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Designing Functiona...
Designing Functionally Substituted Pyridine-Carbohydrazides for Potent Antibacterial and Devouring Antifungal Effect on Multidrug Resistant (MDR) Strains
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- Khan, Farooq-Ahmad (author)
- Univ Karachi, Third World Ctr Sci & Technol, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.;Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.
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- Yaqoob, Sana (author)
- Univ Karachi, Third World Ctr Sci & Technol, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.;Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.
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- Ali, Shujaat (author)
- Univ Karachi, Third World Ctr Sci & Technol, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.;Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.
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- Tanveer, Nimra (author)
- Univ Karachi, Third World Ctr Sci & Technol, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.;Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.
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- Wang, Yan (author)
- Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.
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- Ashraf, Sajda (author)
- Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.
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- Hasan, Khwaja Ali (author)
- Univ Karachi, Dept Biochem, Mol & Struct Biol Res Lab, Karachi 75270, Pakistan.
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- Khalifa, Shaden A. M. (author)
- Stockholms universitet,Institutionen för molekylär biovetenskap, Wenner-Grens institut,Stockholm Univ, Wenner Gren Inst, Dept Mol Biosci, S-10691 Stockholm, Sweden.
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- Shou, Qiyang (author)
- Zhejiang Chinese Med Univ, Clin Med Coll 2, Hangzhou 310053, Peoples R China.
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- Ul-Haq, Zaheer (author)
- Univ Karachi, Dr Panjwani Ctr Mol Med & Drug Res, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.
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- Jiang, Zi-Hua (author)
- Lakehead Univ, Dept Chem, 955 Oliver Rd, Thunder Bay, ON P7B 5E1, Canada.
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- El-Seedi, Hesham (author)
- Uppsala universitet,Institutionen för farmaceutisk biovetenskap,Jiangsu Univ, Int Res Ctr Food Nutr & Safety, Zhenjiang 212013, Peoples R China.;Jiangsu Univ, Jiangsu Educ Dept, Int Joint Res Lab Intelligent Agr & Agriprod Proc, Nanjing 210024, Peoples R China.,Farmakognosi
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Univ Karachi, Third World Ctr Sci & Technol, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan;Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan. Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan. (creator_code:org_t)
- 2022-12-26
- 2023
- English.
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In: Molecules. - : MDPI. - 1431-5157 .- 1420-3049. ; 28:1
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Abstract
Subject headings
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- The emergence of multidrug-resistant (MDR) pathogens and the gradual depletion of available antibiotics have exacerbated the need for novel antimicrobial agents with minimal toxicity. Herein, we report functionally substituted pyridine carbohydrazide with remarkable antimicrobial effect on multi-drug resistant strains. In the series, compound 6 had potent activity against four MDR strains of Candida spp., with minimum inhibitory concentration (MIC) values being in the range of 16-24 mu g/mL and percentage inhibition up to 92.57%, which was exceptional when compared to broad-spectrum antifungal drug fluconazole (MIC = 20 mu g/mL, 81.88% inhibition). Substitution of the octyl chain in 6 with a shorter butyl chain resulted in a significant anti-bacterial effect of 4 against Pseudomonas aeruginosa (ATCC 27853), the MIC value being 2-fold superior to the standard combination of ampicillin/cloxacillin. Time-kill kinetics assays were used to discern the efficacy and pharmacodynamics of the potent compounds. Further, hemolysis tests confirmed that both compounds had better safety profiles than the standard drugs. Besides, molecular docking simulations were used to further explore their mode of interaction with target proteins. Overall results suggest that these compounds have the potential to become promising antimicrobial drugs against MDR strains.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)
Keyword
- multidrug resistance
- MDR strains
- antibiotics resistance
- antimicrobial
- pyridine
Publication and Content Type
- ref (subject category)
- art (subject category)
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Khan, Farooq-Ahm ...
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Yaqoob, Sana
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Ali, Shujaat
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Tanveer, Nimra
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Wang, Yan
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Ashraf, Sajda
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show more...
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Hasan, Khwaja Al ...
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Khalifa, Shaden ...
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Shou, Qiyang
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Ul-Haq, Zaheer
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Jiang, Zi-Hua
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El-Seedi, Hesham
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MEDICAL AND HEAL ...
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Molecules
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Uppsala University
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Stockholm University