Indolizine Derivatives with Biological Activity I: N′-Substituted Hydrazides of Indolizine-2-carboxylic Acid

Characterisation of hydrazides and hydrazine derivatives as novel aspartic protease inhibitors

“…A conserved β-hairpin structure known as flap (Asn76-Thr81) lies perpendicular over the centre of the cleft and interacts with substrates/inhibitors [25]. The hydrazides are predicted to dock at the centre of the substrate-binding cleft with two binding modes.…”

“…They also have been reported as monoamine oxidase inhibitors [25]. We have characterised phenyl hydrazide and hydrazine derivatives as Plasmodium falciparum plasmepsin-II and human cathepsin D inhibitors suggested by virtual screening of an in-house library of synthetic compounds and confirmed by enzyme inhibition studies.…”

Nitro- para- and meta- Substituted 2-Phenylindolizines as Potential Antimicrobial Agents

“…Two earlier reports (18,19) stated that N1-substituted hydrazides of indolizine-2-carboxylic acid were more active than iproniazid in the inhibition of monoamine oxidase. Antonini et al (20) also found that 3-(3-aminopropyl)-2-methylindolizine possessed antiserotonin antihis-0 tamine and antiacetylcholine properties with some CNS activity.…”