Efforts toward the first total synthesis of a mixed-ligand siderophore: Gobichelin-A.

The synthesis of Gobichelin-A, a naturally occurring mixed-ligand siderophore isolated from Streptomyces sp. NRRL F-4415, is described. The target molecule was planned to be synthesized by a convergent process involving the combination of two halves, Gob-A 1st half and Gob-A 2nd half, at the prefinal stage of the synthetic route. By adopting this method, fully protected Gobichelin-A was synthesized in excellent yield.

Comprehensive review on natural pharmacophore tethered 1,2,3-triazoles as active pharmaceuticals.

The privileged 1,2,3-triazole scaffold is drawing researcher's attention due to its widespread applications in diverse fields such as drug discovery (e.g., carboxyamidotriazole), organic synthesis (click-reaction template), polymeric materials (e.g., triazolamer), supramolecular receptors (e.g., triazolophane), fluorescent materials (e.g., metal-organic frameworks), and agricultural sectors (e.g., fungicides). Various 1,2,3-triazole persuasion modules are also currently available in the market that have multiple assets such as active pharmaceuticals and agricultural purposes. Owed to the highly consistent and firmest synthesis approach, that is, click reaction of various azides and acetylene derivatives by copper (I)-catalyzed 1,3-dipolar cycloaddition (CuAAC), highly functionalized 1,2,3-triazoles are prepared in scalar yields for drug discovery. Given the importance of 1,2,3-triazole chemistry, the present review focuses specifically on the synthesis of structurally diverse 1,2,3-triazoles linked to natural pharmacophores and their biological importance. Furthermore, the dual/multi-pharmacophores assimilated 1,2,3-triazoles have listed interesting biological activities that could be valuable as future drug leads. In addition, this comprehensive review can serve as a template for the development of new diverse scaffolds that will ensure for new therapeutic approaches for the existing myriad diseases and disorders.

Synthesis and antioxidant activity of a new class of bis and tris heterocycles.

A series of novel heterocycles, bisbenzoxazolyl/benzothiazolyl/benzimidazolyl pyrazoles/isoxazoles/pyrimidines were synthesized and evaluated for their antioxidant activity. The bisbenzoxazolylisoxazole 10 exhibited good antioxidant activity when compared with the standard ascorbic acid.

The reactivity of gem cyanoester ketene dithiolates towards the development of potent antioxidant heterocycles.

The reactivity of gem cyanoester ketene dithiolates towards the development of a variety of heterocycles was studied and tested for antioxidant property. The compounds bis benzoxazolylmethylthiomethylene pyrazoles and isoxazoles displayed excellent radical scavenging activity when compared with the standard ascorbic acid.

One-pot synthesis of 5-[[Bis(azolylmethylthio)]methylene]pyrimidine-2,4,6-(1H,3H,5H)-triones.

A new class of hitherto unknown trisheterocycles, bisoxadiazolyl/bisthiadiazolyl pyrimidinetriones/thioxopyrimidinediones was prepared in a one-pot reaction and their antimicrobial activity was studied.