Background: Antibiotic resistance is currently considered a major public health problem. This subject underscores the critical need for novel and enhanced antibacterial agents with a novel molecular structure and a new target to prevent cross-resistance. Copper exhibits antimicrobial properties by disrupting bacterial cell membranes and interfering with cellular processes. Copper complexes enhance these properties, offering improved stability and targeted antibacterial activity. Their ability to release copper ions can gradually enhance efficacy while minimizing toxicity. Therefore, investigating the antibacterial properties of new copper complexes is of significance. Methods: In this study, the antibacterial activity of [Cu(dimethylbpy)2Cl]PF6 complex was examined against several Gram-negative bacteria, Pseudomonas aeruginosa, Escherichia coli, klebsiella pneumoniae, salmonella typhi and Gram-positive bacteria Staphylococcus aureus and Micrococcus luteus by determining the minimum inhibitory concentration (MIC). The antibacterial activity of [Cu(dimethylbpy)2Cl]PF6 complex and Gentamicin (as standard compound) were determined using the microplate method. All concentrations were repeated three times. The minimum inhibitory concentration was determined both using the unaided eye and absorbance at 490 nm. Results: The [Cu(dimethylbpy)2Cl]PF6 complex showed higher antibacterial activity against Gram-positive bacteria than Gram-negative bacteria. Among the assayed bacterial strains, the complex was most effective against Micrococcus luteus and Staphylococcus aureus with MIC values of 100 and 250 μM, respectively. Conclusion: This complex displayed antimicrobial potential against some bacterial strains. Therefore, this complex may be used as an effective antibacterial agent in the treatment of infection caused by some bacterial strains, but further research is needed.

Background: Biflavonoids are natural phytocompounds that received enormous at-tention in various remedies due to their diverse biological activities. Biflavonoids have anti-inflammatory, anti-leishmanial, anti-plasmodial, anti-viral and β-secretase inhibitory activity in medicine. Ochnaflavone is a biflavone class natural phytochemical isolated from plants belong-ing to the Ochnaceae family. Methods:: Scientific information on ochnaflavone was collected and analyzed in the present investigation to investigate the biological activities of ochnaflavone. The present paper de-scribes the pharmacological activities and bioanalytical aspects of ochnaflavone based on the available scientific research on ochnaflavone in research work, books and other literature data-bases. Scientific data on ochnaflavone were collected from various scientific databases (Google, Science Direct, Scopus and PubMed) in this paper in order to investigate the health-beneficial potential of ochnaflavone in medicine. Further, the pharmacological activity of ochnaflavone was also collected in a detailed manner and discussed here in order to know the health-beneficial aspects of ochnaflavone. Results:: The therapeutic importance of ochnaflavone has been summarized in the present paper through available literature data on ochnaflavone in the scientific fields. Ochnaflavone was found to be an active phytochemical of Campylospermum excavatum, Cespedesia spathulata, Godoya antioquiensis, Lonicera japonica, Lonicerae Japonicae, Ochna afzelii, Ochna bed-domei, Ochna beddomi, Ochna integerrima, Ochna kibbiensis, Ochna pretoriensis, Ochna squarrosa Linn., Selaginella trichoclada and Triclisia gilletii. Scientific data revealed the bio-logical importance of ochnaflavone for its effectiveness on inflammation, SARS-CoV-2, fungal arthritis, enzymes, mutagenic effect, lymphocyte proliferation, and inhibition of arachidonate release. However, its antimycobacterial activity, cytotoxic effect, anti-HIV-1 activity, and anti-oxidant potential were also presented in this work. Further, analytical data on ochnaflavone has also been described. Conclusion: The present paper describes the therapeutic role of ochnaflavone in human disor-ders with their analytical aspects.

