scholarly journals Biological Activity of Phenothiazine Sulfonamides

Background: Antibacterial activities in “dimethylsulfoxide (DMSO)” were executed by the broth dilution method utilizing nutrient agar. By using the agar cup bioassay method antifungal activities were calculated with “Clotrimazole” as the standard. The novel compounds 1a-j have been evaluated in vitro for their antibacterial activity by “Gram-positive bacteria namely Bacillus subtilis, Bacillus sphaericus and Staphylococcus aureus and three Gram-negative bacteria Pseudomonas aeruginosa”, “Klebsiella aerogenes and Chromobacterium violaceum”. All ten compounds were analysed for their antifungal activity against five test “organisms Aspergillus niger, Chrysosporium tropicum, Rhizopus oryzae, Fusarium moniliforme and Curvularia lunata”. Among the isolated compounds 1d and 1e evinced dynamic Movement towards both gram certain What's more gram negative microscopic organisms. Mixes 1d Also 1f uncovered useful antifungal action. All the secluded compounds were scrutinized for their antibacterial and antifungal activities and most of the compounds manifested remarkable anti bacterial and anti fungal activity.

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4391
Author(s):  
Lingling Xiao ◽  
Lu Yu ◽  
Pei Li ◽  
Jiyan Chi ◽  
Zhangfei Tang ◽  
...  

In this study, using the botanical active component thiochromanone as the lead compound, a total of 32 new thiochromanone derivatives containing a carboxamide moiety were designed and synthesized and their in vitro antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo), Xanthomonas oryzae pv. oryzicolaby (Xoc), and Xanthomonas axonopodis pv. citri (Xac) were determined, as well as their in vitro antifungal activities against Botryosphaeria dothidea (B. dothidea), Phomopsis sp., and Botrytis cinerea (B. cinerea). Bioassay results demonstrated that some of the target compounds exhibited moderate to good in vitro antibacterial and antifungal activities. In particular, compound 4e revealed excellent in vitro antibacterial activity against Xoo, Xoc, and Xac, and its EC50 values of 15, 19, and 23 μg/mL, respectively, were superior to those of Bismerthiazol and Thiodiazole copper. Meanwhile, compound 3b revealed moderate in vitro antifungal activity against B. dothidea at 50 μg/mL, and the inhibition rate reached 88%, which was even better than that of Pyrimethanil, however, lower than that of Carbendazim. To the best of our knowledge, this is the first report on the antibacterial and antifungal activities of this series of novel thiochromanone derivatives containing a carboxamide moiety.


2017 ◽  
Vol 82 (2) ◽  
pp. 127-139 ◽  
Author(s):  
Satbir Mor ◽  
Rajni Mohil ◽  
Savita Nagoria ◽  
Ashwani Kumar

A series of sixteen 1-(4-arylthiazol-2-yl)-1?-(aryl/heteroaryl)-3,3?-dimethyl-[ 4,5?-bi-1H-pyrazol]-5-ols (7a?p) was synthesized starting from dehydroacetic acid (DHA, 1) via the stepwise formation of thiosemicarbazone (2), 3-(1-(2-(4-arylthiazol-2-yl)hydrazono)ethyl)-4-hydroxy-6-methyl-2H-pyran- -2-ones (4a?d) and 1-(1-(4-arylthiazol-2-yl)-5-hydroxy-3-methyl-1H-pyrazol- -4-yl)butane-1,3-diones (5a?d) in high yields. The in vitro antibacterial and antifungal activities of the synthesized bipyrazoles 7a?p were investigated against two Gram-positive bacterial strains, viz. Bacillus subtilis (MTCC 441) and Staphylococcus aureus (MTCC 7443), one Gram-negative bacterial strain, viz. Escherichia coli (MTCC 42), and two fungal strains, viz. Candida albicans (MTCC 183) and Aspergillus niger (MTCC 282). The compounds 7a and 7e were found to exhibit better inhibitory activity against A. niger than the reference fluconazole. Moreover, the antifungal activities of the title compounds were more prolific than their antibacterial activities. Furthermore, in order to study binding interactions, docking simulations of compounds 7a, 7m and 7o were performed into the active site of S. aureus 1,4-dihydroxy-2-naphthoyl- -CoA synthase. Keywords: bipyrazoles; antibacterial; antifungal; docking simulations.


