Synthesis and Biological Evaluation of Substituted Heterocyclic Derivatives Using QSAR Approach

Abstract

In recent years, a number of life-threatening infections caused by multi-drug newlineresistant Gram-positive and Gram-negative pathogenic bacteria have reached an alarming newlinelevel in many countries. A number of clinical reports published in the United States and newlineother countries have independently established the emergence of resistance to newlinevancomycin, in methicillin-resistance Staphylococcus aureus (MRSA) isolates and other newlinehuman pathogenic Gram-negative bacteria isolates. Infections caused by these newlinemicroorganisms pose a serious challenge to scientific community to evolve an effective newlinetherapy based on new antibacterial agents. newlineSignificant advances in detection and treatment of cancer have been made in newlinerecent years still the incidence of some malignancies is rampant that need to be newlineeliminated or atleast brought down to acceptable level. Established treatments such as newlinecytotoxic chemotherapy and radiotherapy provide only transient therapeutic benefits for newlinetumor type malignancies that too with severe side effects. The challenge is to develop newlinenew and efficient chemotherapeutic agents so that cancer treatment may be well newlinemanaged. newlineBenzimidazole is an important heterocyclic compound and pharmacophore in newlinemedicinal chemistry and pharmaceutical industry. A wide variety of benzimidazole newlinederivatives have been synthesized and reported for their diverse pharmacological newlineactivities such as antioxidant, antimicrobial, antihelmintic, anticancer, antiviral, newlineantiparasitic, anti-inflammatory, anti-HIV and antihypertensive etc. newlineQuantitative Structure Activity Relationship (QSAR) has proved to be a useful newlinetool for rational search of bioactive molecules. QSAR is essentially a mathematical newlinerelationship between molecular descriptor based on physicochemical properties of a newlinedrug molecule and biological activity. In this context, QSAR helps in identification of newlinethe minimum number of compounds that need to be synthesized having desired newlinebiological activity. The real value of QSAR lies in establishing a predictive scheme newlinebased on biological activity ....