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REPORT - Synthesis of promising antibacterial and antifungal agents: 2-[[(4-Chlorophenyl)sulfonyl](2,3-dihydro-1,4-benzodioxin-6-yl)amino]-N-(un/substituted-phenyl)acetamides

Abbasi MA, Irshad M, Aziz-Ur-Rehman -, Siddiqui SZ, Nazir M, Ali Shah SA, et al.

Pak J Pharm Sci, 2020 Sep;33(5):2161-2170.
PMID: 33824125

In the presented work, 2,3-dihydro-1,4-benzodioxin-6-amine (1) was reacted with 4-chlorobenzenesulfonyl chloride (2) in presence of aqueous basic aqueous medium to obtain 4-chloro-N-(2,3-dihydro-1,4-benzodioxin-6-yl)benzenesulfonamide (3). In parallel, various un/substituted anilines (4a-l) were treated with bromoacetyl bromide (5) in basified aqueous medium to obtain corresponding 2-bromo-N-(un/substituted)phenylacetamides (6a-l) as electrophiles. Then the compound 3 was finally reacted with these electrophiles, 6a-l, in dimethylformamide (DMF) as solvent and lithium hydride as base and activator to synthesize a variety of 2-[[(4-chlorophenyl)sulfonyl](2,3-dihydro-1,4-benzodioxin-6-yl)amino]-N-(un/substituted)phenylacetamides (7a-l). The synthesized compounds were corroborated by IR, 1H-NMR and EI-MS spectral data for structural confirmations. These molecules were then evaluated for their antimicrobial and antifungal activities along with their %age hemolytic activity. Some compounds were found to have suitable antibacterial and antifungal potential, especially the compound 2-[[(4-chlorophenyl)sulfonyl](2,3-dihydro-1,4-benzodioxin-6-yl)amino]-N-(3,5-dimethylphenyl)acetamide (7l) exhibited good antimicrobial potential with low value of % hemolytic activity.

Matched MeSH terms: Fungi/drug effects
Fulltext Bacterial and fungal keratitis in Upper Egypt: in vitro screening of enzymes, toxins and antifungal activity

Gharamah AA, Moharram AM, Ismail MA, Al-Hussaini AK

Indian J Ophthalmol, 2014 Feb;62(2):196-203.
PMID: 24008795 DOI: 10.4103/0301-4738.116463

This work was conducted to study the ability of bacterial and fungal isolates from keratitis cases in Upper Egypt to produce enzymes, toxins, and to test the isolated fungal species sensitivity to some therapeutic agents.

Matched MeSH terms: Fungi/drug effects
Fulltext Antimicrobial and antioxidant activities of new metal complexes derived from 3-aminocoumarin

Kadhum AA, Mohamad AB, Al-Amiery AA, Takriff MS

Molecules, 2011 Aug 15;16(8):6969-84.
PMID: 21844844 DOI: 10.3390/molecules16086969

3-Aminocoumarin (L) has been synthesized and used as a ligand for the formation of Cr(III), Ni(II), and Cu(II) complexes. The chemical structures were characterized using different spectroscopic methods. The elemental analyses revealed that the complexes where M=Ni(II) and Cu(II) have the general formulae [ML(2)Cl(2)], while the Cr(III) complex has the formula [CrL(2)Cl(2)]Cl. The molar conductance data reveal that all the metal chelates, except the Cr(III) one, are non-electrolytes. From the magnetic and UV-Visible spectra, it is found that these complexes have octahedral structures. The stability for the prepared complexes was studied theoretically using Density Function Theory. The total energy for the complexes was calculated and it was shown that the copper complex is the most stable one. Complexes were tested against selected types of microbial organisms and showed significant activities. The free radical scavenging activity of metal complexes have been determined by measuring their interaction with the stable free radical DPPH and all the compounds have shown encouraging antioxidant activities.