2014 ◽  
Vol 60 (2) ◽  
pp. 29-40 ◽  
Author(s):  
Ömer Ertürk

Abstract In this study the antibacterial and antifungal activities of extracted Achillea latiloba Ledeb. ex Nordm (Asteraceae) samples in acetone, ethyl acetate, ethanol, methanol and dimethyl sulfoxide (DMSO) from Trabzon Province (Turkey) were investigated. Antimicrobial activity of A. latiloba varied depending on the extract of samples, dosage of extracts, and the extraction solvents for all test microorganisms. Staphylococcus aureus, Streptococcus salivarius, Klebsiella pneumoniae, Escherichia coli, Salmonella enteritidis, Streptococcus pneumoniae, Bacillus cereus, Listeria monocytogenes, Streptococcus mutans, Pseudomonas aeruginosa, Bacillus licheniformis, Micrococcus luteus, Bacillus subtillis, Proteus vulgaris and Candida albicans were studied with use of disc diffusion and agar dilution method. The results indicated that each of the crude extracts of Achillea latiloba exhibited a more or less pronounced antibacterial and antifungal potency both in Gram-positive and Gram-negative bacteria and fungi. While in the Gram-negative group, the most sensitive microorganism to Achillea latiloba were S. enteritidis and Streptococcus mutans which is Gram-positive. In the Gram-positive group, the microorganisms most sensitive to Achillea latiloba were Streptococcus mutans and L. monocytogenes. However, the least sensitive microorganism was P. vulgaris. The results presented in this paper suggest that Achillea latiloba possesses additional antimicrobial activities that has an effect against some Gram-negative, Gram-positive bacteria and fungi.


2021 ◽  
Vol 43 (5) ◽  
pp. 578-578
Author(s):  
Khalil Ahmad Khalil Ahmad ◽  
Habib ur Rehman Shah Habib ur Rehman Shah ◽  
Areeba Ashfaq Areeba Ashfaq ◽  
Muhammad Ashfaq Muhammad Ashfaq ◽  
Muhammad Kashif Muhammad Kashif ◽  
...  

In this study, In Vitro antibacterial and antifungal activities of azo series based on transition metal complexes (Cu2+, Zn2+, Mn2+, Co2+ and Ni2+) with already our reported ligands named as; [(E)-1-(1, 3-dioxolan-2-yl)-2-phenyldiazene] (K-1), [(E)-1-(1, 3-dioxolan-2-yl)-2-(4-methylphenyl)diazene] (K-2), 2-[(E)-phenyl diazenyl]-1H-benzimidazole] (K-3), [(E)-1-(1, 3-dioxolan-2-yl)-2-(4-ethylphenyl)diazene] (K-4), and [(E)-1-(1, 3-dioxolan-2-yl)-2-(2-methylphenyl)-diazene] (K-5) were studied. FTIR 1H-NMR and mass spectrometric techniques were applied for interpretation of synthesized complexes. 4.05-4.07 ppm chemical shift appearance of azo group confirms azo coupling with transition metal complexes. N=N, C-H, C-N and C-O groups are also confirmed by FTIR which exhibited peaks at 1400-1500, 2090-3090, 1100-1180, 1010-1060 and 625-780 cm-1. Furthermore, mass spectroscopic data also gives strong indication for the synthesis of metal complexes. All the newly synthesized complexes were screened for their antibacterial and antifungal activities. Antibacterial and antifungal activity against S. aureus, E.coli and A.niger, A.ustus and C.albican at conc. 250 and#181;g/ml showed excellent activity by K-1 complexes (Co2+, Cu2+, Ni2+), K-5 complexes (Zn2+, Mn2+, Cu2+), K-2 complexes (Co2+, Cu2+, Mn2+) and K-3 (Zn2+, Mn2+, Co2+, Cu2+) as compared to standard drug (Ampicillin). Hence, based on this study, it was concluded that these azo based complexes may act as a platform for designing more active antibacterial and antifungal agents.


2006 ◽  
Vol 1 (4) ◽  
pp. 348-355 ◽  
Author(s):  
S. Subramania ◽  
D. Sathish Kumar . ◽  
P. Arulselvan . ◽  
G.P. Senthilkumar .

Author(s):  
Sudip Kumar Mandal

 Objective: The wide variety of biological activities of different indane derivatives makes them an interesting moiety in the field of medicinal chemistry. The objective of the study was to identify and develop novel antimicrobial agents from indanyl analogs.Methods: Recently synthesized indanyl analogs (4a-c and 5a-o) were examined against various pathogenic microorganisms (Gram-positive and Gram-negative bacteria and fungi) using serial dilution method. These analogs were found to possess antibacterial and antifungal activities with minimum inhibitory concentration values ranging between 1.56 and 100 μg/mL.Results: The results revealed that the entire compounds showed mild-to-moderate antibacterial activities and moderate-to-excellent antifungal activities against the pathogenic microorganisms as compared to the standard drugs ciprofloxacin and fluconazole, respectively. Compounds 4a, 5a, 5b, 5d, 5e, 5i, and 5j exhibited antifungal activities superior to the reference drug.Conclusion: Based on the structure-activity relationship, it can conclude that the indan-3-oxo-1-acetic acid moiety is essential for the activities and lipophilic alkoxy substituents on indane ring have enhanced the biological activity. Further, structure-activity relationship studies of the compounds 4a, 5a, and 5b are needful to find the new lead as antimicrobial agent.


Sign in / Sign up

Export Citation Format

Share Document