Original Scientific Article Synthesis and In vitro Antimicrobial Activity of Novel (original) (raw)
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A new series of 2-[4-(4-substitutedbenzamido/ phenylacetamido)phenyl] benzothiazole derivatives (6a–k) were synthesized and evaluated for antibacterial and antifungal activities against Staphylococcus aureus, Bacillus subtilis, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Escherichia coli with their drug-resistant isolates and a yeast Candida albicans. Microbiological results indicated that the compounds possessed a broad spectrum of activity against the tested microorganisms at minimum inhibitory concentration (MIC) values between 100 and 6.25 lg/ml. Compounds 6d and 6k exhibited significant antibacterial activity showing 6.25 lg/ml MIC values against drugresistant S. aureus and P. aeruginosa isolates, respectively.
A new series of 2-[4-(4-substitutedbenzamido / phenylacetamido / phenylpropionamido) benzyl / phenyl]benzothiazole derivatives (6a−6w) were synthesized and evaluated for antibacterial and antifungal activities against Staphylococcus aureus, Bacillus subtilis, Klebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli with their drug-resistant isolates and a yeast Candida albicans. Microbiological results indicated that the compounds possessed a broad spectrum of activity against the tested microorganisms at MIC values between 200 and 6.25 µg/ml. Compounds 6e and 6j exhibited the greatest activity with MIC values of 6.25 µg/ml against Pseudomonas aeruginosa, and Staphylococcus aureus isolate, respectively.(doi: 10.5562/cca2064)
Il Farmaco, 2000
The synthesis of some N-(o-hydroxyphenyl)benzamides and benzacetamides (2a-2p) in order to determine their in vitro antimicrobial activity against two Gram-positive bacteria, three Gram-negative bacteria and the fungus Candida albicans is described. The new compounds were compared with several control drugs. The derivative 2g, 4-amino-N-(o-hydroxyphenyl)benzamide, was found active at an MIC value of 25 mg/ml against the Gram-negative microorganism Klebsiella pneumoniae. Most of the compounds exhibited antibacterial activity at an MIC value of 25 mg/ml against Pseudomonas aureginosa. For the antifungal activity against C. albicans, compounds 2e, 2h and 2m were found more active than the other derivatives (MIC 12.5 mg/ml). The antimicrobial activity of some of these benzamide and phenylacetamide derivatives , possible metabolites of benzoxazoles, was also compared with that of the cyclic analogues 3-8. Compound 2f possesses two dilutions better antifungal activity than its cyclic analogue the benzoxazole derivative 5 against C. albicans, while having one dilution better antibacterial activity against Streptococcus faecalis and K. pneumoniae.
2010
Benzothiazole are important group of compounds repo rt d to have various biological activities and hence the present study was undertaken in order to synthesize same new compounds built upon this nucleus with the hope to enhance the biol ogical properties of newly designed compounds. In the present work 2-substituted benzot hiazole (a) was prepared from p-tolnidine via cyclization reaction then N-2-benzothiazolyl th iourea was synthesized by reacting (a) with ammonium thiocyanate. Then its semicarbazide deriva tive was formed reacting with hydrazine hydrate in ethylene glycol which was reacted with v arious acetophenons to form respective derivatives. Chemical structure of product and thei r purity was ascertained by TLC, MP and various spectral methods as FTIR and NMR. The inhib tion of microorganism under standard condition was determined to demonstrate antimicrobi al activity of derivatives using gram positive and gram negative bacteria such as St phylococcus aureus, Pseudomonas....
Antibiotics
In this manuscript, we describe the design, preparation, and studies of antimicrobial activity of a series of novel heteroarylated benzothiazoles. A molecular hybridization approach was used for the designing compounds. The in vitro evaluation exposed that these compounds showed moderate antibacterial activity. Compound 2j was found to be the most potent (MIC/MBC at 0.23–0.94 mg/mL and 0.47–1.88 mg/mL) On the other hand, compounds showed good antifungal activity (MIC/MFC at 0.06–0.47 and 0.11–0.94 mg/mL respectively) with 2d being the most active one. The docking studies revealed that inhibition of E. coli MurB and 14-lanosterol demethylase probably represent the mechanism of antibacterial and antifungal activities.