Matched MeSH terms: Fungi/drug effects*
Chemical compositions, antioxidant and antimicrobial activity of the essential oils of Piper officinarum (Piperaceae)

Salleh WM, Ahmad F, Yen KH, Sirat HM

Nat Prod Commun, 2012 Dec;7(12):1659-62.
PMID: 23413576

This study was designed to investigate the antioxidant and antimicrobial activities of the essential oils from Piper officinarum C. DC. GC and GC/MS analysis of the leaf and stem oils showed forty one components, representing 85.6% and 93.0% of the oil, respectively. The most abundant components in the leaf oil were beta-caryophyllene (11.2%), alpha-pinene (9.3%), sabinene (7.6%), beta-selinene (5.3%) and limonene (4.6%), while beta-caryophyllene (10.9%), alpha-phellandrene (9.3%), linalool (6.9%), limonene (6.7%) and alpha-pinene (5.0%) were the main components of the stem oil. The antioxidant activities were determined by using complementary tests: namely beta-carotene-linoleic acid, DPPH radical scavenging and total phenolic assays. The stems oil showed weak activity (IC50 = 777.4 microg/mL) in the DPPH system, but showed moderate lipid peroxidation inhibition in the beta-carotene-linoleic acid system (88.9 +/- 0.35%) compared with BHT (95.5 +/- 0.30%). Both oils showed weak activity against P. aeruginosa and E. coli with M IC values of 250 microg/mL.

Matched MeSH terms: Fungi/drug effects
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: Fungi/drug effects
Biogenic approach to synthesize rod shaped Gd2 O3 nanoparticles and its optimization using response surface methodology-Box-Behnken design model

Surendra TV, Mohana Roopan S, Khan MR

Biotechnol Prog, 2019 07;35(4):e2823.
PMID: 31017346 DOI: 10.1002/btpr.2823

The rare earth metal oxide nanoparticles such as gadolinium oxide nanoparticles (Gd2 O3 NPs) have been synthesized by green synthesis process using methanolic extract of Moringa oleifera (M oleifera) peel. In this process, the Gd2 O3 NPs formation was observed at 280-300 nm in UV-Vis spectroscopy. The XRD pattern of the synthesized Gd2 O3 NPs was exactly matched with JCPDS No 3-065-3181which confirms the crystalline nature of Gd2 O3 NPs. In addition, Energy-dispersive X-ray spectroscopy (EDX) analysis was stated that Gd and O elements were present as 70.31 and 29.69%, respectively in Gd2 O3 NPs. The SEM and TEM analysis were said Gd2 O3 NPs are in rod shape and 26 ± 2 nm in size. Further the synthesized Gd2 O3 NPs were confirmed by X-ray photoemission spectroscopy (XPS). The synthesized Gd2 O3 NPs were further examined for anti-fungal activity against Alternaria saloni (A saloni) and Sclerrotium rolfsii (S rolfsii) and it showed moderate activity. Also, Gd2 O3 NPs evaluated as good antibacterial agent against different Gram +ve and Gram -ve bacteria. Moreover, the toxicity of the Gd2 O3 NPs on red blood cells (RBCs) of the human blood was determined using hemolytic assay, the obtained results were stated the synthesized Gd2 O3 NPs are nontoxic to the human erythrocytes. The photocatalytic activity against malachite green (MG) dye was tested and confirmed as 92% of dye was degraded within 2 hr by Gd2 O3 NPs. The results were stated the green synthesized Gd2 O3 NPs are good anti-fungal agents, nontoxic and we can use as a photocatalyst. Copyright © 2019 John Wiley & Sons, Ltd.

Matched MeSH terms: Fungi/drug effects
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: Fungi/drug effects
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: Fungi/drug effects
2-Mercaptobenzimidazole Schiff Bases: Design, Synthesis, Antimicrobial Studies and Anticancer Activity on HCT-116 Cell Line

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

Mini Rev Med Chem, 2019;19(13):1080-1092.
PMID: 30306865 DOI: 10.2174/1389557518666181009151008

