4122-79-6

Upstream product

• 109-01-3 1-methyl-piperazine 
• 106-89-8 epichlorohydrin 

Downstream Products

• 101932-30-3 5-<4-Methyl-piperazinomethyl>-3-<5-nitro-furfurylidenamino>-oxazolid-2-on 
• 1092361-82-4 C₂₆H₃₄F₃N₃O₂S₂ 
• 412308-64-6 3-Amino-5-<4-methyl-piperazinomethyl>-oxazolid-2-on 

Relevant academic research and scientific papers

Innovative Disulfide Esters of Dithiocarbamic Acid as Women-Controlled Contraceptive Microbicides: A Bioisosterism Approach

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.

2-Amino-2-oxazolines, V: Synthesis of some 5-dialkylaminomethyl-2-amino-2-oxazolines and evaluation of their diuretic activity.

A series of 5-dialkylaminomethyl-2-amino-2-oxazolines was prepared and screened for diuretic activity. These compounds were previously examined for their lipophilic behaviour using a reversed-phase HPLC technique. The capacity factors, expressed as log k'w, were correlated with the partition coefficient log P. A QSAR analysis of the diuretic activity in relation with the lipophilicity was attempted for these structurally related compounds.