Prevalence of microbial infections and new rising pathogens are signified as causative agent for variety of serious and lethal health crisis in past years. Despite medical advances, bacterial and fungal infections continue to be a rising problem in the health care system. As more bacteria develop resistance to antibiotics used in therapy, and as more invasive microbial species develop resistance to conventional antimicrobial drugs. Relevant published publications from the last two decades, up to 2024, were systematically retrieved from the MEDLINE/PubMed, SCOPUS, EMBASE, and WOS databases using keywords such as quinolones, anti-infective, antibacterial, antimicrobial resistance and patents on quinolone derivatives. With an approach of considerable interest towards novel heterocyclic derivatives as novel anti-infective agents, researchers have explored these as essential tools in vistas of drug design and development. Among heterocycles, quinolones have been regarded extremely essential for the development of novel derivatives, even able to tackle the associated resistance issues. The quinolone scaffold with its bicyclic structure and specific functional groups such as the carbonyl and acidic groups, is indeed considered a valuable functionalities for further lead generation and optimization in drug discovery. Besides, the substitution at N-1, C-3 and C-7 positions also subjected to be having a significant role in anti-infective potential. In this article, we intend to highlight recent quinolone derivatives based on the SAR approach and anti-infective potential such as antibacterial, antifungal, antimalarial, antitubercular, antitrypanosomal and antiviral activities. Moreover, some recent patents granted on quinolone-containing derivatives as anti-infective agents have also been highlighted in tabular form. Due consideration of this, future research in this scaffold is expected to be useful for aspiring scientists to get pharmacologically significant leads.

Methicillin-resistant Staphylococcus aureus (MRSA) is one of the prime pathogens responsible for surgical site infection (SSI). Treatment of SSI remains challenging because of resistant nature of MRSA, which is a major threat in recent years. Our previous work revealed the antibacterial potential of catechin isolated from cashewnut shell against MRSA. However, the application of catechin to treat MRSA-mediated SSI is hampered because of its poor solubility and low trans-dermal delivery. Hence, the present study focused on developing catechin-in-cyclodextrin-in-phospholipid liposome (CCPL) and evaluating its physicochemical characteristics and anti-infective efficacy through in vitro and in vivo models. Encapsulation of catechin with β-cyclodextrin and soybean lecithin was confirmed through UV-Vis spectroscopy, FTIR, and XRD techniques, while TEM imaging revealed the size of CCPL (206 nm). The CCPL displayed a higher level of water solubility (25.13%) and in vitro permeability (42.14%) compared to pure catechin. A higher level of encapsulation efficiency (98.9%) and antibacterial activity (19.8 mm of ZOI and 31.25 μg/mL of MIC) were noted in CCPL compared to the catechin/cyclodextrin complex. CCPL recorded significant and dose-dependent healing of the incision, significant reduction of bacterial count, improved epithelization, and effective prevention of inflammation in skin samples of SSI-induced Balb/c mice. Data of the present work suggest that the CCPL could be considered as a novel and potential candidate to mitigate MRSA-mediated SSI after clinical trials.

New antimicrobial agents derived from endosymbio-tic fungi with unique and targeted mode of action are crucially rudimentary to combat multidrug-resistant infections. Most of the fungi isolated as endosymbionts show close morphological feature resemblance to plant pathogenic or free-living forms, and it is difficult to differentiate these different lifestyles. A fungal endosymbiont strain CLB44 was isolated from Combretum latifolium Blume (Combretaceae). CLB44 was then identified as Alternaria longissima based on morphological and internal transcribed spacer (ITS) intervening 5.8S rRNA gene sequence analysis. ITS2 RNA secondary structure analysis was carried out using mfold server with temperature 37 °C, and anti-infective potential was determined by MIC and disk diffusion methods. ITS2 RNA secondary structure analysis clearly distinguished endosymbiotic A. longissima CLB44 from free-living and pathogenic A. longissima members in the same monophyletic clade. Secondary metabolites produced effectively inhibited Pseudomonas aeruginosa (25 μg/ml), Escherichia coli (25 μg/ml), methicillin-resistant Staphylococcus aureus (50 μg/ml), Candida albicans (100 μg/ml), and other human pathogens. This study emerges as an innovative finding that explores newly revealed ITS2 RNAs that may be an insight as new markers for refining phylogenetic relations and to distinguish fungal endosymbionts with other free-living or pathogenic forms. A. longissima CLB44, in the emerging field of endosymbionts, will pave the way to a novel avenue in drug discovery to combat multidrug-resistant infections. The sequence data of this fungus is deposited in GenBank under the accession no. KU310611.