Nitroimidazole derivative, preparation method and applications thereof
The invention relates to a nitroimidazole derivative, a preparation method and applications thereof, wherein specifically the compound has a structure represented by a formula I, and various groups and various substituents are defined in the specification. The invention further discloses a preparation method of the compound and applications of the compound in prevention, relieve and/or treatment of diseases caused by anaerobic bacteria infection.
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Paragraph 0139-0141; 0147-0151
(2020/02/29)
High selectivity and high purity method of preparing morpholine
The present invention discloses a high selectivity and high purity method for preparing morinidazole. Specifically, the invention relates to a preparation method of an antimicrobial drug morinidazole (1-[3-(4-morpholinyl)-2-hydroxypropyl] 2-methyl-5-nitro-1H-imidazole). The method is by successively conducting ring opening, salt formation, dissociation and recrystallization on 1-(2,3-epoxypropyl)-2-methyl-5-nitroimidazole to obtain the morinidazole. The method disclosed by the invention ca n prepare morinidazole in a high selectivity and high purity way.
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Paragraph 0037
(2017/08/25)
2-Methyl-4/5-nitroimidazole derivatives potentiated against sexually transmitted Trichomonas: Design, synthesis, biology and 3D-QSAR study
Trichomoniasis is the most prevalent, non-viral sexually transmitted diseases (STD) caused by amitochondriate protozoan Trichomonas vaginalis. Increased resistance of T.?vaginalis to the marketed drug Metronidazole necessitates the development of newer chemical entities. A library of sixty 2-methyl-4/5-nitroimidazole derivatives was synthesized via nucleophilic ring opening reaction of epoxide and the efficacies against drug-susceptible and -resistant Trichomonas vaginalis were evaluated. All the molecules except two were found to be active against both susceptible and resistant strains with MICs ranging 8.55–336.70?μM and 28.80–1445.08?μM, respectively. Most of the compounds were remarkably more effective than the standard Metronidazole. This study analyzes the in?vitro and in?vivo activities of the new 5-nitroimidazoles, which were found to be safe against human cervical HeLa cells with good selectivity index. The exploration of SAR by the synthesis of four different prototypes and 3D-QSAR study has shown the importance of prototype 1 over other prototypes.
Mandalapu, Dhanaraju,Kushwaha, Bhavana,Gupta, Sonal,Singh, Nidhi,Shukla, Mahendra,Kumar, Jitendra,Tanpula, Dilip K.,Sankhwar, Satya N.,Maikhuri, Jagdamba P.,Siddiqi, Mohammad I.,Lal, Jawahar,Gupta, Gopal,Sharma, Vishnu L.
p. 820 - 839
(2016/09/23)
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