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Design, Synthesis, SAR Study, Antimicrobial and Anticancer Evaluation of Novel 2-Mercaptobenzimidazole Azomethine Derivatives

Tahlan S, Narasimhan B, Lim SM, Ramasamy K, Mani V, Shah SAA

Mini Rev Med Chem, 2020;20(15):1559-1571.
PMID: 30179132 DOI: 10.2174/1389557518666180903151849

BACKGROUND: Various analogues of benzimidazole are found to be biologically and therapeutically potent against several ailments. Benzimidazole when attached with heterocyclic rings has shown wide range of potential activities. So, from the above provided facts, we altered benzimidazole derivatives so that more potent antagonists could be developed. In the search for a new category of antimicrobial and anticancer agents, novel azomethine of 2-mercaptobenzimidazole derived from 3-(2- (1H-benzo[d]imidazol-2-ylthio)acetamido)benzohydrazide were synthesized.
RESULTS AND DISCUSSION: The synthesized analogues were characterized by FT-IR, 1H/13C-NMR and MS studies as well C, H, N analysis. All synthesized compounds were evaluated for in vitro antibacterial activity against Gram-positive (B. subtilis), Gram-negative (E. coli, P. aeruginosa, K. pneumoniae and S. typhi) strains and in vitro antifungal activity against C. albicans and A. niger strains by serial dilution method, the minimum inhibitory concentration (MIC) described in μM/ml. The in vitro anticancer activity of synthesized compounds was determined against human colorectal carcinoma cell line (HCT- 116) using 5-fluorouracil as standard drug.
CONCLUSION: In general, most of the synthesized derivatives exhibited significant antimicrobial and anticancer activities. Compounds 8, 10, 15, 16, 17, 20 and 22 showed significant antimicrobial activity towards tested bacterial and fungal strains and compound 26 exhibited significant anticancer activity.

Matched MeSH terms: Anti-Infective Agents/chemical synthesis*
Design, Synthesis and Therapeutic Potential of Some 6, 6'-(1,4- phenylene)bis(4-(4-bromophenyl)pyrimidin-2-amine)analogues

Kumar S, Narasimhan B, Lim SM, Ramasamy K, Mani V, Shah SAA

Mini Rev Med Chem, 2019;19(7):609-621.
PMID: 30526456 DOI: 10.2174/1389557519666181210162413

BACKGROUND: A series of 6, 6'-(1,4-phenylene)bis(4-(4-bromophenyl)pyrimidin-2-amine) derivatives has been synthesized by Claisen-Schmidt condensation and its chemical structures was confirmed by FT-IR, 1H/13C-NMR spectral and elemental analyses. The molecular docking study was carried out to find the interaction between active bis-pyrimidine compounds with CDK-8 protein. The in vitro antimicrobial potential of the synthesized compounds was determined against Gram-positive and Gram-negative bacterial species as well fungal species by tube dilution technique. Antimicrobial results indicated that compound 11y was found to be most potent one against E. coli (MICec = 0.67 µmol/mL) and C. albicans (MICca = 0.17 µmol/mL) and its activity was comparable to norfloxacin (MIC = 0.47 µmol/mL) and fluconazole (MIC = 0.50 µmol/mL), respectively.
CONCLUSION: Anticancer screening of the synthesized compounds using Sulforhodamine B (SRB) assay demonstrated that compounds 2y (IC50 = 0.01 µmol/mL) and 4y (IC50= 0.02 µmol/mL) have high antiproliferative potential against human colorectal carcinoma cancer cell line than the reference drug (5- fluorouracil) and these compounds also showed best dock score with better potency within the ATP binding pocket and may also be used lead for rational drug designing.

Matched MeSH terms: Anti-Infective Agents/chemical synthesis
Ameliorative effect of Albizia chinensis synthesized ZnO-NPs on Mycoplasma pneumoniae infected pneumonia mice model

Yu L, Lu M, Zhang W, Alarfaj AA, Hirad AH, Zhang H

Microb Pathog, 2020 Apr;141:103960.
PMID: 31953224 DOI: 10.1016/j.micpath.2019.103960

BACKGROUND: Mycoplasma pneumoniae (MP) is a common cause of community-acquired pneumonia (CAP) among the children and adults that results upper and lower respiratory tract infections.
OBJECTIVE: This study was aimed to inspect the ameliorative action of A. chinensis synthesized ZnONPs against M. pneumoniae infected pneumonia mice model.
MATERIALS AND METHODS: ZnO NPs was synthesized from Albizia chinensis bark extract and characterized by UV-Vis spectroscopy, Fourier Transform Infrared (FTIR), Transmission Electron Microscopy (TEM), energy dispersive X-ray (EDX) and atomic force microscope (AFM) analyses. The antibacterial effectual of synthesized ZnONPs were examined against clinical pathogens. The pneumonia was induced to BALB/c mice via injecting the M. pneumoniae and treated with synthesized ZnONPs, followed by the total protein content, total cell counts and inflammatory mediators level was assessed in the BALF of experimental animals. The Histopathological investigation was done in the lung tissues of test animals.
RESULTS: The outcomes of this work revealed that the formulated ZnONPs was quasi-spherical, radial and cylindrical; the size was identified as 116.5 ± 27.45 nm in diameter. The in vitro antimicrobial potential of formulated ZnO-NPs displayed noticeable inhibitory capacity against the tested fungal and bacterial strains. The administration of synthesized ZnO-NPs in MP infected mice model has significantly reduced the levels of total protein, inflammatory cells, inflammatory cytokines such as IL-1, IL-6, IL-8, tumour necrosis factor-alpha (TNF-a) and transforming growth factor (TGF). Besides, the histopathological examination of MP infected mice lung tissue showed the cellular arrangements were effectively retained after administration of synthesized ZnO-NPs.
CONCLUSION: In conclusion, synthesized ZnO-NPs alleviate pneumonia progression via reducing the level of inflammatory cytokines and inflammatory cells in MP infected mice model.

Matched MeSH terms: Anti-Infective Agents/chemical synthesis
Recent Update on the Anti-infective Potential of β-carboline Analogs

Faheem, Kumar BK, Sekhar KVGC, Kunjiappan S, Jamalis J, Balaña-Fouce R, et al.

Mini Rev Med Chem, 2021;21(4):398-425.
PMID: 33001013 DOI: 10.2174/1389557520666201001130114

β-Carboline, a naturally occurring indole alkaloid, holds a momentous spot in the field of medicinal chemistry due to its myriad of pharmacological actions like anticancer, antiviral, antibacterial, antifungal, antileishmanial, antimalarial, neuropharmacological, anti-inflammatory and antithrombotic among others. β-Carbolines exhibit their pharmacological activity via diverse mechanisms. This review provides a recent update (2015-2020) on the anti-infective potential of natural and synthetic β-carboline analogs focusing on its antibacterial, antifungal, antiviral, antimalarial, antileishmanial and antitrypanosomal properties. In cases where enough details are available, a note on its mechanism of action is also added.

Matched MeSH terms: Anti-Infective Agents/chemical synthesis