an early anti-MERS-CoV pre-lead series, with compound 22 as a solid starting point for further optimization.