Background: In various microorganisms, various defense mechanisms have evolved against the commercially available antimicrobial agents with increased resistance. Natural antimi-crobial agents of plant origin are better alternatives when an infectious disease arises due to resistant microbial strains. Here, we have evaluated the efficacy of total phenolics and total flavonoids with antioxidant and antimicrobial potential of Artemisia sieversiana Ehrhl Ex Willd. plant extracted with methanol, ethyl acetate, ethanol, n-hexane, and chloroform using soxhlet procedures Methods: The evaluation of TPC was achieved with Folin-Ciocalteu’s reagent method and quanti-tative estimation of TFC was done with the aluminum chloride colorimetric method. The antioxi-dant activities were estimated using FRSA-DPPH and TAC methods. The inhibitory activities of five solvent extracts of A. sieversiana against 2 gram-positive and 2 gram-negative pathogenic bac-terial strains (B. subtilis, P. aerogenosa, S. aureus, and E. coli) were evaluated using the well dif-fusion technique. Results: The highest percentage yields of A. sieversiana extracts were obtained in ethanol (4.8 g, 12.1%) and methanol (4.01 g, 10%), while minimum extract yield was obtained in n-hexane (0.53 g, 1.34%). Both phenolics and flavonoids were higher in ethanol, methanol, and ethyl acetate ex-tracts while minimal in n-hexane extracts. Ethanol extract has shown maximum (69%) DPPH ac-tivity with a lower IC50 value (181 μg/ml), while the highest IC50 values of 330 and 325μg/ml were recorded for n-hexane and ethyl acetate extracts. The ethyl acetate and chloroform extracts dis-played overall highest TAC values. All the tested extracts of A. sieversiana exhibited variable in-hibitory effects in a dose-dependent manner against the tested bacterial strains with minimum 9.08 ± 0.23 to maximum 21.23 ± 7.04 mm inhibition zones. Methanol and ethyl acetate extracts at 2 to 4 mg/ml showed greater MIC results against P. aeruginosa in comparison to the B. subtilis strain. Conclusion: The extracts of A. sieversiana have been found to be rich in TPC and TFC with re-markable antibacterial and antioxidant efficacies, and the plant extracts could be employed as pos-sible alternatives to synthetic drugs in various nutraceutical and pharmaceutical industries.

Background: Emerging antibiotic resistance (ABR) in Proteus spp., especially to third-generation cephalosporins (3GCc), carbapenems, and fluoroquinolones, challenges the treatment outcome and infection prevention. Limited studies pose a knowledge gap between them and ABR. Methods: We investigated the in vitro efficacy of therapeutic options and prevalence of β-lac-tamase and plasmid-mediated quinolone resistance (PMQR) traits in 3GC- and/or fluoroquino-lone-nonsusceptible Proteus (P.) spp. (n=27) in Kolkata, India, during 2021–2022. P. mirabilis was commonly isolated (>80%) from superficial and urine samples. The majority of the isolates (48-78%) remained susceptible to piperacillin-tazobactam, meropenem, amikacin, cefoperazone-sulbactam, and cefepime. Results: All isolates showed >0.2 multiple-antibiotic resistance index, with >65% being multi-drug and >30% being extensively drug-resistant. blaTEM (n=9), blaNDM (n=9), and qnrA (n=6) were commonly noted with the co-production of β-lactamases and PMQR in ten (37%) isolates. More than 50% of the isolates were devoid of the tested acquired genes. Conclusion: The study concludes that superbugs dominate, with limited occurrence of plasmid-borne markers in this geographic location.

