The thiourea based 4-amino-1,8-naphthalimide molecules 1-5 were designed as fluorescent anion sensors and their photophysical properties investigated upon recognition of biologically relevant anions such as acetate, dihydrogen phosphate and fluoride in DMSO. Synthesised in a single step from their respective aniline precursors, 6-9, these molecules were designed on the fluorophore-spacer-recept...

Heteroarotinoids (Hets) are a novel class of heterocycles which contain an aryl ring and a heterocylic ring and which show potential as anticancer drugs [1]. These heteroarotinoids control cell growth, differentiation, and apoptosis of the cancer cells. Heteroarotinoids were originally derived from an arotinoid class related to retinoids by strategically placing a heteroatom (O,N,S) in the mole...

An efficient and odourless procedure for a one-pot synthesis of thioesters by the reaction of benzoic anhydrides, thiourea and various organic halides (primary, allylic, and benzylic) or structurally diverse, electron-deficient alkenes (ketones, esters, and nitriles) in the presence of Et3N has been developed. In this method, thiobenzoic acids were in situ generated from the reaction of thioure...

Dihydropyrazines (DHPs), which break DNA strands and exhibit several other biological activities by generating radical species and high chemical reactivity as shown in our previous papers, reacted with thiourea to give tetraazaindene derivatives which were new compounds, even though thiourea is scavenges radicals. These derivatives can break DNA strands and inhibit the growth of Escherichia col...

With poor (low) solubility in the aquatic environment, highly toxic drugs (aspirin, doxorubicin, daunorubicin, sulfonamides and others), a low level of glycyrrhizic acid (HA) leads to decrease toxicity increases their biological activity due water. The stability constants (stability) value Gibbs energy synthesized supramolecular complex have been calculated, theoretical experimental research me...

The catalytic activity of racemic thiourea derivatives of Tröger’s base (±)-2–4 in Michael additions of malonate derivatives to trans-β-nitrostyrene was studied. Due to the low basicity of Tröger’s base, the outcome of the addition reactions was strongly dependent on the pKa of the nucleophile. Thiourea catalysts (±)-2, 3 were resolved on the chiral stationary phase Whelk O1. Unfortunately, ena...

Deuterium isotope effects were evaluated as a strategy to optimize the pharmacokinetics of 7-(3,5-dimethyl-1H-1,2,4-triazol-1-yl)-3-(4methoxy-2-methylphenyl)-2,6-dimethylpyrazolo[5,1-b]oxazole (NVSCRF38), a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist. In an attempt to suppress O-demethylation of NVSCRF38 without losing activity against the CRF1 receptor, the protons at the...

A series of new 4-(5-(3-cyano-4-isobutoxyphenyl)-4-methylthiazole-2-carbonyl)-N-(substituted phenyl)piperazine-1-carboxamides 8(a-e)/carbothioamides 8(f-j) were accomplished for biological interest by the simple addition of active functionalized arylisocyanates 7(a-e)/arylisothiocyanates 7(f-j) with 2-isobutoxy-5-(4-methyl-2-(piperazine-1-carbonyl)thiazol-5-yl)benzonitrile (4). Compound 4 was s...

Thiourea is the parent compound of a group of compounds known t.o have goitrogenic activity. These substances prevent the formation of organically bound iodine from iodide ion (l-6), but the mechanism of this action is unknown. ‘Paper I of this series (7) showed that when thiourea labeled with radioactive sulfur was administered to rats the concentration of radioactivity in the thyroid gland 24...