Study of the anti(myco)bacterial and antitumor activities of prolinate and N-amidocarbothiolprolinate derivatives based on fused tetrahydropyrrolo[3,4-c]pyrrole-1,3(2H,3aH)-dione, bearing an indole ring

Poyraz, Samet; Canacankatan, Necmiye; Belveren, Samet; Yetkin, Derya; Kibar, Kezban; Ülger, Mahmut; Sansano, José M.; Özçelik, Nefise Dilek; Yılmaz, Şükran; Döndaş, H. Ali

doi:10.1007/s00706-018-2286-8

Cited by 8 publications

(3 citation statements)

References 31 publications

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“…Our research group designed the synthesis of significant hybrid compound series containing cyclic or bicyclic pyrrolidine rings and reported their bioactive properties. The pyrrolidine hybrids were incorporated with important pharmacophore moieties such as N -benzoylthiourea, thiohydantoin, thiazole, imidazole, and indole ( Belveren et al, 2017 ; Poyraz et al, 2017 ; Poyraz et al, 2018 ; Belveren et al, 2019 ; Poyraz et al, 2023b ).…”

Section: Polysubstituted Pyrrolidinesmentioning

confidence: 99%

“…Compound 16c , containing the 4-chlorophenyl group, showed better antituberculosis (anti-TB) activity than the reference ethambutol. Compounds 15a and 15b , which are among the pyrrolidine derivatives used in the synthesis of the corresponding compounds, also showed four times higher activity (MIC: 31.25 μg/mL) against A. baumannii than the reference ampicillin (MIC: 125 μg/mL) ( Poyraz et al, 2018 ).…”

Section: Polysubstituted Pyrrolidinesmentioning

confidence: 99%

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Recent insights about pyrrolidine core skeletons in pharmacology

Poyraz,

Döndaş,

Döndaş

et al. 2023

Front. Pharmacol.

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To overcome numerous health disorders, heterocyclic structures of synthetic or natural origin are utilized, and notably, the emergence of various side effects of existing drugs used for treatment or the resistance of disease-causing microorganisms renders drugs ineffective. Therefore, the discovery of potential therapeutic agents that utilize different modes of action is of utmost significance to circumvent these constraints. Pyrrolidines, pyrrolidine-alkaloids, and pyrrolidine-based hybrid molecules are present in many natural products and pharmacologically important agents. Their key roles in pharmacotherapy make them a versatile scaffold for designing and developing novel biologically active compounds and drug candidates. This review aims to provide an overview of recent advancements (especially during 2015–2023) in the exploration of pyrrolidine derivatives, emphasizing their significance as fundamental components of the skeletal structure. In contrast to previous reviews that have predominantly focused on a singular biological activity associated with these molecules, this review consolidates findings from various investigations encompassing a wide range of important activities (antimicrobial, antiviral, anticancer, anti-inflammatory, anticonvulsant, cholinesterase inhibition, and carbonic anhydrase inhibition) exhibited by pyrrolidine derivatives. This study is also anticipated to serve as a valuable resource for drug research and development endeavors, offering significant insights and guidance.

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Section: Polysubstituted Pyrrolidinesmentioning

confidence: 99%

Section: Polysubstituted Pyrrolidinesmentioning

confidence: 99%

Recent insights about pyrrolidine core skeletons in pharmacology

Poyraz,

Döndaş,

Döndaş

et al. 2023

Front. Pharmacol.

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“…The hybrids 60a,b (MIC: 31.2–62.5 μg/ml) and 61a–c (MIC: 15.6–62.5 μg/ml; Figure 9) showed considerable activity against S. aureus , B. subtilis , A. hydrophila , E. coli , and A. baumanii , and the activity was comparable to or superior to that of ampicillin (MIC: 15.6–125 μg/ml). [ 126–128 ] The SAR indicated that the methoxy group at the phenyl ring was critical for the activity for hybrids 60 , and the replacement of the methoxy group by the chloro group led to a great loss of activity.…”

Section: Indole/isatin–pyrrole/furan/thiophene Hybridsmentioning

confidence: 99%

Indole/isatin‐containing hybrids as potential antibacterial agents

Song

Bian

et al. 2020

Archiv der Pharmazie

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The emergence and worldwide spread of drug-resistant bacteria have already posed a serious threat to human life, creating the urgent need to develop potent and novel antibacterial drug candidates with high efficacy. Indole and isatin (indole-2,3-dione) present a wide structural and mechanistic diversity, so their derivatives possess various pharmacological properties and occupy a salient place in the development of new drugs. Indole/isatin-containing hybrids, which demonstrate a promising activity against a panel of clinically important Gram-positive and Gram-negative bacteria, are privileged scaffolds for the discovery of novel antibacterial candidates. This review, covering articles published between January 2015 and May 2020, focuses on the development and structure-activity relationship (SAR) of indole/isatincontaining hybrids with potential application for fighting bacterial infections, to facilitate further rational design of novel drug candidates.

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Ultrasonic Cavitation Facilitates Rapid Synthesis of Trisubstituted Pyrazole Scaffolds through Michael Addition/Domino Cyclization

Kannan

Naveen

Jagadeesan³

et al. 2019

ChemistrySelect

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A series of aryl/indolyl substituted 4, 5‐dihydro‐1H‐pyrazole derivatives were synthesized via a domino method based on Michael addition mediated cyclization of appropriate chalcones. The chalcones were prepared by Witting reaction in which substituted aromatic aldehydes were treated with stable ylides under eco‐friendly ultrasonic cavitation. The pyrazole scaffolds were obtained in excellent yields within a short span of time.

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Study of the anti(myco)bacterial and antitumor activities of prolinate and N-amidocarbothiolprolinate derivatives based on fused tetrahydropyrrolo[3,4-c]pyrrole-1,3(2H,3aH)-dione, bearing an indole ring

Abstract: Study of the anti(myco)bacterial and antitumor activities of prolinate and N-amidocarbothiolprolinate derivatives based on fused tetrahydropyrrolo[3,4c]pyrrole-1,3(2H,3aH)-dione, bearing an indole ring

Cited by 8 publications

References 31 publications

Recent insights about pyrrolidine core skeletons in pharmacology

Recent insights about pyrrolidine core skeletons in pharmacology

Indole/isatin‐containing hybrids as potential antibacterial agents

Ultrasonic Cavitation Facilitates Rapid Synthesis of Trisubstituted Pyrazole Scaffolds through Michael Addition/Domino Cyclization

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