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27 results on '"Hong, Weiqian"'

9. A Phase 1, Randomized, Double‐Blind, Placebo‐Controlled, Single Ascending Dose Trial of AWZ1066S, an Anti‐Wolbachia Candidate Macrofilaricide.

Author

Devereux, Graham, Bula, Marcin, Tripp, Karen, Fitzgerald, Richard, Eraut, Nicola, Alam, Muhammad Salman, Moriyama, Tomoyuki, Shinkyo, Raku, Walker, Lauren, Wang, Duolao, Gusovsky, Fabian, van der Velde, Jeannette, Turner, Joseph D., Hong, Weiqian David, O'Neill, Paul M., Taylor, Mark J., and Ward, Stephen A.

Subjects
NEGLECTED diseases, LYMPHATIC diseases, ONCHOCERCIASIS, FILARIASIS, LIVER enzymes
Abstract

AWZ1066S has been developed as a potential treatment for the neglected tropical diseases lymphatic filariasis and onchocerciasis. AWZ1066S targets the Wolbachia bacterial endosymbiont present in the causative nematode parasites. This phase 1, first‐in‐human study aimed to assess the safety and pharmacokinetics of AWZ1066S in healthy human participants. In a randomized double‐blind, placebo‐controlled, single ascending dose study, healthy adults received a single oral dose of AWZ1066S (or placebo) and were followed up for 10 days. The planned single doses of AWZ1066S ranged from 100 to 1600 mg, and each dose was administered to a cohort of 8 participants (6 AWZ1066S and 2 placebo). In total 30 people participated, 18 (60%) female, median age 30.0 years (minimum 20, maximum 61). The cohorts administered 100, 200, 300, and 400 mg of AWZ1066S progressed unremarkably. After single 700‐mg doses all 4 participants developed symptoms of acute gastritis and transient increases in liver enzymes. The severity of these adverse events ranged from mild to severe, with 1 participant needing hospital admission. Pharmacokinetic analysis indicated that AWZ1066S is rapidly absorbed with predictable pharmacokinetics. In conclusion, safety concerns prevented this study from reaching the human exposures needed for AWZ1066S to be clinically effective against lymphatic filariasis and onchocerciasis. [ABSTRACT FROM AUTHOR]

Published
2024
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11. A Phase 1, Randomized, Double‐Blind, Placebo‐Controlled, Single Ascending Dose Trial of AWZ1066S, an Anti‐WolbachiaCandidate Macrofilaricide

Author

Devereux, Graham, Bula, Marcin, Tripp, Karen, Fitzgerald, Richard, Eraut, Nicola, Alam, Muhammad Salman, Moriyama, Tomoyuki, Shinkyo, Raku, Walker, Lauren, Wang, Duolao, Gusovsky, Fabian, Velde, Jeannette, Turner, Joseph D., Hong, Weiqian David, O'Neill, Paul M., Taylor, Mark J., and Ward, Stephen A.

Abstract

AWZ1066S has been developed as a potential treatment for the neglected tropical diseases lymphatic filariasis and onchocerciasis. AWZ1066S targets the Wolbachiabacterial endosymbiont present in the causative nematode parasites. This phase 1, first‐in‐human study aimed to assess the safety and pharmacokinetics of AWZ1066S in healthy human participants. In a randomized double‐blind, placebo‐controlled, single ascending dose study, healthy adults received a single oral dose of AWZ1066S (or placebo) and were followed up for 10 days. The planned single doses of AWZ1066S ranged from 100 to 1600 mg, and each dose was administered to a cohort of 8 participants (6 AWZ1066S and 2 placebo). In total 30 people participated, 18 (60%) female, median age 30.0 years (minimum 20, maximum 61). The cohorts administered 100, 200, 300, and 400 mg of AWZ1066S progressed unremarkably. After single 700‐mg doses all 4 participants developed symptoms of acute gastritis and transient increases in liver enzymes. The severity of these adverse events ranged from mild to severe, with 1 participant needing hospital admission. Pharmacokinetic analysis indicated that AWZ1066S is rapidly absorbed with predictable pharmacokinetics. In conclusion, safety concerns prevented this study from reaching the human exposures needed for AWZ1066S to be clinically effective against lymphatic filariasis and onchocerciasis.

