Heterocyclic system. XI. Synthesis of 1H,4H‐pyrazolo[4,3‐b]pyrrolizine and 2H,4H‐pyrazolo[4,3‐b]pyrrolizine derivatives

Massa, S.; Mai, Antonello; Artico, M.; Corelli, Federico

doi:10.1002/jhet.5570270653

Cited by 10 publications

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“…Compounds 20 and 21 represent a further elaboration of known carboxylic acids into amides with different physicochemical properties, in particular an amide with a basic nitrogen that is protonated at physiological pH ( 21 ) and a more lipophilic amide ( 20 ). Thus, 1-phenyl-5-(1 H -pyrrol-1-yl)-1 H -pyrazole-4-carboxylic acid ( 24 ) and 1-(4-chlorophenyl)-4-methyl-5-(1 H -pyrrol-1-yl)-1 H -pyrazole-3-carboxylic acid ( 25 ) were reacted with N , N , N ′-trimethylethylenediammine and piperonylamine, respectively, in the presence of EDC/HOBt to give the expected amides 20 and 21 (Scheme ).…”

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Screen of Unfocused Libraries Identified Compounds with Direct or Synergistic Antibacterial Activity

Mugnaini

Sannio

Brizzi

et al. 2020

ACS Med. Chem. Lett.

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Antibiotic resistance is an increasingly important global public health issue, as major opportunistic pathogens are evolving toward multidrug- and pan-drug resistance phenotypes. New antibiotics are thus needed to maintain our ability to treat bacterial infections. According to the WHO, carbapenem-resistant Acinetobacter, Enterobactericaeae, and Pseudomonas are the most critical targets for the development of new antibacterial drugs. An automated phenotypic screen was implemented to screen 634 synthetic compounds obtained in-house for both their direct-acting and synergistic activity. Fourteen percent and 10% of the compounds showed growth inhibition against tested Gram-positive and Gram-negative bacteria, respectively. The most active direct-acting compounds showed a broad-spectrum antibacterial activity, including on some multidrug-resistant clinical isolates. In addition, 47 compounds were identified for their ability to potentiate the activity of other antibiotics. Compounds of three different scaffolds (2-quinolones, phenols, and pyrazoles) showed a strong potentiation of colistin, some being able to revert colistin resistance in Acinetobacter baumannii.

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confidence: 99%