A Ni-catalyzed C-S bond forming reaction has been developed for the synthesis of 2-aminobenzothiazole by the coupling of 2-haloanilines (-bromo and -iodo) with isothiocyanates. The key advantages of this procedure are ligand-free condition, inexpensive catalyst, high yields, and simple purification of the products by nonchromatographic technique.

In the reaction of hydrazide of thiophene-2-acetic acid (1) with isothiocyanates, the respective thiosemicarbazides 2a-g were obtained. Further cyclization with 2% NaOH led to formation of 4-substituted-3-(thiophene- 2-yl-methyl)-Delta2-1,2,4-triazoline-5-thiones (3a-g). These compounds showed promising antimycotic activity.

Diastereoselective syntheses of 3-aryl-(S/R)-6-methyl-1-[(S/R)-1-phenylethyl)]-2-thioxotetrahydro pyrimidin-4(1H)-ones were achieved in good yields by the condensation of aryl isothiocyanates with ethyl 3-(1-phenylethylamino)butanoate in a one-pot reaction. Benzylation of these substrates illustrated that the orientations of the exocylic and endocylic groups determine the stereochemical outcome...

Acyl isothiocyanates and their functional derivatives (acyl thioureas acyl thiosemicarbazides) are an important group of organic compounds that widely used in the synthesis heterocycles chemistry as catalysts, ligands, colorimetric hemosensors, etc. In recent years, there has been increased interest towards this class promising biologically active compounds, especially since latest advances med...

A blockwise iterative synthetic strategy for the preparation of linear, dendritic and branched full-carbohydrate architectures has been developed by using sugar azido(carbamate) isothiocyanates as key templates; the presence of intersaccharide thiourea bridges provides anchoring points for hydrogen bond-directed molecular recognition of phosphate esters in water.

Two aromatic isothiocyanates, derived from isoindoline nitroxides, were synthesized and selectively reacted with 2'-amino groups in RNA. The spin labels displayed limited mobility in RNA, making them promising candidates for distance measurements by pulsed EPR. After conjugation to RNA, a tetraethyl isoindoline derivative showed significant stability under reducing conditions.

Sulforaphane (SFN) and moringin (GMG-ITC) are edible isothiocyanates present as glucosinolate precursors in cruciferous vegetables and in the plant Moringa oleifera respectively, and recognized for their chemopreventive and medicinal properties. In contrast to the well-studied SFN, little is known about the molecular pathways targeted by GMG-ITC. We investigated the ability of GMG-ITC to inhibi...

BACKGROUND Essential oils are often used in alternative medicine as analgesic and anti-inflammatory remedies. However, the specific compounds that confer the effects of essential oils and the molecular mechanisms are largely unknown. TRPM8 is a thermosensitive receptor that detects cool temperatures and menthol whereas TRPA1 is a sensor of noxious cold. Ideally, an effective analgesic compound ...

Natural isothiocyanates, present in cruciferous vegetables and synthetic phenylhexyl isothiocyanate (PHI) are chemopreventive agents which act by blocking the initiation of carcinogen-induced tumors in rodents. We have demonstrated that isothiocyanates are also growth regulators, inhibiting cell cycle cdk activity and up-regulating inhibitor p21WAF1 (p21) in cancer cells. The up-stream mechanis...

BACKGROUND Tropaeolum pentaphyllum Lam. tubers (Tropaeolaceae) are known and used as a condiment and for the treatment of skin infections in Southern Brazil. However, its activity and composition has not yet been investigated. Thus, different extracts and the essential oil from the tubers were tested against a range of microorganisms. The most active extracts were submitted to chromatographic a...