Organometallic Derivatives of Decoquinate Targeted toward <i>Toxoplasma gondii</i>

نویسندگان

چکیده

Toxoplasmosis is an infection contracted by exposure to Toxoplasma gondii and can have deleterious health effects on pregnant women their children. Current treatments for the are complex considerable undesired side effects, raising need new treatments. Herein, we report synthesis, characterization, biological testing of some organometallic derivatives commercially available, broad-spectrum antiparasitic, decoquinate (DCQ). The cyclic secondary amine was functionalized with a range groups (i.e., ferrocene, ruthenocene, phenyl) either methyl or vinyl bridges. Through measurement half maximal inhibitory concentrations (IC50) T. proliferation assays, it found that ferrocenylvinyl-DCQ oxygen-alkylated phenylvinyl-DCQ product reduced parasite 84% at 1 μM, which approached parent drug (96%). These data provide possible roadmap future investigations derivatization DCQ yield better toxoplasmosis, particularly functionalization ketone.

برای دانلود رایگان متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Organometallic cobalamin anticancer derivatives for targeted prodrug delivery via transcobalamin-mediated uptake.

Herein we report the synthesis of new water-soluble vitamin B12 prodrugs bearing metal complexes at the β-upper side of the cobalt center. A total of three derivatives with the general design {Co-C[triple bond, length as m-dash]C-bpy-M}, where M represents a cytotoxic metal complex, were prepared and tested for their cytotoxicity against MCF-7 breast cancer cells. The choice of the metal was or...

متن کامل

Anodic properties of diarylethene derivatives having organometallic piano-stool tags.

The half-sandwich tamoxifen derivative, Mn(CO)(3)(η(5)-C(5)H(4)(Et)C=C(C(6)H(5))(2)), gives a radical cation which is charge-delocalized between the "cymantrenyl" and diphenylethene moieties and undergoes facile metal-carbonyl substitution reactions. Mn and Re complexes with finely tuned redox potentials can be obtained for cancer cell inhibition studies.

متن کامل

Novel harmine derivatives for tumor targeted therapy

Harmine is a beta-carboline alkaloid found in medicinal plant PeganumHarmala, which has served as a folk anticancer medicine. However, clinical applications of harmine were limited by its low pharmacological effects and noticeable neurotoxicity. In this study, we modified harmine to increase the therapeutic efficacy and to decrease the systemic toxicity. Specifically, two tumor targeting harmin...

متن کامل

the foreign policy of russia toward caucasus 2000-2008

after the soviet union dissolution, a chaotic period was begun in the russia. russia lost its glory and felt disgrace. the first group of elites came to power under yeltsin; they tried to re-define russia’s identity as a european country and build a foreign policy on this baseline. therefore russia tried to become closer with the west especially with the u.s. according to their view the sovie...

15 صفحه اول

Application of fundamental organometallic chemistry to the development of a gold-catalyzed synthesis of sulfinate derivatives.

The development of a gold(I)-catalyzed sulfination of aryl boronic acids is described. This transformation proceeds through an unprecedented mechanism which exploits the reactivity of gold(I)-heteroatom bonds to form sulfinate anions. Further in situ elaboration of the sulfinate intermediates leads to the corresponding sulfones and sulfonamides, two pharmacophores routinely encountered in drug ...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

ژورنال

عنوان ژورنال: Organometallics

سال: 2022

ISSN: ['1520-6041', '0276-7333']

DOI: https://doi.org/10.1021/acs.organomet.2c00204