School Of Basic And Applied Sciences

Permanent URI for this communityhttps://kr.cup.edu.in/handle/32116/17

Browse

Has files: NoSubject: search.filters.subject.heterocyclic compounds

Search Results

Now showing 1 - 2 of 2
  • No Thumbnail Available
    Item
    The medicinal perspective of 2,4-thiazolidinediones based ligands as antimicrobial, antitumor and antidiabetic agents: A review
    (John Wiley and Sons Inc, 2022-06-18T00:00:00) Kajal, Kumari; Singh, Gurpreet; Pradhan, Tathagata; Bhurta, Deendyal; Monga, Vikramdeep
    2,4-Thiazolidinedione (2,4-TZD), commonly known as glitazone, is a ubiquitous heterocyclic pharmacophore possessing a plethora of pharmacological activities and offering a vast opportunity for structural modification. The diverse range of biological activities endowed with a novel mode of action, low cost, and easy synthesis has attracted the attention of medicinal chemists. Several researchers have integrated the TZD core with different structural fragments to develop a wide range of lead molecules against various clinical disorders. The most common sites for structural modifications at the 2,4-TZD nucleus are the N-3 and the active methylene at C-5. The review covers the recent development of TZD derivatives such as antimicrobial, anticancer, and antidiabetic agents. Various 2,4-TZD based agents or drugs, which are either under clinical development or in the market, are discussed in the study. Different synthetic methodologies for synthesizing the 2,4-TZD core are also included in the manuscript. The importance of various substitutions at N-3 and C-5 and the mechanisms of action and structure�activity relationships are also discussed. We hope this study will serve as a valuable tool for the scientific community engaged in the structural exploitation of the 2,4-TZD core for developing novel drug m\olecules for life-threatening ailments. � 2022 Deutsche Pharmazeutische Gesellschaft.
  • No Thumbnail Available
    Item
    Recent advances for construction and late-stage diversification of indole core via C-H bond activation/functionalization
    (Elsevier, 2021-02-26T00:00:00) Sinha, Arun Kumar; Kumar, Rakesh
    Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials. Owing to such a huge potential, continuous efforts are being put forward to construct or diversify this scaffold. This chapter provides an overview of various recently developed methodologies for the construction of indole core via C-H bond activation/functionalization. In particular, Pd- and Ru-mediated cyclization strategies involving Csp2-H functionalization of monofunctionalized arene substrates with the unsaturated bond of alkene and alkyne are highlighted herein. Also, late-stage diversification of indole system (C4-C7 position) via direct C-H activation is covered. Furthermore, the mechanistic aspects of some of these reactions are discussed as well. � 2021 Elsevier Inc. All rights reserved.