Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–4

Abstract

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials, which is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules. [...]

8‐Hydroxyquinoline‐2‐Carboxanilides as Antiviral Agents Against Avian Influenza Virus

“…They are able to affect specifically many different target structures in cells and are known metal chelators. Thus, their mechanisms of action can be considered as complex,,,, which meets the modern definition of so‐called multi‐target agents . Within the investigation of simple derivatives of 8‐hydroxyquinolines, 8‐hydroxyquinoline‐2‐carboxanilides were prepared, and their antimycobacterial and antibacterial activities were described .…”

Investigation of Anti-Inflammatory Potential of N-Arylcinnamamide Derivatives

“…Thus, cinnamides can be considered as a privilege structure or a scaffold (a part) of more complex molecules in medicinal chemistry [23,24] The series of N-arylcinnamide derivatives presented in this work was previously tested for their anti-microbial activity (compounds 1-15 and 17) [25,26], and three new derivatives 16 and 18 were prepared and characterized. Based on the concepts of polypharmacology, multifactorial diseases, and multitarget drugs [27], as well as the above-mentioned results, a group of eighteen N-arylcinnamanilides was chosen for the screening of their ability to moderate the inflammation-like reaction in vitro.…”

Design and Synthesis of Novel Antimicrobial Agents

“…The self-assembled nanobiotic shown improved broad-spectrum bactericidal action specifically against E. coli and MRSA by disrupting the cell wall and possibly other membrane structures, according to in vitro data. Excellent tolerability was also demonstrated in in vivo testing, where it was discovered that the nanobiotic could protect mice from MRSA skin infections and save them from E. coli -induced sepsis [ 72 ].…”

“…The supertryptophan residue (2,5,7-tri-tertbutyltryptophane) and cationic peptides were coupled to create AMPs with MIC values ranging from 2 to 16 µg/mL against both Gram-positive and Gram-negative bacteria. The best candidate that demonstrated a significant increase in the survival rate in vivo in septic mice was the Tbt-β 2,2 h bis-Arg-OMe compound ( 23 , Figure 10 ) [ 110 ]. Shrimp antilipopolysaccharide factors (ALFs) were employed by Matos et al [ 111 ] to create a cysteine-free α-helix secondary structure peptide that closely follows the amino acid sequence of the central β-hairpin of Litopenaeus vannamei ALFs (Litvan ALF-E 33-52 (YVNRSPYLKKFEVHYRADVK), Litvan ALF-F 31-50 (TYFVTPKVKSFELYFKGRMT), Litvan ALF-G 35-54 (SYSTRPYFLRWRLKFKSKVW)).…”

“…By binding to a specific location on the ribosome (30S subunit), ODLs, which are cationic peptides made by NRPSs gene cluster enzymes of Xenorhabdus nematophila , disrupt the ability of bacteria to interpret and translate genetic code. As a result, it causes miscoding when producing new proteins, which causes bacterial cell death [ 138 , 139 ]. To tackle Gram-negative, Gram-positive, and multidrug-resistant bacteria, NOSO-502 ( 46 , Figure 11 ) is a new class of bacterial ribosomal inhibitors ODLs that is safe and highly selective [ 140 ].…”