New 6‐(4‐Bromophenyl)‐imidazo[2,1‐b]thiazole Derivatives: Synthesis and Antimicrobial Activity.

Ulusoy, Nuray; Kiraz, Mehmet Sabır; Kuecuekbasmaci, Oemer

doi:10.1002/chin.200308120

Cited by 8 publications

(8 citation statements)

References 1 publication

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In continuation of our previous studies on the biological properties of imidazo [2,1-b]thiazole derivatives, [21][22][23][24][25][26][27] in this study, we reported the antibacterial, antitubercular and antiviral activity evaluation of some arylidenehydrazide derivatives bearing imidazo [2,1-b]thiazole moiety. …”

Section: Introductionmentioning

confidence: 71%

Antibacterial, Antitubercular and Antiviral Activity Evaluations of Some Arylidenehydrazide Derivatives Bearing Imidazo[2,1-<i>b</i>]thiazole Moiety

Güzeldemirci

Karaman

Küçükbasmacı

2017

tjps

View full text Add to dashboard Cite

ÖZObjectives: The aim of this study was to determine the probable antibacterial, antitubercular, and antiviral activities of some N 2 -arylidene-(6-(4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl) acetic acid hydrazides (3a-j). Further structural optimization of the identified lead structures can lead us to new more active potential antibacterial, antitubercular, and antiviral agents. Materials and Methods:Antibacterial activities of the title compounds against Staphylococcus aureus ATCC 29213, Pseudomonas aeruginosa ATCC 27853 and Escherichia coli ATCC 25922. These molecules were also evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv (ATCC 27294) using the BACTEC 460 radiometric system and BACTEC 12B medium. Moreover, all the compounds (3a-j) were also evaluated against some DNA and RNA viruses in Madin-Darby Canine Kidney, Crandell-Rees Feline Kidney (CRFK), Vero, human embryonic lung (HEL) and HeLa cells. Results:Among the tested compounds, 3i displayed the highest efficacy against S. aureus and E. coli. Compound 3j, 5-nitro-2-furfurylidene derivative showed the highest antituberculosis activity (IC 50 : 6.16 μg/mL and IC 90 : 14.390 μg/mL). Compound 3i showed the most potent antiviral activity against feline corona virus in CRFK cell cultures (antiviral EC 50 : 7.5 μM and SI>13). Furthermore, compounds 3c and 3g displayed activity against herpes simplex virus-1 and vaccinia virus in HEL cell cultures (antiviral EC 50 values of 9; 16 and 20; 14 μM, respectively). Conclusion:On the basis of aforementioned results, it can be conluded that imidazo[2,1-b]thiazole derivatives bearing hydrazone moieties serve as promising chemical probes to design therapeutic agents with antibacterial, antitubercular, and antiviral properties.

show abstract

Section: Introductionmentioning

confidence: 71%

Antibacterial, Antitubercular and Antiviral Activity Evaluations of Some Arylidenehydrazide Derivatives Bearing Imidazo[2,1-<i>b</i>]thiazole Moiety

Güzeldemirci

Karaman

Küçükbasmacı

2017

tjps

View full text Add to dashboard Cite

show abstract

“…These effects limit significantly application of some drugs and lead to the development of novel drugs. Thiazole derivatives have attracted the interest of medicinal chemists due to a variety of their biological activities including antibacterial, anti-fungal, anti-HIV, anti-hypertension, anti-inflammatory, anti-cancer, anti-convulsive and anti-depressant [5][6][7][8][9][10]. The mechanisms of 1,3-thiazole derivatives antitumor activity may be associated with DNA intercalation [11,12], PRL-3, SHP-2 and JSP-1 inhibition [13][14][15][16], tumor necrosis factor (TNFα) [17], anti-apoptotic bio-complex Bcl-XL-BH3 [18], integrin avb3 [19], others.…”