Background and Aim: Lipopolysaccharides (LPS) from Salmonella typhi will attach with Toll-Like Receptor 4 (TLR-4) and trigger an inflammatory response to fight the pathogen. Due to infection, the HMGB1 is produced by immune cells or secreted passively from dead cells. Fur-thermore, the antimicrobial peptide, cathelicidin was secreted to neutralize and eliminate these path-ogens. This study aims to examine the interaction of Cathelicidin antimicrobial peptide (CAMP), TLR-4, and HMGB-1 on inhibiting bacterial growth in Salmonella infection. Methods: This study is an experiment that uses a pre-post-test design. Mice balb/c were separated into three groups; group A received levofloxacin for five days, group B received a placebo, and group C was the control. Both groups, A and B, received an injection of S. Typhi strain thy1. Blood samples were taken from three groups on the 4th, 10th, and 30th day to calculate CAMP, TLR-4, and HMGB-1 mRNA gene expression levels. To determine bacterial colony, peritoneal fluid was taken three times on the 4th, 10th, and 30th day to calculate bacterial colony. Results: Our finding observed that the expression of mRNA CAMP was inversely related to bacte-rial colony count, which means that higher CAMP mRNA expression was associated with reduced bacterial colony count in groups A and B. The expression of HMGB-1 mRNA was found to be positively correlated with bacterial growth in group A. Meanwhile, TLR-4 mRNA expression did not significantly correlate with bacterial colony count in any groups. method: This study is an experiment that uses a pre-post-test design. Mice balb/c were separated into three groups; group A received levofloxacin for five days, group B received a placebo, and group C was the control. Both groups, A and B, received an injection of S. Typhi strain thy1. Blood samples were taken from three groups on the 4th, 10th, and 30th day to calculate CAMP, TLR-4, and HMGB-1 mRNA gene expression levels. To determine bacterial colony, peritoneal fluid was taken three times on the 4th, 10th, and 30th day to calculate bacterial colony. Conclusions: CAMP, TLR-4, and HMGB-1 affect bacterial infections. Higher expression CAMP mRNA levels lower colony counts. Meanwhile, decreasing TLR-4 and HMGB-1 mRNA expression were found during the study, due to reducing growth bacteria. result: The expression of mRNA CAMP and bacterial colony count correlated negatively. The expression of HMGB-1 mRNA correlated with bacterial growth. Higher CAMP mRNA expression was found to relate to reduced bacterial colony count in groups A and B using linear regression.

Background: Herpes simplex Virus type 1 (HSV-1) is a contagious human pathogen causing severe infection. In recent decades, the virus has become dormant and resistant to available treatment creating the need for the development of new therapeutic agents against it. Benzotriazole is a versatile molecule with a wide range of activities like antibacterial, antiprotozoal, antiulcer, anthelmintic, and antiproliferative activity. Methods: A series of 2-(1H- benzotriazole-1-yl) N- substituted acetohydrazide derivatives were synthesized using the method given in the literature. The derivatives were obtained in good yield and characterized by spectral methods of analysis. The antiviral activity against the glycoprotein B of Herpes Simplex Virus-I (HSV-I) was determined using molecular docking (2GUM). Result: All compounds had strong binding affinity over the standard Acyclovir. Compound 5h had the highest binding affinity and the highest inhibitory activity. Conclusion: The Benzotriazole-N- substituted acetohydrazide derivatives has the highest bind-ing affinity and good inhibition of glycoprotein B of Herpes Simplex Virus-I (HSV-I), which makes it a good antiviral agent.

Background: Test substrates are routinely used in laboratories to test the efficacy of various reactions, and while many substrates have found success as test substrates, not much is known about their potential intrinsic properties. On that note, some bromoaniline compounds were synthesized and repurposed by studying their antibacterial activity. Methods: The in-vitro antibacterial tests were done against S. aureus, K. pneumoniae, B. subtilis, and E. coli. Tests were carried out to understand the mode of action of the compounds where changes in permeability and integrity of cell membrane resulting in the leakage of UV absorbing materials were observed. Computational studies were performed by employing density functional theory (DFT) in the Gaussian09 software for determining the reactivity of the studied compounds. Molecular docking studies were executed to define the interaction of the synthesized compounds with microbial target proteins, Dihydrofolate reductase (PDB ID: 3SRW) and DNA gyrase subunit B (PDB ID: 1KZN). Results: The compound’s response to the mode of action tests showed alteration in the membrane permeability and its antimicrobial effectiveness at different pH contributed it to being a potential antibiotic. The results of DFT studies revealed that the molecular descriptors indicate better reactivity of compound 8b which is in agreement with the experiments performed. Molecular docking studies revealed that interactions of the compounds at the active sites of target proteins depict that the compounds are likely to bind to the protein enhancing their potential as antibacterial agents. Conclusions: This work concludes that simple molecules synthesized effortlessly through a simple and environmentally benign pathway, can pose as a good therapeutic agent

