Combinatorial Libraries of Bis-heterocyclic Compounds with Skeletal Diversity

Abstract

Combinatorial solid-phase synthesis of bis-heterocyclic compounds, characterized by the presence of two heterocyclic cores connected by a spacer of variable length/structure, provided structurally heterogeneous libraries with skeletal diversity. Both heterocyclic rings were assembled on resin in a combinatorial fashion.

Microwave‐Assisted Synthesis of Novel Bis(thiazoles) Incorporating Piperazine Moiety

“…In addition, bis-heterocyclic compounds as well as hybrid molecules, whose pharmacophores are integrated into a single molecule, were reported to display various biological activities, especially as fungicidal, antibacterial, tuberculostatic, anthelmintic, and antiamoebic [15][16][17][18][19][20][21][22]. Because of the significant bioactivity and wide range of application of piperazine and thiazole derivatives as well as bis-heterocyclic compounds, several publications reported concerning the synthesis of these derivatives [23][24][25][26][27][28][29][30][31].…”

Synthesis of Novel Bis(thiazolylchromen‐2‐one) Derivatives Linked to Alkyl Spacer via Phenoxy Group

“…In addition to the therapeutic activities of coumarin derivatives, their less damage to normal cells were also reported [25]. Furthermore, bis-heterocyclic compounds exhibit various biological activities, including antibacterial, fungicidal, tuberculostatic, antiamoebic, anthelmintic, and plant growth regulative properties [26][27][28][29].…”

<strong>Synthesis of <em>bis</em>-heterocycles type spacer containing 1,5-disubstituted-1<em>H</em>-tetrazoles</strong>

“…Two heterocyclic moieties with the similar or different biological activity can be suitably placed to synthesize complex molecules with potential application in the field of medicinal chemistry [2][3][4]. Recent reports on the drugs approved by FDA, includes libraries of molecules containing bis-heterocycle [5][6].…”