Background
The emergence of bacterial resistance is a major public health problem. It is essential to develop and synthesize new therapeutic agents with better activity. The mode of actions of ...certain newly developed antimicrobial agents, however, exhibited very limited effect in treating life threatening systemic infections. Therefore, the advancement of multi-potent and efficient antimicrobial agents is crucial to overcome the increased multi-drug resistance of bacteria and fungi. Cancer, which remains as one of the primary causes of deaths and is commonly treated by chemotherapeutic agents, is also in need of novel and efficacious agents to treat resistant cases. As such, a sequence of novel substituted benzamides was designed, synthesized and evaluated for their antimicrobial and anticancer activities.
Methodology
All synthesized compounds were characterized by IR, NMR, Mass and elemental analysis followed by in vitro antimicrobial studies against Gram-positive (
Staphylococcus aureus
), Gram-negative (
Salmonella typhi
and
Klebsiella pneumoniae
) bacterial and fungal (
Candida albicans
and
Aspergillus niger
) strains by the tube dilution method. The in vitro anticancer evaluation was carried out against the human colorectal carcinoma cell line (HCT116), using the Sulforhodamine B assay.
Results, discussion and conclusion
Compound
W6
(MIC
sa, st, kp
= 5.19 µM) emerged as a significant antibacterial agent against all tested bacterial strains
i.e.
Gram-positive (
S. aureus
), Gram-negative (
S. typhi, K. pneumoniae
) while compound
W1
(MIC
ca, an
= 5.08 µM) was most potent against fungal strains (
A. niger
and
C. albicans
) and comparable to fluconazole (MIC = 8.16 µM). The anticancer screening demonstrated that compound
W17
(IC
50
= 4.12 µM) was most potent amongst the synthesized compounds and also more potent than the standard drug 5-FU (IC
50
= 7.69 µM).
Background
Dihydrofolate reductase (DHFR) is an important target for antimetabolite class of antimicrobials because it participates in purine synthesis. 2-mercaptobenzimidazole (2MBI) has similar ...structural features as purine nucleotides. Given that benzimidazole and similar heteroaromatics have been broadly examined for their anticancer potential, so, we hereby report the design, synthesis and biological studies (i.e. antimicrobial and anticancer studies) of 2MBI derivatives.
Methodology
The antimicrobial activity of synthesized 2MBI derivatives were evaluated against Gram positive and Gram negative bacterial species as well as fungal species by tube dilution technique whereas their anticancer activity was assessed against human colorectal carcinoma cell line (HCT116) by Sulforhodamine B (SRB) assay. They were also structurally characterized by IR, NMR, MS and elemental analyses.
Results, discussion and conclusion
The antimicrobial activity findings revealed that compound
N1
(MIC
bs,st,
ca
= 1.27, 2.54, 1.27 µM),
N8
(MIC
ec
= 1.43 µM),
N22
(MIC
kp,an
= 2.60 µM),
N23
and
N25
(MIC
sa
= 2.65 µM) exhibited significant antimicrobial effects against tested strains, i.e. Gram-positive, Gram-negative (bacterial) and fungal strains. The anticancer screening results demonstrated that compounds
N9
,
N18
(IC
50
= 5.85, 4.53 µM) were the most potent compounds against cancer cell line (HCT116) even more than 5-FU, the standard drug (IC
50
= 9.99 µM).
Background
Nitrogen containing heterocycles are widely used and investigated by pharmaceutical industry, as they are important in discovery and designing of new drug molecules. Drugs with a ...benzimidazole nucleus possess exclusive structural features and electron-rich atmosphere, which enable them to bind to a number of biologically important targets and result in a wide range of activities. This has served as the basis of the present study whereby new scaffolds with benzimidazole moiety were designed and synthesized.
Methods
The structures of synthesized compounds were confirmed by physicochemical and spectral means. The synthesized compounds were screened for their antimicrobial and antiproliferative activities by tube dilution and Sulforhodamine B (SRB) assays, respectively.
Results and conclusion
The in vitro biological screening results revealed that compound
Z24
exhibited promising antimicrobial and anticancer activities which are comparable to standards.
A series of 1,2,4-triazole derivatives (1–17) was synthesized and evaluated for its antimicrobial and anticancer potentials. Antimicrobial screening of the synthesized compounds indicated that they ...were most potent against Aspergillus niger and compound 14 was found to be the most active. Compound 7 showed appreciable anticancer activity against HCT 116, a colon cancer cell line. QSAR analysis indicated the importance of topological parameter, valence third order molecular connectivity index (3χv) and electronic parameter, dipole moment (μ) in describing the antimicrobial activity of the synthesized compounds.