Background: Heterocyclic scaffolds have gained exceptional devotion in the recent years due to their marked utility in bio-organic field. Among these, pyrazole remains a privileged scaffold as broad array of medicinally active agents encompasses this heterocycle as a core nucleus. Pyrazole is a five-membered, aromatic ring containing two nitrogen atoms at adjacent positions are readily able to show interactions with numerous receptor (s), enzymes located on the target cells in biological system. Pyrazole-containing compounds are acknowledged with anticyclooxygenases (anti-inflammatory), carbonic anhydrase inhibitor, α-glycosidase inhibitor, and cholinesterase enzymes inhibitor and anti-DNA gyrases activities. Noticeably, rimonabant, phenylbutazone, fipronil, difenamizole, celecoxib, antipyrine, fezolamide and betazole are few representatives of pyrazole containing drugs. Objectives: The manuscript aims to review the detailed synthetic approaches applied for the synthesis of pyrazole derivatives. In particular, we examine recent scientific finding on antimicrobial, anti-tubercular, antiviral, anticancer and anti-inflammatory perspectives of pyrazole containing analogues. Methods: Pyrazole analogues have been widely explored by scientific community as large number of papers has been published in this regard. Numerous pyrazole-containing analogues have been designed, synthesized, and screened for their in vitro and in vivo bio-efficacy and many of them endowed with commendable pharmacological activities. Pyrazole analogues with superior applications as antiviral, anticancer, and anti-inflammatory efficacy have also been well documented in patents granted to this heterocyclic nucleus. Results: This review outlines the recent advances in medicinal chemistry of pyrazole analogues with a special emphasize of structure-activity relationships to afford ideas for the rational drug-design and discovery and their impact on desired pharmacological applications. Conclusion: The information provided in this manuscript may help the medicinal chemists to generate robust pyrazole analogues with high efficacy.

Abstract: Pests, such as cockroaches, thrive in polluted conditions that are detrimental to Homo sapiens, suggesting that such species possess mechanisms to protect them-selves against pathogens. Besides their immunity to fight pathogens, we hypothesize that the microbial gut flora of pests produces antimicrobials to thwart communicable diseases. It is proposed that the search for new antimicrobials originating from unusual sources will generate useful leads in the identification of new anti-infective agents.

Background: Herbal medicines are one of the giant creations of nature. Several medicinal agents developed from natural sources, which open a new era of health sciences. Cassia sophera is a prevalent medicinal plant that is locally known as “Kasondi”, belonging to the family Caesalpinaceae. Many secondary metabolites like alkaloids, tannins, anthraquinones, flavonoids are isolated from roots, stems, leaves, flowers, and seeds of C. sophera, which are very effective against several diseases. Objective: Cassia sophera has an enormous potential in public health to protect from diabetes, microbes, and cancer. Hence, the aim of the present review is to collect the reported antidiabetic, antimicrobial, and anticancer activity of Cassia sophera along with a detailed discussion about mechanism of action of var-ious phytoconstituents. Discussion: Antidiabetic activity of Cassia sophera is due to the activation of β cell and stimulation of surviving pancreatic β-cells to release more insulin. Plasma membrane disruption, inhibition of cell wall formation, inhibition of cell division by the Cassia sophera is the prime causes of antimicrobial activity. The anticancer activity of the plant is mainly due to the prevention of reactive oxygen species formation, induction of cell cycle arrest, apoptosis, and angiogenesis. Conclusions: The findings from this review article confirm the potential activities and mechanisms of various phytoconstituents responsible for preventing diabetes, cancer, and microbial infections. Further investigation regarding possible pharmaceutical side effects, contraindications, drug interactions involv-ing drugs synthesized from C. sophera should be carried out by the researchers.