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Design, Synthesis, and Antimicrobial Evaluation of 1,4-dihydroindeno[1,2-]pyrazole Tethered Carbohydrazide Hybrids: Exploring Their ADMET, Ergosterol Inhibition and ROS Inducing Potential

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Journal Medchemcomm
Specialty Chemistry
Date 2019 Jun 14
PMID 31191871
Citations 4
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Abstract

A series of new 1,4-dihydroindeno[1,2-]pyrazole tethered carbohydrazide hybrids () were designed, synthesized and evaluated for their antimicrobial activity. Compounds , , , and demonstrated significant activity against the entire panel of test pathogens. Further, compounds and exhibited significant anti- activity. These potential hybrids ( and ) also exhibited promising ergosterol biosynthesis inhibition against , which was further validated through molecular docking studies. Furthermore, compounds and caused intracellular ROS accumulation in MTCC 3017 and were non-toxic to normal human lung cell line MRC5. studies revealed that they demonstrated drug likeness and an appreciable pharmacokinetic profile. Overall, the findings demonstrate that and may be considered as promising leads for further development of new antifungal drugs.

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References
1.
Kamal A, Ali Hussaini S, Sucharitha M, Poornachandra Y, Sultana F, Kumar C . Synthesis and antimicrobial potential of nitrofuran-triazole congeners. Org Biomol Chem. 2015; 13(36):9388-97. DOI: 10.1039/c5ob01353d. View

2.
Kathiravan M, Salake A, Chothe A, Dudhe P, Watode R, Mukta M . The biology and chemistry of antifungal agents: a review. Bioorg Med Chem. 2012; 20(19):5678-98. DOI: 10.1016/j.bmc.2012.04.045. View

3.
Dutta S, Basu S, Sen K . Binding of diclofenac sodium with bovine serum albumin at different temperatures, pH and ionic strengths. Indian J Exp Biol. 2006; 44(2):123-7. View

4.
Saint S, Chenoweth C . Biofilms and catheter-associated urinary tract infections. Infect Dis Clin North Am. 2003; 17(2):411-32. DOI: 10.1016/s0891-5520(03)00011-4. View

5.
Daina A, Michielin O, Zoete V . SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules. Sci Rep. 2017; 7:42717. PMC: 5335600. DOI: 10.1038/srep42717. View