title: Pharmaceutical importance and synthetic strategies for imidazolidine-2-thione and imidazole-2-thione derivatives.
abstract: Imidazole heterocycles containing oxygen or sulfur heteroatoms are of considerable pharmaceutical interest. Many synthetic strategies for imidazolidine-2-thione and imidazole-2-thione derivatives were developed in the past years. They have been well documented by a steadily increasing number of publications and patents. Substituted imidazolidine-2-thiones and imidazole-2-thiones display remarkable biological activities. For instance, imidazole-2-thione has been reported to exhibit antimicrobial, antifungal, antithyroid, antioxidant, cardiotonic, antihypertensive, Dopamine beta-Hydroxylase (DBH) inhibitory and anti-HIV properties. Imidazolidine-2-thione derivatives have been reported to exhibit antimicrobial activity, anti-HIV activity, antifungal activity and so forth. The main purpose of this review is to present a survey of the literature on the different methods of synthesis and reactions involving imidazolidine-2-thione and imidazole-2-thione during the last few decades. This article summarizes an efficient, microwave-assisted method for the liquid-phase combinatorial synthesis of 3,5-disubstituted-thiohydantoin, also reported previously. Synthesis of metal complexes of imidazolidine-2-thione and its derivatives were reported as antimicrobial agents also discussed in the article. Some of the chiral imidazolidine-2-thione N-and C-nucleoside were reported as precursors for the synthesis of azidonucleosides and fluoronucleosides known for their anti-AIDS activity. Metal complexes of heterocyclic thione ligands were reported to possess antifungal activity. Imidazolidine-2-thione and imidazole-2-thione derivatives have found applications in diverse therapeutic areas. Imidazolidine-2-thiones are also used as a chiral auxiliary and ligand for asymmetric catalysis.
authors.affiliation: Department of Pharmaceutical Chemistry, Institute of Pharmacy, Nirma University, Ahmedabad, Gujarat, India.
authors.forename: Jignasa K
authors.initials: JK
authors.lastname: Savjani
authors.forename: Anuradha K
authors.initials: AK
authors.lastname: Gajjar
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry; D005031:Ethylenethiourea; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry*; D048289:Imidazolidines / Q000138:chemical synthesis* / Q000737:chemistry*; D008872:Microwaves; D015394:Molecular Structure; D004364:Pharmaceutical Preparations / Q000138:chemical synthesis* / Q000737:chemistry*; D013871:Thiones / Q000138:chemical synthesis* / Q000737:chemistry*
chemical_list: D019380:Anti-HIV Agents; D007093:Imidazoles; D048289:Imidazolidines; D004364:Pharmaceutical Preparations; D013871:Thiones; D005031:Ethylenethiourea