Synthesis and antiviral activity of a novel class of HIV-1 protease inhibitors containing a heterocyclic P1′-P2′ amide bond isostere

Design and Synthesis of New Bioactive 1,2,4-Triazoles, Potential Antitubercular and Antimicrobial Agents

“…The 1,2,4-triazole, as well found to exhibit antiasthmatic [14] , antiviral (ribavirin) [15] , antifungal (fluconazole) [16] , antimicrobial [17,18] , antibacterial [19][20][21] , insecticidal [22] , hypnotic [23] , cytotoxic [24] , antitubercular [25] and hypotensive [26,27] activities. This moiety was also found in potent agonist and antagonist receptor ligands [28,29] in HIV-1 protease inhibitors [30] and in thrombin inhibitors [31] .…”

Enantioselective N‐Heterocyclic Carbene Catalyzed Annulation Reactions with Imidazolidinones

“…[1] The exploration of these unconventional reactivity patterns with new electrophilic coupling partners facilitates advances in synthesis and provides access to bioactive natural products and unique, drug-like scaffolds. [2] Substituted imidazoles are a privileged structural motif that is prevalent in pharmaceutical small molecules with diverse biological activities, including inflammation, [3] HIV, [4] depression, [5] and various other disease areas. [6] …”

“…[4b, 7] However, unlike the related oxazolones, new asymmetric methods involving imidazolidinones are scarce in the literature. There have been several recent reports involving the use of alkylidene oxazolones in enantioselective processes, [8] likely due the ability to access unnatural amino acids from these readily available precursors.…”

Solid Phase Synthesis of 3,4,5-Trisubstituted-1,2,4-Triazoles Derivatives from the Resin-Bound Acylhydrazines

“…Compounds possessing the 1,2,4-triazole moiety have been reported to display antimicrobial activity [2], antifungal [3], antibacterial [4,5], anti-inflammatory [6] and antituberculosis [7] activities. They also can be used as peptidomimetic moieties and as hydrogen bond acceptors [8,9] or as amide bond isostere for the design of receptor ligands in order to enhance their pharmacokinetic properties [10]. It is also well established that various derivatives of 1,2,4-triazole can be used for treating non-Hodgkin's lymphoma [11].…”