Published
2024
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13. Novel Sophoridine Derivatives as Potential Larvicidal Agents against Aedes albopictus: Synthesis, Biological Evaluation, Acetylcholinesterase Inhibition, and Morphological Study

Author

Ang, Song, primary, Cao, Nana, additional, Zheng, Wende, additional, Zhang, Zhen, additional, Li, Jinxuan, additional, Yan, Zhenping, additional, Su, Kaize, additional, Wong, Wing-Leung, additional, Zhang, Kun, additional, Hong, Weiqian David, additional, and Wu, Panpan, additional

Published
2023
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14. Ligand and structure-based approaches for the exploration of structure–activity relationships of fusidic acid derivatives as antibacterial agents

Author

Zheng, Wende, primary, Tu, Borong, additional, Zhang, Zhen, additional, Li, Jinxuan, additional, Yan, Zhenping, additional, Su, Kaize, additional, Deng, Duanyu, additional, Sun, Ying, additional, Wang, Xu, additional, Zhang, Bingjie, additional, Zhang, Kun, additional, Wong, Wing-Leung, additional, Wu, Panpan, additional, Hong, Weiqian David, additional, and Ang, Song, additional

Published
2023
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15. Study of the Repellent Activity of 60 Essential Oils and Their Main Constituents against Aedes albopictus, and Nano-Formulation Development

Author

Wu, Weifeng, primary, Yang, Yu, additional, Feng, Yingmiao, additional, Ren, Xiaofei, additional, Li, Yuling, additional, Li, Wenjiao, additional, Huang, Jietong, additional, Kong, Lingjia, additional, Chen, Xiaole, additional, Lin, Zhongze, additional, Hou, Xiaohui, additional, Zhang, Longlai, additional, Chen, Yajie, additional, Sheng, Zhaojun, additional, and Hong, Weiqian, additional

Published
2022
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17. Synthesis and Biological Evaluation of Novel Fusidic Acid Derivatives as Two-in-One Agent with Potent Antibacterial and Anti-Inflammatory Activity

Author

Tu, Borong, primary, Cao, Nana, additional, Zhang, Bingjie, additional, Zheng, Wende, additional, Li, Jiahao, additional, Tang, Xiaowen, additional, Su, Kaize, additional, Li, Jinxuan, additional, Zhang, Zhen, additional, Yan, Zhenping, additional, Li, Dongli, additional, Zheng, Xi, additional, Zhang, Kun, additional, Hong, Weiqian David, additional, and Wu, Panpan, additional

Published
2022
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18. Larvicidal Activity of Two Rutaceae Plant Essential Oils and Their Constituents Against Aedes albopictus (Diptera: Culicidae) in Multiple Formulations

Author

Jian, Rongchao, primary, Lin, Yuan, additional, Li, Yuling, additional, Wu, Weifeng, additional, Ren, Xiaofei, additional, Liang, Zhanyuan, additional, Kong, Lingjia, additional, Cai, Jinglin, additional, Lao, Canyao, additional, Wu, Min, additional, Chen, Wenhua, additional, Chen, Jing, additional, Hong, Weiqian David, additional, and Sheng, Zhaojun, additional

Published
2022
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20. Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205

Author

Woodley, Christopher M., primary, Nixon, Gemma L., additional, Basilico, Nicoletta, additional, Parapini, Silvia, additional, Hong, Weiqian David, additional, Ward, Stephen A., additional, Biagini, Giancarlo A., additional, Leung, Suet C., additional, Taramelli, Donatella, additional, Onuma, Keiko, additional, Hasebe, Takashi, additional, and O’Neill, Paul M., additional

Published
2021
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21. Chemical Composition, Antimicrobial and Insecticidal Activities of Essential Oils of Discarded Perfume Lemon and Leaves (Citrus Limon (L.) Burm. F.) as Possible Sources of Functional Botanical Agents

Author

Wu, Panpan, primary, Tang, Xiaowen, additional, Jian, Rongchao, additional, Li, Jiahao, additional, Lin, Maoyu, additional, Dai, Huachao, additional, Wang, Kangpeng, additional, Sheng, Zhaojun, additional, Chen, Baizhong, additional, Xu, Xuetao, additional, Li, Chen, additional, Lin, Zhongze, additional, Zhang, Qingmin, additional, Zheng, Xi, additional, Zhang, Kun, additional, Li, Dongli, additional, and Hong, Weiqian David, additional

Published
2021
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22. Therapeutic Potential of Nitazoxanide: An Appropriate Choice for Repurposing versus SARS-CoV-2?

Author

Stachulski, Andrew V., primary, Taujanskas, Joshua, additional, Pate, Sophie L., additional, Rajoli, Rajith K. R., additional, Aljayyoussi, Ghaith, additional, Pennington, Shaun H., additional, Ward, Stephen A., additional, Hong, Weiqian David, additional, Biagini, Giancarlo A., additional, Owen, Andrew, additional, Nixon, Gemma L., additional, Leung, Suet C., additional, and O’Neill, Paul M., additional

Published
2020
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23. Larvicidal Activity of Two RutaceaePlant Essential Oils and Their Constituents Against Aedes albopictus(Diptera: Culicidae) in Multiple Formulations

