6270-19-5Relevant articles and documents
Preparation method of 3-hydrazino-5-morpholinomethyl-2-oxazolidinone
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Paragraph 0093; 0096, (2020/07/12)
The invention provides a preparation method of 3-hydrazino-5-morpholinomethyl-2-oxazolidinone, and belongs to the technical field of chemical synthesis. The preparation method comprises the followingsteps: carrying out a cyclization reaction on 1-Boc protective hydrazine-3-morpholine-2-propanol and a carbonic ester substance to obtain 3-Boc protective hydrazine-5-morpholinomethyl-2-oxazolidinone;and finally hydrolyzing to obtain the AMOZ. The chemical structural formula of the 1-Boc protective hydrazine-3-morpholine-2-propanol is shown in the specification, the chemical structural formula ofthe 3-Boc protective hydrazine-5-morpholinomethyl-2-oxazolidinone is shown in the specification, and the chemical structural formula of the AMOZ is shown in the specification; and the carbonic estersubstance contains at least one of diethyl carbonate, dimethyl carbonate, di-tert-butyl decarbonate, and dipropyl carbonate. The method is simple in synthetic route, the AMOZ is synthesized by adopting a one-pot method, and the catalyst is used in the preparation process, so that the loss in the synthesis process is greatly reduced, the synthesis yield and the recovery rate are relatively high; and the method is suitable for mass production.
Innovative Disulfide Esters of Dithiocarbamic Acid as Women-Controlled Contraceptive Microbicides: A Bioisosterism Approach
Mandalapu, Dhanaraju,Lal, Nand,Kumar, Lokesh,Kushwaha, Bhavana,Gupta, Sonal,Kumar, Lalit,Bala, Veenu,Yadav, Santosh K.,Singh, Pratiksha,Singh, Nidhi,Maikhuri, Jagdamba P.,Sankhwar, Satya N.,Shukla, Praveen K.,Siddiqi, Imran,Gupta, Gopal,Sharma, Vishnu L.
, p. 1739 - 1753 (2015/10/06)
In an ongoing effort to discover an effective, topical, dual-function, non-surfactant contraceptive vaginal microbicide, a novel series of 2,2′-disulfanediylbis(3-(substituted-1-yl)propane-2,1-diyl) disubstituted-1-carbodithioates were designed by using a bioisosterism approach. Thirty-three compounds were synthesized, and interestingly, most demonstrated multiple activities: they were found to be spermicidal at a minimal effective concentration of 1-0.001 %, trichomonacidal against drug-susceptible and resistant Trichomonas strains at minimal inhibitory concentration (MIC) ranges of 10.81-377.64 and 10.81-754.14 μM, respectively, and fungicidal at MIC 7.93-86.50 μM. These compounds were also found to be non-cytotoxic to human cervical (HeLa) epithelial cells and vaginal microflora (Lactobacilli) in vitro. The most promising compound, 2,2′-disulfanediylbis(3-(pyrrolidin-1-yl)propane-2,1-diyl)dipyrrolidine-1-carbodithioate (5), exhibited spermicidal activity 15-fold higher than that of the marketed spermicide Nonoxynol-9 (N-9) and also demonstrated microbicidal potency. To identify common structural features required for spermicidal activity, a 3D-QSAR analysis was carried out, as well as in vivo efficacy studies and fluorescent labeling studies to determine the biological targets of compound 5. Change it out: A series of disulfide esters of dithiocarbamic acid were synthesized to block free sulfhydryl groups present in sperm and Trichomonas for a safe dual-action spermicide. A majority of the compounds demonstrated multiple activities with good safety profiles, with the most promising compound exhibiting spermicidal activity 15-fold higher than that of the marketed spermicide Nonoxynol-9.
PYRROLO-NITROGENOUS HETEROCYCLIC DERIVATIES,THE PREPARATION AND THE PHARMCETICAL USE THEEOF
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Page/Page column 75, (2010/04/23)
The invention provides new pyrrolo-nitrogenous heterocyclic derivatives represented by formula (I) or their salts, the preparation thereof, pharmaceutical compositions containing such derivatives and the use of such derivatives as therapeutic agents, especially as protein kinase inhibitors, wherein each substituent in formula (I) is same as defined in the description.