BACKGROUND: Increased rate of mortality due to the development of resistance to currently available antimicrobial and anticancer agents initiated the need to develop new chemical entities for the treatment of microbial infections and cancer.
OBJECTIVE: The present study was aimed to synthesize and evaluate antimicrobial and anticancer activities of Schiff bases of 2-mercaptobenzimidazole.
METHODS: The Schiff bases of 2-mercaptobenzimidazole were synthesized from 4-(2-(1H-benzo[d]- imidazol-2-ylthio)acetamido)benzohydrazide. The synthesized compounds were evaluated for antimicrobial and anticancer activities by tube dilution method and Sulforhodamine-B (SRB) assay, respectively.
RESULTS: Compounds 8 (MICpa, an = 2.41, 1.20 µM/ml), 10 (MICse, sa = 2.50 µM/ml), 20 (MICec = 2.34 µM/ml) and 25 (MICca = 1.46 µM/ml) showed significant antimicrobial activity against tested bacterial and fungal strains and compounds 20 (IC50 = 8 µg/ml) and 23 (IC50 = 7 µg/ml) exhibited significant anticancer activity.
CONCLUSION: In general, the synthesized derivatives exhibited moderate antimicrobial and anticancer activities. Compounds 8 and 25 having high antifungal potential among the synthesized compounds may be taken as lead molecules for the development of novel antifungal agents.

Matched MeSH terms: Fungi/drug effects
Chemical characterization and antimicrobial activity of rhizome essential oils of very closely allied Zingiberaceae species endemic to Borneo: Alpinia ligulata K. Schum. and Alpinia nieuwenhuizii Val

Yusoff MM, Ibrahim H, Hamid NA

Chem Biodivers, 2011 May;8(5):916-23.
PMID: 21560240 DOI: 10.1002/cbdv.201000270

Two poorly studied, morphologically allied Alpinia species endemic to Borneo, viz., A. ligulata and A. nieuwenhuizii, were investigated here for their rhizome essential oil. The oil compositions and antimicrobial activities were compared with those of A. galanga, a better known plant. A fair number of compounds were identified in the oils by GC-FID and GC/MS analyses, with large differences in the oil composition between the three species. The rhizome oil of A. galanga was rich in 1,8-cineole (29.8%), while those of A. ligulata and A. nieuwenhuizii were both found to be extremely rich in (E)-methyl cinnamate (36.4 and 67.8%, resp.). The three oils were screened for their antimicrobial activity against three Gram-positive and three Gram-negative bacteria and two fungal species. The efficiency of growth inhibition of Staphylococcus aureus var. aureus was found to decline in the order of A. nieuwenhuizii>A. ligulata ∼ A. galanga, while that of Escherichia coli decreased in the order of A. galanga>A. nieuwenhuzii ∼ A. ligulata. Only the A. galanga oil inhibited the other bacteria and the fungi tested.

Matched MeSH terms: Fungi/drug effects
Chemical constituents and antimicrobial activity of the leaf and rhizome oils of Alpinia pahangensis Ridl., an endemic wild ginger from peninsular Malaysia

Awang K, Ibrahim H, Rosmy Syamsir D, Mohtar M, Mat Ali R, Azah Mohamad Ali N

Chem Biodivers, 2011 Apr;8(4):668-73.
PMID: 21480512 DOI: 10.1002/cbdv.201000225

The essential oils from the leaves and rhizomes of Alpinia pahangensis Ridl., collected from Pahang, Peninsular Malaysia, were obtained by hydrodistillation, and their chemical compositions were determined by GC and GC/MS analyses. The major components of the rhizome oil were γ-selinene (11.60%), β-pinene (10.87%), (E,E)-farnesyl acetate (8.65%), and α-terpineol (6.38%), while those of the leaf oil were β-pinene (39.61%), α-pinene (7.55%), and limonene (4.89%). The investigation of the antimicrobial activity of the essential oils using the broth microdilution technique revealed that the rhizome oil of A. pahangensis inhibited five Staphylococcus aureus strains with minimum inhibitory concentration (MIC) values between 0.08 and 0.31 μg/μl, and four selected fungi with MIC values between 1.25 and 2.50 μg/μl.

Matched MeSH terms: Fungi/drug effects