Bioorganic & medicinal chemistry letters · 2014
Design and synthesis of substituted morpholin/piperidin-1-yl-carbamodithioates as promising vaginal microbicides with spermicidal potential.
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Bala Veenu, Jangir Santosh, Kumar Vikas, Mandalapu Dhanaraju, Gupta Sonal, Kumar Lalit, Kushwaha Bhavana, Chhonker Yashpal S, Krishna Atul, Maikhuri Jagdamba P, Shukla Praveen K, Bhatta Rabi S, Gupta Gopal, Sharma Vishnu L
Аннотация
A series of seventeen morpholin/piperidin-1-yl-carbamodithioate (3-19) were synthesized as topical vaginal microbicidal spermicides. The synthesized compounds were evaluated for their anti-Trichomonas activity against MTZ susceptible and resistant strains along with their spermicidal and antifungal potential. All the synthesized compounds were assessed for their safety through cytotoxic assay against human cervical cell line (HeLa) and compatibility with vaginal flora, Lactobacillus. The study identified eleven dually active compounds with apparent safety. The plausible mode of action of these compounds was through sulfhydryl binding, confirmed via reduction in available free thiols on human sperm. The most promising compound 9 significantly inhibited (P<0.001) thiol-sensitive sperm hexokinase. The stability of compound 9 in simulated vaginal fluid (SVF) was performed via HPLC-PDA method, which supported its utility for vaginal administration.