136816-99-4Relevant academic research and scientific papers
In vitro antibacterial and antifungal activity and computational evaluation of novel indole derivatives containing 4-substituted piperazine moieties
Altuntas, Tunca Gul,Y?lmaz, Nilüfer,Ece, Abdulilah,Altanlar, Nurten,?lgen, Süreyya
, p. 1079 - 1086 (2018/10/31)
Background: Lack of specificity and occurence of resistance to current antibacterial and antifungal agents are major shortcomings for the treatment of microbial diseases. Finding novel antimicrobial agents is therefore highly needed to develop more potent drugs. Within this framework, several indole derivatives were designed and reported in the literature. Methods: In vitro antibacterial and antifungal activities of previously synthesized novel indole compounds containing 4-substituted piperazine moieties were tested against Staphylococcus aureus (ATCC 25923), Methicilline resistant Staphylococcus aureus (MRSA, ATCC 43300), Escherichia coli (ATCC 25922), Bacillus subtilis (ATCC 6633) and Candida albicans (ATTC 10231). Sultamicillin T, ampicillin, ciprofloxacin and fluconazole were used as positive controls. Molecular docking was used to study the interaction of active compounds with their receptor. Results: Fifteen compounds were synthesized and their antibacterial activities were similar to that of the reference drugs used as controls. Compounds 4 and 15 were more active (MIC 25 μg/ml) than ampicillin (MIC 50 μg/ml) against MRSA, while they showed the same activity as sultamicillin T (MIC 25 μg/ml). All compounds showed lower activity than ciprofloxacin (MIC 25 μg/ml) against the tested microorganisms. However, none of the compounds showed remarkable antifungal activity against C. albicans. Conclusion: Compound 6 showed the best interaction with the amino acid residues of the targeted cofactor NAD+.
Synthesis and antioxidant activity of indole derivatives containing 4-substituted piperazine moieties
Altuntas, Tunca Gul,Yilmaz, Nilüfer,?oban, Tülay,?lgen, Süreyya
, p. 380 - 386 (2017/03/17)
Background: Oxidative stress caused by reactive oxygen species (ROS) plays a significant role in many human disorder such as cancer, rheumatoid arthritis, atherosclerosis, stroke, neurodegeneration, and diabetes as well as the process of aging. Compounds interfere with the action of ROS might be useful in prevention and treatment of these pathologies. Indole nucleus seems to protect the nervous system against oxidative stress. Methods: Herein, several indole compounds containing 4-substituted piperazine moieties were synthesized. Compounds 1, and 4-15 were obtained by amidification reaction using 1,1'-carbonyldiimidazole (CDI) and compounds 2 and 3 were obtained by the reaction of amine and substituted chloropyridine ring using potassium carbonate. Antioxidant activities of compounds were determined by in vitro lipid peroxidation levels on rat liver, superoxide formation and 2,2-diphenyl-1-picrylhydrazyl (DPPH) stable radical scavenging activities in comparison with vitamine E (α-tocopherol). Results: The results indicated that compounds 6 (75%), 7 (66%), 8 (75%), 11 (88%), and 12 (69%) showed strong inhibiory effects on superoxide radical formation compare to vitamine E (62%). Compound 11 can be considered as the most active one among them. Compound 10 (38%) showed slight activity in lipid peroxidation inhibition assay. Compounds are not good inhibitor of DPPH except compound 10, which has also slight inhibition (20%).
Anti-aids piperazines
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, (2008/06/13)
The present invention includes diaromatic substituted heterocyclic compounds (III) STR1 which are useful in treating individuals infected with the HIV virus. The invention includes certain previously generically disclosed anti-AIDS piperazinyl compounds (V) and a method of treating HIV infected individuals with the indoles of formula (V) and the anti-AIDS amines (X).
Discovery, synthesis, and bioactivity of bis(heteroaryl)piperazines. 1. A novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors
Romero,Morge,Biles,Berrios-Pena,May,Palmer,Johnson,Smith,Busso,Tan,Voorman,Reusser,Althaus,Downey,So,Resnick,Tarpley,Aristoff
, p. 999 - 1014 (2007/10/02)
A variety of analogues of 1-[4-methoxy-3,5-dimethylbenzyl]-4-[3- (ethylamino)-2-pyridyl]piperazine hydrochloride (U-80493E) were synthesized and evaluated for their inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). Replacement of the substituted aryl moiety with various substituted indoles provided bis(heteroaryl)piperazines (BHAPs) that were 10-100-fold more potent than U-80493E. The pyridyl portion of the lead molecule was found to be very sensitive to modifications. Extensive preclinical evaluations of several of these compounds led to the selection of 1-[(5-methoxyindol-2-yl)carbonyl]-4-[3-(ethylamino)-2- pyridyl]piperazine methanesulfonate (U-87201E, atevirdine mesylate) for clinical evaluation.