Author

Jian, Rongchao, Lin, Yuan, Li, Yuling, Wu, Weifeng, Ren, Xiaofei, Liang, Zhanyuan, Kong, Lingjia, Cai, Jinglin, Lao, Canyao, Wu, Min, Chen, Wenhua, Chen, Jing, Hong, Weiqian David, and Sheng, Zhaojun

Abstract

Aedes albopictus(Skuse) is a vector of several arboviruses, such as dengue, chikungunya, West Nile, and Zika viruses. At present, the use of synthetic insecticides is the main vector control strategy. However, the widespread and long-term use of insecticides has aroused several problems, including insecticide resistance, environmental pollution, and non-target species effects, thereby encouraging researchers to search for new alternatives derived from natural products. In recent decades, essential oils (EOs) as natural alternatives to control mosquitoes have received increasing attention. In the initial larvicidal activity screen, two Rutaceaeplants (Citrus aurantiumand Citrus paradisi) EOs were selected and evaluated for killing Ae. albopictuslarvae. The LC50values of C. aurantiumand C. paradisiEOs against Ae. albopictuswere 91.7 and 100.9 ppm, respectively. The main components of C. aurantiumEO include diethyl o-phthalate (37.32%), limonene (10.04%), and methyl dihydrojasmonate (6.48%). The main components of C. paradisiEO include limonene (60.51%), diethyl o-phthalate (11.75%), linalool (7.90%), and styralyl acetate (6.28%). Among these main components of the two EOs, limonene showed potent larvicidal activity, with the LC50value of 39.7 ppm. The nanoemulsions of limonene were prepared and characterized. The duration of larvicidal activity was greater in the limonene nanoemulsions than when limonene was applied in solvent. This study demonstrates that EOs of plants in family Rutaceaeare a potential resource to develop new larvicides, and nanoemulsification is an effective method for improving the physicochemical properties and efficacy of natural products as larvicides.

Published
2022
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26. Synthesis and structure–activity relationship of N4-benzylamine-N2-isopropyl-quinazoline-2,4-diamines derivatives as potential antibacterial agents

Author

Jiang, Zhengyun, Hong, Weiqian, Cui, Xiping, Gao, Hongcan, Wu, Panpan, Chen, Yingshan, Shen, Ding, Yang, Yang, Zhang, Bingjie, Taylor, Mark, Ward, Steve, O'Neill, Paul M., Zhao, Suqing, and Zhang, Kun

Subjects
qv_354, qw_142, wb_330, qv_150
Abstract

A series of N4-benzylamine-N2-isopropyl-quinazoline-2,4-diamine derivatives has been synthesized and tested for antibacterial activity against five bacterial strains. Twelve different substituents on the N4-benzylamine group have been investigated along with replacement of the quinazoline core (with either a benzothiophene or regioisomeric pyridopyrimidine ring systems). In order to develop structure activity relationships, all derivatives were tested for their antibacterial activities against Escherichia coli and Staphylococcus aureus via Kirby–Bauer assays and minimum inhibitory concentration assays. Eight of the most potent compounds against S. aureus and E. coli were also screened against one strain of methicillin-resistant S. aureus (MRSA), Staphylococcus epidermidis and Salmonella typhimurium to further examine their antibacterial activities. Lead compound A5 showed good activities with MICs of 3.9 μg mL−1 against E. coli, S. aureus and S. epidermidis and 7.8 μg mL−1 against MRSA. Selected front runners were also screened for their DMPK properties in vitro to assess their potential for further development.

Published
2017

27. Identification and prioritization of novel anti-Wolbachia chemotypes from screening a 10,000-compound diversity library

Author

Johnston, Kelly, Cook, Darren, Berry, Neil, Hong, Weiqian David, Clare, Rachel, Goddard, Megan, Ford, Louise, Nixon, Gemma, O'Neill, Paul, Ward, Steve, and Taylor, Mark

Subjects
wc_880, qx_650, biochemical phenomena, metabolism, and nutrition, wc_885, qx_460
Abstract

Lymphatic filariasis and onchocerciasis are two important neglected tropical diseases (NTDs) that cause severe disability. Control efforts are hindered by the lack of a safe macrofilaricidal drug. Targeting the Wolbachia bacterial endosymbionts in these parasites with doxycycline leads to a macrofilaricidal outcome, but protracted treatment regimens and contraindications restrict its widespread implementation. The Anti-Wolbachia consortium aims to develop improved anti-Wolbachia drugs to overcome these barriers. We describe the first screening of a large, diverse compound library against Wolbachia. This whole-organism screen, streamlined to reduce bottlenecks, produced a hit rate of 0.5%. Chemoinformatic analysis of the top 50 hits led to the identification of six structurally diverse chemotypes, the disclosure of which could offer interesting avenues of investigation to other researchers active in this field. An example of hit-to-lead optimization is described to further demonstrate the potential of developing these high-quality hit series as safe, efficacious, and selective anti-Wolbachia macrofilaricides.

Published
2017

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