Mahesh A. Barmade

Developing steroidal aromatase inhibitors-an effective armament to win the battle against breast cancer.

Breast cancer, an emerging disease among the women population, occurs due to overexpression of estrogens. The enzyme aromatase plays a key rate limiting role in the biosynthesis of estrogens. Certain clinical advantages of the use of exemestane, a steroidal aromatase inhibitor over non-steroidal aromatase inhibitors have drawn the attention of researchers for the development of novel steroidal aromatase inhibitors.The current review is a humble attempt to compile the reports by various researchers till date on the synthesis of steroidal aromatase inhibitors. It has been tried to encompass the structural modifications carried out by various researchers in the steroid ring system by taking up the functional group modifications on rings A, B, ring A/B junction, ring-D, ring modifications, bridged derivatives and heterocyclic ring-fused derivatives in a systematic way.

Medicinal Chemistry Perspective of Fused Isoxazole Derivatives.

Nitrogen containing heterocyclic rings with an oxygen atom is considered as one of the best combination in medicinal chemistry due to their diversified biological activities. Isoxazole, a five membered heterocyclic azole ring is found in naturally occuring ibetonic acid along with some of the marketed drugs such as valdecoxib, flucloxacillin, cloxacillin, dicloxacillin, and danazol. It is also significant for showing antipsychotic activity in risperidone and anticonvulsant activity in zonisamide, the marketed drugs. This review article covers research articles reported till date covering biological activity along with SAR of fused isoxazole derivatives.

A comprehensive patents review on cannabinoid 1 receptor antagonists as antiobesity agents

Introduction: Obesity is a rapidly expanding worldwide health problem. Various targets are investigated presently for the treatment of obesity, but there remains an unmet need for an effective drug therapy with acceptable efficacy levels and reduced side effects. Targeting peripherally located cannabinoid 1 (CB1) receptors is an attractive strategy as these receptors play a vital role in energy homeostasis. Areas covered: CB1 receptor antagonists constitute one of the most important categories of compounds of interest for the control of obesity. In this review, the authors focus on recent advances (since 2007) in diverse chemical classes of patented compounds belonging to the category of CB1 receptor antagonists. Expert opinion: Safer CB1 receptor antagonists for the treatment of obesity can be discovered by developing such compounds that act peripherally. Increasing the polar service area, decreasing the lipophilicity and designing of neutral antagonists and allosteric inhibitors are some interesting strategies that could offer promising results.

Discovery of anti-malarial agents through application of in silico studies.

Among the various parasitic diseases, malaria is the deadliest one. Due to the emergence of high drug resistance to the existing drug candidates there is a global need for development of new drug candidates which will be effective against resistant strains of malaria parasite. In silico molecular modeling approaches have been playing an important role in the discovery of novel lead molecules having antimalarial activity. Present review is an effort to cover all the developments related to the application of computational techniques for the design and discovery of novel antimalarial compounds since the year 2011 onwards.

Synthesis and Biological Significance of Six- and Seven-membered Vicinal Diaryl Heterocycles

Abstract Vicinal diaryl containing heterocycles have proved their central role in medicinal chemistry by exhibiting diversified biological activities. Molecules based on these scaffolds, for example, coxibs class of compounds were among the block buster molecules in the market. Replacing the central core of the diaryl heterocycles with different biologically active hetero-scaffolds increased the number of marketed drugs. Majority of the diaryl COX-2 inhibitors were based on five-membered central core but one molecule with six-membered scaffold, that is, etoricoxib is also currently available in the market. In this chapter, efforts have been made to disclose different strategies used for the synthesis and design of novel vicinal diaryl compounds with six- and seven-membered central core.

Biological Spectrum of Vicinal Diaryl-Substituted Fused Heterocycles

Abstract In the drug discovery process, fusion of two or more heterocyclic rings is an effective strategy for designing new drugs. Diaryl fused heterocyclic compounds have shown a high impact in the field of medicinal chemistry as the number of diaryl fused heterocyclic compounds having a variety of biological activities are increasing day by day. In this chapter, we have focused on the synthesis and biological activities of a number of vicinal diaryl fused heterocyclic scaffolds such as diaryl hydropyrrolizines, diaryl pyrrolidinoisoxazolidines, diaryl imidazolothiazolines, diaryl imidazothiadiazoles, diaryl 2,3,8,8a-tetrahydroindolizin-5-(1H)-ones, diaryl indoles, diaryl heteroaryl-fused pyridines, diaryl heteroaryl pyrimidines, diaryl chromanes, diaryl quinolines, diaryl quinoxalines, diaryl purines, etc.

Vicinal Diaryl Heterocyclic System: A Privileged Scaffold in the Discovery of Potential Therapeutic Agents

Abstract Heterocyclic chemistry has provided numerous heterocyclic compounds, which have been used effectively for the development of drugs for the management of several health conditions. Enormous interest has been generated in heterocyclic compounds which could mimic the structures and biological activities of the naturally occurring drugs. Over the last 2 decades, a large number of vicinal diaryl heterocyclic compounds have been synthesized and reported in the literature having a variety of biological activities such as anticancer, antihypercholesterolemic, antiviral, antimicrobial, anti-inflammatory, analgesic, etc. This chapter highlights the importance and biological significance of the chemical entities belonging to the class of vicinal diaryl heterocyclic compounds as clinically used drugs or novel potential lead molecules.