Quinolines, a perpetual, multipurpose scaffold in medicinal chemistry.

Synthetic small molecules as anti-biofilm agents in the struggle against antibiotic resistance.

Biofilms are intricate bacterial assemblages that attach to diverse surfaces using an extracellular polymeric substance that protects them from the host immune system and conventional antibiotics. Biofilms cause chronic infections that result in millions of deaths around the world every year. Since the antibiotic tolerance mechanism in biofilm is different than that of the planktonic cells due to its multicellular structure, the currently available antibiotics are inadequate to treat biofilm-associated infections which have led to an immense need to find newer treatment options. Over the years, various novel antibiofilm compounds able to fight biofilms have been discovered. In this review, we have focused on the recent and intensively researched therapeutic techniques and antibiofilm agents used for biofilm treatment and grouped them according to their type and mode of action. We also discuss some therapeutic approaches that have the potential for future advancement.

/pdf/recent-strategies-to-combat-biofilms-using-antimicrobial-2ytni9o5.pdf

Recent Strategies to Combat Biofilms Using Antimicrobial Agents and Therapeutic Approaches

A series of novel thienopyridines and pyridothienoquinolines (3a,b–14) was synthesized, starting with 2-thioxo-1,2-dihydropyridine-3-carbonitriles 1a and 1b. All compounds were evaluated for their in vitro antimicrobial activity against six bacterial strains. Compounds 3a,b, 4a, 5b, 6a,b, 7a, 9b, 12b, and 14 showed significant growth inhibition activity against both Gram-positive and Gram-negative bacteria compared with the reference drug. The most active compounds (4a, 7a, 9b, and 12b) against Staphylococcus aureus were also tested for their in vitro inhibitory action on methicillin-resistant Staphylococcus aureus (MRSA). The tested compounds showed promising inhibition activity, with the performance of 12b being equal to gentamicin and that of 7a exceeding it. Moreover, the most promising compounds were also screened for their Escherichia coli DNA gyrase inhibitory activity, compared with novobiocin as a reference DNA gyrase inhibitor. The results revealed that compounds (3a, 3b, 4a, 9b, and 12b) had the highest inhibitory capacity, with IC50 values of 2.26–5.87 µM (that of novobiocin is equal to 4.17 µM). Docking studies were performed to identify the mode of binding of the tested compounds to the active site of E. coli DNA gyrase B.

https://www.mdpi.com/1420-3049/24/20/3650/pdf

Synthesis, Docking Studies, and In Vitro Evaluation of Some Novel Thienopyridines and Fused Thienopyridine-Quinolines as Antibacterial Agents and DNA Gyrase Inhibitors.

\n\nHeterocyclic compounds are an integral part of the chemical and life sciences\nand constitute a considerable quantum of the modern research that is being currently pursued throughout\nthe world.\n\n\n\nThis review was prepared by collecting the available literature reports on various databases\nand an extract was prepared for each report after thorough study and compiling the recent literature\nreports on heterocyclic amides from 2007 to 2018.\n\n\n\nThis review summarizes the bio-potential of heterocyclic amides as antimicrobial, anticancer,\nanti-tubercular and antimalarial agents which would be very promising in the field of medicinal chemistry.\n\n\n\nA wide variety of heterocyclic amides have already been reported and some are currently\nbeing used as active medicaments for the treatment of disease. Still, the research groups are focusing on\nthe development of newer heterocyclic amide derivatives with better efficacy, potency and lesser side\neffects. This area has got the tremendous potential to come up with new chemical entities of medicinal\nimportance.\n

Recent Development on Importance of Heterocyclic Amides as Potential Bioactive Molecules: A Review

Synthesis of novel pyrazolo[3,4-b]quinolinyl acetamide analogs, their evaluation for antimicrobial and anticancer activities, validation by molecular modeling and CoMFA analysis.

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Synthesis of novel pyrazolo[3,4-b]quinolinyl acetamide analogs, their evaluation for antimicrobial and anticancer activities, validation by molecular modeling and CoMFA analysis.