There is undeniable evidence that many N-heterocycles exhibit a wide range of biological functions. Recently, derivatives with better bioactivities have been generated by condensing the different heterocycles. Pyrazolopyridines have been able to pique the interest of many researchers among many other condensed heterocycles, due to the wide range of actions they exhibit. Furthermore, each type of condensed heterocycle has been specifically highlighted in this review in terms of design and biological activities. In silico methods and structure-activity relationship have also been discussed wherever reported.