The present book describes the synthesis, characterization, in silico and in vitro study of some sulfahydrazone substituted 4(3H)-Quinazolinone derivatives. We are sure that the work will be guide line for researcher working in the field of medicinal chemistry. In silico study of a novel sulfahydrazone substituted quinazolinone library screened six compounds out of 70 possible derivatives with drug like property for further in vitro exploration of anti malarial and anti tuberculosis drug activity. Although three synthesized compounds inhibited the growth of MRSA strain, suggest that it may have a future potency to use against the MRSA infection.