Synthesis, anti-inflammatory activity, inverse molecular docking, and acid dissociation constants of new naphthoquinone-thiazole hybrids.

Chronic Inflammation is associated with various types of diseases that involves pro-inflammatory cytokines like IL-6 and TNF-α. High costs and serious side effects of available anti-inflammatory/immunomodulatory drugs led us to design new compounds with promising anti-inflammatory activities. Many drugs and biologically important compounds involve naphthoquinone and thiazole moieties in their core structures.

Potentiometric Study of the Dissociation and the Metal Complex-formation Competence of 5-(3,3-dimethyl-1-triazeno)-imidazole-4-carboxamide (Dacarbazine).

A potentiometric investigation has been carried out to disclose the coordination properties of Dacarbazine, 5-(3,3-dimethyl-1-triazeno)-imidazole-4-carboxamide (abbreviated DTIC) with particular transition metal ions (Zn2+, Cu2+, Ni2+ and Co2+). The coordination of DTIC with these metal ions results in several complexes emerging in solution. The aim of this work is to determine the protonation constants of the DTIC and to show the extent of its coordination with (Zn2+, Cu2+, Ni2+ and Co2+), in other words, establish the stability of the complexes formed between the DTIC and these metal ions by the determination of their stability constants.

Synthesis, biological properties, and acid dissociation constant of novel naphthoquinone-triazole hybrids.

A series of novel 1,4-naphthoquinone-triazole hybrids, N-(3-amino-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-2-(4-R-1H-1,2,3-triazol-1-yl)acetamide, was synthesized by click chemistry in the presence of sodium ascorbate and copper(II) sulfate pentahydrate in 81-94% yield. Various biological properties of the synthesized compounds including DNA binding/cleavage, antioxidant, antibacterial and antifungal properties were evaluated. The DNA binding study was performed using dsDNA and G-quadruplex DNA.

Synthesis, antimicrobial activity and acid dissociation constants of methyl 5,5-diphenyl-1-(thiazol-2-yl)pyrrolidine-2-carboxylate derivatives.

In this study, a series of polysubstituted methyl 5,5-diphenyl-1-(thiazol-2-yl)pyrrolidine-2-carboxylate derivatives were designed and synthesized by the cyclization reaction of methyl 1-(benzoylcarbamothioyl)-5,5-diphenylpyrrolidine-2-carboxylates and 2-bromo-1-(4-substituted phenyl)ethanones in 70-96% yield. The starting pyrrolidine derivatives were synthesized via a 1,3-dipolar cycloaddition reaction in 83-88% yield. The stereochemistry of one of these methyl 5,5-diphenyl-1-(thiazol-2-yl)pyrrolidine-2-carboxylate derivatives was characterized by a single crystal X-ray diffraction study and the acid dissociation constants of these compounds were determined.

Determination of Acid Dissociation Constants (pK a ) of Bicyclic Thiohydantoin-Pyrrolidine Compounds in 20% Ethanol-Water Hydroorganic Solvent.

The acid dissociation constants of potential bioactive fused ring thiohydantoin-pyrrolidine compounds were determined by potentiometric titration in 20% (v/v) ethanol-water mixed at 25 ± 0.1°C, at an ionic background of 0.1 mol/L of NaCl using the HYPERQUAD computer program.

Determination of Equilibrium Constants of Some Novel Antioxidant Compounds and Study on their Complexes with Some Divalent Metal ions in Ethanol-water Mixed.

This study aims to investigate the nature and type of complexes formed in solution, between novel antioxidant compounds [P1(4-(1-(3-hydroxy-4-methoxyphenyl)propyl)benzene-1,2-diol) and P2(4-(1-(3-hydroxy-4-methoxyphenyl)propyl)benzene-1,3-diol)] and the ions Cu2+, Ni2+, Zn2+ and Co2+. Potentiometric titration technique was used to follow the formation of complexes during the course of coordination. The stability of the complexes formed was controlled through the determination of stability constants in aqueous ethanol solution at 25 ± 0.