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Design and synthesis of substituted morpholin/piperidin-1-yl-carbamodithioates as promising vaginal microbicides with spermicidal potential

Authors :
Praveen K. Shukla
Vikas Kumar
Veenu Bala
Gopal Gupta
Dhanaraju Mandalapu
Sonal Gupta
Rabi Sankar Bhatta
Santosh Jangir
Yashpal S. Chhonker
Lalit Kumar
Vishnu L. Sharma
Jagdamba P. Maikhuri
Bhavana Kushwaha
Atul Krishna
Source :
Bioorganic & Medicinal Chemistry Letters. 24:5782-5786
Publication Year :
2014
Publisher :
Elsevier BV, 2014.

Abstract

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

Details

ISSN :
0960894X
Volume :
24
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....4a405e827459e1209fb5466963ed99d0
Full Text :
https://doi.org/10.1016/j.bmcl.2014.10.040