•Brief overview of chalcones and their importance in medicinal chemistry.•Chalcones are the molecules composed of three-carbon, unsaturated carbonyl system connecting two aromatic rings.•Chalcone ...exhibit a wide range of biological activities such as antihypertensive, antimicrobial, anticancer, anti-diabetic, anti-ulcer, antiviral, antioxidant, anti-inflammatory, anti-gout, anti-angiogenic and antimalarial.•Butein, Xanthohumol, Isoliquiritigenin, Cardamonin, licochalcone, Metochalcone, sofalcone, Hesperidin trimethylchalcone and hesperidin methylchalcone are some Chalcone containing drugs.•Discussion of various methods for synthesizing chalcone derivatives.•Synthesized mostly by Claisen-Schmidt Condensation mechanism using strong acid/base.•Exploration of potential applications and future directions in drug development.•Summary of key findings and contributions from the review.•Emphasis on the significance of chalcone derivatives in drug discovery and development.
Chalcones (1, 3-diaryl-2-propen-1-ones), a class of organic compounds known for their distinctive chemical structure and remarkable pharmacological properties, have garnered significant attention in the fields of medicinal chemistry and drug development. Chalcones are versatile molecules containing open chain flavonoids composed of three-carbon, unsaturated carbonyl system connecting two aromatic rings. Chalcone group containing compounds are promising synthons and bioactive scaffolds of great medicinal interest and demonstrated a wide range of biological activities, including antioxidant, anti-inflammatory, anticancer, antimicrobial, and more. Their mechanisms of action involve modulation of various cellular pathways, making them valuable assets in the quest for novel therapeutics. Additionally, the abundance of chalcone precursors in nature aligns with the growing emphasis on sustainable and eco-friendly drug development. This review synthesizes the extensive research on chalcones, highlighting their significance as a rich source of potential drug agent and their pivotal role in the development of innovative therapies across various medical disciplines.
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A new series of pyrazole derivatives was synthesized and its chemical structure was confirmed by physicochemical and spectral means. The synthesized compounds were evaluated for their in vitro ...antimicrobial, antioxidant, antidiabetic and anti-inflammatory activities. The antimicrobial results showed that, compounds Intermediate 1 (MICbs= 14.74µM), P10 (MICkp=12.95 µM), P14 (MICsa=16.26 µM), P19 (MICec=17.34 µM), and P20 (MICst=12.41 µM) shown significant antibacterial activity, but compound P7 (MICca= 13.19 µM) and Intermediate 5 (MICan= 17.29 µM) shown significant antifungal activitywhen compared to standard medications. Compound P4 had the highest level of antioxidant potential (IC50 = 52.21 µM), whereas Compound P12 demonstrated the highest level of antidiabetic potential (IC50 = 38.00 µM). Compound P2 has excellent potency against inflammation, with IC50 values 29.55 µM. Further, the molecular docking study has been carried to find out the interaction between active pyrazole compounds with 4FFW, 2CDU and IFJ4 (PDB id) indicated that compound P12, P4 and P10 showed good docking score with better potency within the ATP binding pocket respectively and may be used as a lead for rational drug designing of the novel molecules.To get more light on the regioselective synthesis of new hybrid compounds, mechanistic studies were performed using DFT calculations with B3LYP/6–31G(d,p) basis set.
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Benzimidazole is a heterocyclic moiety whose derivatives are present in many of the bioactive compounds and posses diverse biological and clinical applications. Benzimidazole agents are the vital ...pharmacophore and privileged sub-structures in chemistry of medicine. They have received much interest in drug discovery because benzimidazoles exhibited enormous significance. So attempts have been made to create repository of molecules and evaluate them for prospective inherent activity. They are extremely effective both with respect to their inhibitory activity and favorable selectivity ratio.
Benzimidazole is most promising category of bioactive heterocyclic compound that exhibit a wide variety of biological activities in medicinal field. The present review only focus on antimicrobial activity of reported benzimidazole derivatives may serve as valuable source of information for researchers who wish to synthesize new molecules of benzimidazole nucleus which have immense potential to be investigated for newer therapeutic possibilities.
Heterocyclic compounds are inevitable in a numerous part of life sciences. These molecules perform various noteworthy functions in nature, medication and innovation. Nitrogen-containing heterocycles ...exceptionally azoles family are the matter of interest in synthesis attributable to the way that they happen pervasively in pharmacologically dynamic natural products, multipurpose arranged useful materials also profoundly powerful pharmaceuticals and agrochemicals. Benzimidazole moiety is the key building block for several heterocyclic scaffolds that play central role in the biologically functioning of essential molecules. They are considered as promising class of bioactive scaffolds encompassing diverse varieties of activities like antiprotozoal, antihelminthic, antimalarial, antiviral, anti-inflammatory, antimicrobial, anti-mycobacterial and antiparasitic. Therefore in the present review we tried to compile the various pharmacological activities of different derivatives of heterocyclic benzimidazole moiety.
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