Section: Introductionmentioning

confidence: 99%

Antineoplastic activity of novel thiazole derivatives

Finiuk¹,

Hreniuh²,

Ostapiuk³

et al. 2017

Biopolym. Cell

View full text Add to dashboard Cite

The development of novel efficient substances for anticancer chemotherapy is an important problem of medicinal chemistry. Aim. To evaluate the level of cytotoxic action of novel thiazole derivatives towards tumor cell lines of different origin. Methods. Four N acylated 2-amino-5-benzyl-1,3-thiazoles (5a-d) were synthesized by reaction of 2-amino-5-R-benzyl-1,3-thiazoles with acid chlorides in the presence of triethylamine in the dioxane medium. Anticancer screening of the synthesized thiazoles was performed by the MTT assay. Results. Thiazole derivatives were shown to exert antineoplastic activity towards different types of tumor cells. The anti-glioma and anti-melanoma selectivity of these derivatives action was demonstrated. The compound 5a was found to be the most toxic for human glioblastoma U251 cells and human melanoma WM793 cells. At the same time, the created compounds possessed low toxicity towards pseudo-normal cells. Conclusion. The novel thiazole derivative 5a was the most toxic against human glioblastoma and melanoma cells. K e y w o r d s: thiazole derivatives, 2-amino-5-benzyl-1,3-thiazoles, anticancer activity, leukemia, glioblastoma, melanoma.

show abstract

“…The 2-amino-1,3-thiazoles are biologically important compounds with a wide range of medicinal and biological applications including antibacterial, antifungal, anti-HIV, anti-hypertension, antiinflammatory, anticancer, anticonvulsant, and antidepressant [1][2][3][4][5][6]. Some 2-amino-1,3-thiazole derivatives have been reported as ligands of thrombopoietin [7,8], neuropeptide Y5 [9] and adenosine receptors [10,11] and as inhibitors of several physiological important enzymes like cyclindependant kinase [12], poly (ADP-Ribose) polymerase [13], urokinase [14] etc.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis and Docking Studies of Novel 1, 2, 3-Triazolyl Phenylthiazole Analogs as Potent Anti-HIV-1 NNRT Inhibitors

Kasralikar¹,

Jadhavar²,

Bhansali³

et al. 2017

Med chem

View full text Add to dashboard Cite

In an attempt to design and synthesize a new class of anti-HIV-1 RTIs i.e., 4-(phenyl)-N,N-bis((1-phenyl-1H-1,2,3-triazol-4-yl)methyl)thiazol-2-amine derivatives, substituted 2-amino-4-phenylthiazoles were alkylated with propargyl bromide to obtain dialkyne 2-amino-4-phenylthiazoles. This dialkyne 2-amino-4-phenylthiazole was reacted with aryl azides to generate small library of 15 compounds (4a-o) by click chemistry. The obtained derivatives were studied for as an anti-HIV-1 NNRT Inhibitors. All synthesized compounds of 1,2,3-triazolylphenylthiazole series were be docked into the non-nucleoside inhibitor binding pocket (NNIBP) of HIV-1 RT and highly inhibiting derivatives studied for in vitro anti-HIV-1 assay.

show abstract

New 6‐(4‐Bromophenyl)‐imidazo[2,1‐b]thiazole Derivatives: Synthesis and Antimicrobial Activity.

Cited by 8 publications

References 1 publication

Antibacterial, Antitubercular and Antiviral Activity Evaluations of Some Arylidenehydrazide Derivatives Bearing Imidazo[2,1-<i>b</i>]thiazole Moiety

Antibacterial, Antitubercular and Antiviral Activity Evaluations of Some Arylidenehydrazide Derivatives Bearing Imidazo[2,1-<i>b</i>]thiazole Moiety

Antineoplastic activity of novel thiazole derivatives

Design, Synthesis and Docking Studies of Novel 1, 2, 3-Triazolyl Phenylthiazole Analogs as Potent Anti-HIV-1 NNRT Inhibitors

Contact Info

Product

Resources

About