International Journal of Pharmacy and Pharmaceutical Sciences, 2015
Objective: Synthesis, characterization and antimicrobial evaluation of some new 1,3-benzothiazolyl pyrazole derivatives. Methods: Aseries of novel2-[3-(substituted phenyl)-4-formylpyrazol-1-yl]-6-chloro benzothiazole derivatives (5a-g) have been synthesized by cyclization through Vilsmeier-Haack reaction on hydrazones (4a-g)of substituted aromatic ketones with 6-chloro benzothiazol-2-yl hydrazine under microwave irradiation in fairly good yields. All the newly synthesized compounds were characterized by IR, 1 Results: The results revealed that all 1,3-benzothiazole pyrazole derivatives(5a-g) were synthesized in satisfactory yields and pharmacologically evaluated for their in vitro antimicrobial activity. All the synthesized compounds were in good agreement with elemental and spectral data. Some of the tested compounds showed good to moderate antimicrobial activity against all tested pathogenic bacterial and fungal strains. HNMR, Mass spectral studies and elemental analysis and were screened for their in vitro antibacterial and antifungal activities also. Conclusion: For the present investigation we have prepared benzothiazole derivatives that are incorporated with pyrazolyl moiety with the hope of potentiating the activity of two such units in the same compound. Compounds 5b, 5c, and 5a showed excellent antibacterial and antifungal activities as compared to reference drugs norfloxacin and ketoconazole.
Synthesis and evaluation of some new benzothiazole derivatives as potential antimicrobial agents
European Journal of Medicinal Chemistry, 2010
As benzothiazole has proven to be good antimicrobial agent, a novel series of Schiff bases of benzothiazole derivatives were synthesized. Thus condensation of 5-[2-(1,3-benzothiazol-2-yl-amino) ethyl]-4-amino-3-mercapto-(4H)-1,2,4-triazole 5 with appropriate aromatic aldehydes afforded 5-[2-(1,3benzothiazol-2-yl-amino)ethyl]-4-(arylideneamino)-3-mercapto-(4H)-1,2,4-triazoles 6aeg. Structures of the synthesized compounds were elucidated on the basis of elemental analyses and spectral data. All the synthesized compounds were screened for their antimicrobial activity.
2017
S N H 2 N OCH 3 + S N OCH 3 NH C N S N Ar N NH Ar (3) (4) (5a-5h) A new series of N-(6-methoxybenzo[d]thiazol-2-yl)-2-substituted phenyl-1H-benz[d]imidazole-1-carbothioamide derivatives (5a-5h) has been synthesized and evaluated for antibacterial, antifungal and antimalarial effects. All these compounds were characterized and screened for their in vitro antimicrobial activity against selected bacterial and fungal strains. Titled compounds were also evaluated for their antimalarial activity against P. falciparum. Antimicrobial activity screening results showed that some compounds namely 5b against P. aeruginosa, 5c against S. aureus and E. coli, 5d against E. coli and P. aeruginosa and 5g against E. coli from the series have emerged as prospective antibacterial leads endowed with excellent activity (MIC 12.5-62.5 μg/ml). While only one fungal strain C. albicans was susceptible towards synthesized compounds. On the other hand, compounds 5c and 5h exhibited noteworthy antimalarial acti...
International Journal of Pharmacy and Pharmaceutical Sciences, 2016
Objective: A new series of 2-{4-(t-amino)-2-(but-2-yn-1-yl)}-1,3-benzothiazole derivatives, 2-[4-(pyrrolidin-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ2), 2-[4-(2-methylpiperidin-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ3), 2-[4-(piperidin-1-yl) but-2-yn-1-yl]-1,3-benzothiazole (BZ4), 2-[4-(azepan-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ5), 2-[4-(4-methylpiperazin-1-yl) but-2-yn-1-yl]-1,3-benzothiazole (BZ6), 2-[4-(2, 6dimethylpiperidin-1-yl) but-2-yn-1-yl]-1, 3-benzothiazole (BZ7) were synthesized and screened in vitro as potential antimicrobial agents. Methods: In-vitro antimicrobial activity evaluation was done, by agar diffusion method and broth dilution test against Staphylococcus aureus ATCC 6538p, Candida albicans ATCC 10231, Pseudomonas aeruginosa ATCC 9027, Escherichia coli ATCC 8739, and Bacillus subtilis ATCC 6633. Minimum inhibitory concentration (MIC) and Minimum bactericidal concentration (MBC) were determined. The results of antimicrobial testing were compared to two positive control drugs ciprofloxacin (5 µg/ml) and fluconazole (500µg/ml). Results: Compound 2-[4-(azepan-1-yl) but-2-yn-1-yl]-1,3-benzothiazole (BZ5) showed the highest antibacterial activity against S. aureus with MIC value of 15.62 µg/ml while; Compound 2-[4-(2,6-dimethylpiperidin-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ7) exhibited the highest antibacterial activity against P. aeruginosa with MIC value of 31.25 µg/ml. Compounds 2-[4-(pyrrolidin-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ2) and 2-[4-(azepan-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ5) showed the highest antifungal activity against C. albicans with MIC value of 15.62 µg/ml (for both). Conclusion: The results obtained showed variation in the antibacterial and antifungal activity based on the structure of the cyclic amines in these amino acetylenic benzothiazole derivatives.