Synthesis and biological investigations of some novel thiazolylbenzimidazoles, and benzimidazolyl-thiazolo[4,5-d]pyrimidines (original) (raw)
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2013
We have synthesized a series of α bromoketones& thiadiazole with various benzimidazoles. The compounds were confirmed by physical parameters (solubility, melting point), chromatographic methods (TLC) and at last spectroscopic methods (IR, NMR). Since our titled compounds are known to possess antimicrobial activity, the compounds were screened for their antibacterial and antifungal activity by cup-plate method. All the benzimidazole substituted thiadiazole derivatives (B1,B2,B and B4) showed significant activities compared to the standards ciprofloxacin for significant activity against E.coli,andS.aureusat 50, 100,300 and 500 mcg/ml and Miconazole significant activity againstCandida albicansat 50, 100, 300,500 mcg/ml. The benzimidazole showed mild antibacterial activities and significant antifungal activities.
2017
A series of novel 5-amino-1,3,4-thiadiazole-2-thiol and 1,3,4-thiadiazole-2,5-dithiol derivatives of benzimidazole were synthesized through nucleophilic substitution reaction of 5-substituted-2-(chloromethyl)-1H-benzimidazole, structures of the synthesized compounds were proved by spectral methods of analysis ( FT-IR, 1H and 13C NMR ). All the target compounds were screened for their antibacterial activity toward gram-negative (E.coli, P. aeruginosa) and Gram-positive (B. subtilis, S. aureus) bacteria, most of the synthesized derivatives exhibited good to moderate activity toward both Gram-positive (B. subtilis, S. aureus) and Gram-negative (E.coli, P. aeruginosa) bacteria.
Pharmaceutical Chemistry Journal, 2014
The aim of this study was to describe the synthesis of four new 2-(3,4-diphenyl-3H-thiazol-2-ylidene)amino-4,6-dimethylpyrimidine derivatives, which were screened for their anticandidal activity and cytotoxicity. The title compounds (2a -2d) were synthesized via the reaction of 1-phenyl-3-(4,6-dimethylpyrimidin-2-yl)thiourea with phenacyl bromides. Anticandidal activity of the synthesized compounds was evaluated using microbroth dilution method. All compounds were also investigated for their cytotoxic effects on A549 and NIH3T3 cell lines. Compound 2c can be considered as the most promising anticandidal agent due to its inhibitory effects on Candida albicans, C. glabrata, C. tropicalis with a MIC value of 125 mg/mL and low toxicity to NIH3T3 cells (IC 50 = 193.32 mg/mL). Although compound 2a was the most effective derivative against A549 cells with an IC 50 value of 0.0623 mM, it is not a good candidate for cancer treatment because of its high toxicity against NIH3T3 cells (IC 50 = 0.00316 mM).
Synthesis of some novel 2,4-disubstituted thiazoles as possible antimicrobial agents
European Journal of Medicinal Chemistry, 2008
A series of novel 4-aryl/chloroalkyl-2-(2,3,5-trichlorophenyl)-1,3-thiazoles (5a–g and 7a–e) were synthesized by condensing 2,3,5-trichlorobenzenecarbothioamide with phenacyl bromide/dichloroacetone. 2,3,5-Trichlorobenzaldehyde thiosemicarbazone on treatment with phenacyl bromide afforded 4-aryl-2-(2,3,5-trichlorophenylidenehydrazino)-1,3-thiazoles (10a–g) in good yield. The newly synthesized compounds are characterized by IR, 1H NMR and mass spectral studies. These compounds were also screened for their antibacterial and antifungal activities. Preliminary results reveal that some of the synthesized compounds are showing promising antimicrobial activity.Some novel 1,3-thiazoles containing 2,3,5-trichlorophenyl moiety were prepared by the reaction of various substituted phenacyl bromides and 1,3-dichloroacetone. The newly synthesized compounds were characterized by IR, 1H NMR and mass spectral studies. These compounds were also screened for their antibacterial and antifungal activities. Preliminary result reveals that some of the synthesized compounds showed promising antimicrobial activity.
Medicinal Chemistry Research, 2015
A series of new (E)-2-(5-substituted benzylidene-2,4-dioxothiazolidin-3-yl)-N-(6-thiocyanatobenzo[d]thiazol-2-yl)acetamides have been synthesized. The structures of title compounds have been confirmed by elemental analyses, IR, 1 H NMR and 13 C NMR spectral data. All the synthesized compounds were tested for antimicrobial and antitubercular activity and also were evaluated for anti-HIV activity. Several compounds exhibited good antibacterial activity (9, 15, 27 and 31 against E. coli; 8 and 28 against S. aureus); some displayed good antifungal activity (4, 7, 19, 23, 24, 25 and 31 against C. albicans). Compounds 14, 20 and 22 showed good antitubercular activity. Unfortunately, none of the compounds were found to be active against anti-HIV-1. However, one of the intermediates, the 2-chloro-N-(6-thiocyanatobenzo[d]thiazol-2-yl)acetamide, showed significant cytotoxicity for MT-4 cells (CC 50 = 8.0 lM).
International Journal of Research in Advent Technology
The newly synthesized biologically active series of 2-(benzo[d]thiazol-2-ylthio)ethanethioyl)-2-(substituted)benzylidenehydrazinecarbonothioamide 6a-6f were prepared. These compounds synthesized from 1,3 benzothiazole-2-thiol, Thiosemicarbazide (TSC) and chloroaylchloride (CAC) were crucial functionalities containing the wide variety of biological activities and have a broad range of therapeutic properties. The structure of the synthesized compounds was confirmed by spectral data and evaluated for their in vitro antibacterial activities against Gram-positive and Gram-negative bacteria and antifungal index terms-1,3 benzothiazole-2-thiol, 2-Mercaptobenzothiazole, Thiosemicarbazide, Antibacterial, Antifungal.