当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Design, synthesis and biological evaluation of chalconyl blended triazole allied organosilatranes as giardicidal and trichomonacidal agents.

Design, synthesis and biological evaluation of chalconyl blended triazole allied organosilatranes as giardicidal and trichomonacidal agents.

Abstract：

:A series of chalconyl blended triazole allied silatranes (7a-g/8a-g/9a-g) were synthesized in good yields using a simple, economical and biocompatible synthetic route. The blend of three different pharmacologically active moieties into a single scaffold resulted into synergistic effect in their bio-activity. Various substitutions were tried to study the structure activity relationship (SAR) of the synthesized compounds on the basis of biological results. All the newly synthesized compounds were well characterized by IR, (1)H and (13)C NMR, low resolution mass spectroscopy and elemental analysis. The structures of 7a and 7c were authenticated by single crystal X-ray crystallography. These compounds were screened by using Molinspiration software for their physicochemical properties and all the compounds showed good oral bioavailability. The antiparasitic activity of the newly synthesized compounds was evaluated against unicellular parasites (Giardia lamblia and Trichomonas vaginalis) in comparison to standard drug (metronidazole) by 3-(4,5-dimethylthiazol-yl)-diphenyl tetrazolium bromide (MTT) assay. All the compounds displayed significant activity against G. lamblia and T. vaginalis with IC50 values ranging from 19.58-131.2 μM to 18.24-101.26 μM respectively. The entire library of compounds was found to be more active than metronidazole except 9a, 9f and 9g. Notably, 9e and 7e were found to be most significant against G. lamblia and T. vaginalis respectively.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Singh G,Arora A,Mangat SS,Rani S,Kaur H,Goyal K,Sehgal R,Maurya IK,Tewari R,Choquesillo-Lazarte D,Sahoo S,Kaur N

doi

10.1016/j.ejmech.2015.11.029

subject

Has Abstract

pub_date

2016-01-27 00:00:00

pages

287-300

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(15)30366-4

journal_volume

108

pub_type

杂志文章

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