CAS: 22162-15-8; (2-Methyl-4-Nitrophenyl)Methanol

上下游产品

1-(bromomethyl)-2-methyl-4-nitrobenzene 2-methyl-4-nitrobenzoic acid 4-nitro-o-xylene2-methyl-4-nitro-benzaldehyde Methyl 4-[N-methyl-N-(2-methyl-4-nitrobenzyloxycarbonyl)amino]phenylacetate 4-[N-Methyl-N-(2-methyl-4-nitrobenzyloxycarbonyl)amino]phenylacetic acid N-[2-(N,N-Dimethylamino)ethyl] 4-[N-methyl-N-(2-methyl-4-nitrobenzyloxycarbonyl)amino]phenylacetamide

4-硝基邻二甲苯置于sodium Hydroxide,N-溴代丁二酰亚胺(Nbs),偶氮二异丁腈,溶剂黄146体系中,用 甲醇,乙酸乙酯 用作溶剂,化学反应 36.5H,反应生成2-甲基-4-硝基苄醇
参考文献:口服活性ccr5拮抗剂,作为抗hiv-1药物2:含有吡啶n-氧化物部分的苯胺衍生物的合成和生物活性.
标题:口服活性ccr5拮抗剂,作为抗hiv-1药物2:含有吡啶n-氧化物部分的苯胺衍生物的合成和生物活性.
摘要:为了开发口服活性ccr5拮抗剂,我们研究了含有新的极性取代基(例如膦酸酯,氧化膦或吡啶n-氧化物部分)的1-苯并benzo庚因衍生物,以取代先前报道的季铵部分.在这些化合物中,2-(α-羟基苄基)吡啶n-氧化物5E在大鼠中表现出中等的ccr5拮抗活性并具有可接受的药代动力学特征.随后进行了化学修饰,发现具有(S)-构型羟基的化合物(S)-5F比(R)-异构体更具活性.用具有4-[2-(丁氧基)乙氧基]苯基的1-苯并ze庚因环替换具有4-甲基苯基的1-苯并x庚因环增强了结合测定中的活性.此外,在苯胺部分的苯基上引入3-三氟甲基导致hiv-1包膜介导的膜融合测定的活性大大提高.特别是,化合物(S)-5S在融合试验中显示出最强的ccr5拮抗活性(ic(50)= 7.2 Nm)和抑制作用(ic(50)= 5.4 Nm),并且在大鼠中具有非常好的药代动力学特性.
Doi:10.1248/cpb.52.818

专利信息

专利号:US-12275686-B2
优先权日:2022-02-22
标 题 :NO donor compound, preparation method thereof, pharmaceutical composition comprising same, and use thereof
发明人：GOU SHAOHUA; YANG WANXIANG
权利人:UNIV SOUTHEAST
摘要:Disclosed is NO donor compound and preparation method, pharmaceutical composition, and use. The compound has a structure represented by formula The NO donor compound and the pharmaceutical composition thereof, as hypoxia-activated NO donors, may be prepared as drugs for treating myocardial hypoxic damage disease. The prepared drugs can exert efficacy at both the cellular level and the animal level, and the synthesis method of the compound is simple and easy to operate.