ChemInform Abstract: Synthesis and Use of Pseudopeptides Derived from 1,2,4‐Oxadiazole‐, 1,3,4‐Oxadiazole‐, and 1,2,4‐Triazole‐Based Dipeptidomimetics

Abstract

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Design, synthesis, characterization, and antibacterial activity of {5-chloro-2-[(3-substitutedphenyl-1,2,4-oxadiazol-5-yl)-methoxy]-phenyl}-(phenyl)-methanones

“…The 1,2,4-oxadiazole ring system has received considerable attention in the pharmaceutical industry as heterocyclic amide and ester isosteres [1]. Similar ring systems are present in various biologically interesting compounds such as muscarinic receptor agonists [2], tyrosine kinase inhibitors [3], anti-inflammatory agents [4], selective H 3 receptor antagonists [5], antitumor agents [6], monoamine oxidasea inhibitors [7], anticonvulsant [8], and anti-HIV agents [9].…”

Mild and Efficient One-Pot Synthesis of 3,5-Disubstituted 1,2,4-Oxadiazoles from Nitriles Mediated by K3PO4

“…[6] In addition, anticancer activity of some 3,5-disubstituted-1,2,4-oxadiazoles has recently been reported. [7] The 1,2,4-oxadiazoles are also widely used as heterocyclic amide or ester bioisosters [8] and in the design of dipeptidomimetics as peptide building blocks, [9] and are found in several drugs and drug leads [4] including the metabotropic glutamate subtype 5 (mGlu 5) receptor ( Fig. 1, 1), [10] the muscarinic receptor for the treatment of Alzheimer ' s disease (Fig.…”

Design and Synthesis of 3,5‐Disubstituted‐1,2,4‐Oxadiazoles as Potent Inhibitors of Phosphodiesterase4B2

“…Recently, there has been growing interest in compounds containing the 1,2,4‐oxadiazole scaffold because of their unique chemical structure and broad spectrum of biological properties including tyrosine kinase inhibition (18), muscarinic agonism (19), histamine H3 antagonism (20), antiinflammation (21), anticancer (22–24), and monoamine oxidase inhibition (25). The 1,2,4‐oxadiazoles are also widely used as heterocyclic amide or ester bioisosters (26) and in the design of dipeptidomimetics as peptide building blocks (27,28). Incorporation of 1,2,4‐oxadiazole ring in the second generation PDE4 inhibitors may improve their metabolic stability and inhibition activities (Figure 1).…”