CAS: 41195-90-8; 2,3-Dichlorophenylisocyanate

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CAS号32315-10-9 三光气 | CAS号608-27-5 2,3-二氯苯胺

光气,2,3-二氯苯胺置于三乙胺体系中,用 二氯甲烷,甲苯 作为反应溶剂,化学反应 4.08H,反应生成 2,3-二氯苯基异氰酸酯
参考文献:Phenotypic Optimization Of Urea-thiophene Carboxamides To Yield Potent,Well Tolerated,And Orally Active Protective Agents Against Aminoglycoside-Induced Hearing Loss
标题:Phenotypic Optimization Of Urea-thiophene Carboxamides To Yield Potent,Well Tolerated,And Orally Active Protective Agents Against Aminoglycoside-Induced Hearing Loss
摘要:Hearing Loss Is A Major Public Health Concern With No Pharmaceutical Intervention For Hearing Protection Or Restoration. Using Zebrafish Neuromast Hair Cells,A Robust Model For Mammalian Auditory And Vestibular Hair Cells,We Identified A Ureathiophene Carboxamide,1 (Orc-001),As Protective Against Aminoglycoside Antibiotic (Aga)-Induced Hair Cell Death. The 50% Protection (Hc50) Concentration Conferred By 1 Is 3.2 Mu M With Protection Against 200 Mu M Neomycin Approaching 100%. Compound 1 Was Sufficiently Safe And Drug-Like To Validate Otoprotection In An In Vivo Rat Hearing Loss Model. We Explored The Structureactivity Relationship (Sar) Of This Compound Series To Improve Otoprotective Potency,Improve Pharmacokinetic Properties And Eliminate Off-Target Activity. We Present The Optimization Of 1 To Yield 90 (Orc-13661). Compound 90 Protects Mechanosensory Hair Cells With Hc50 Of 120 Nm And Demonstrates 100% Protection In The Zebrafish Assay And Superior Physiochemical,Pharmacokinetic,And Toxicologic Properties,As Well As Complete In Vivo Protection In Rats.
DOI:10.1021/acs.Jmedchem.7B00932