He Zhao

Wuxi People's Hospital

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Hongbin Cao

Beijing Normal University

Yongbing Xie

Institute of Process Engineering

Min Zhang

South China University of Technology

Terrence R. Burke

National Cancer Institute

Chenming Liu

Zhejiang University

Penghui Du

Southern University of Science and Technology

Huanfeng Jiang

South China University of Technology

Andrew Thurkauf

Repligen (United States)

Zhi Sun

University of Chinese Academy of Sciences

Nouri Neamati

University of Michigan–Ann Arbor

Cooperative Institutions

Chinese Academy of Sciences

203

BioMimetic Systems (United States)

138

Biosensores (Spain)

134

University of Chinese Academy of Sciences

125

Institute of Process Engineering

Peking University

Shanghai Jiao Tong University

Tianjin University

Zhejiang University

Huazhong University of Science and Technology

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Arylamide Inhibitors of HIV-1 Integrase

Journal of Medicinal Chemistry (1997)

He Zhao Nouri Neamati Abhijit Mazumder Sanjay Sunder Yves Pommier

Based on data derived from a large number of HIV-1 integrase inhibitors, similar structural features can be observed, which consist of two aryl units separated by a central linker. For many inhibitors fitting this pattern, at least one aryl ring also requires ortho bis-hydroxylation for significant inhibitory potency. The ability of such catechol species to undergo in situ oxidation to reactive quinones presents one potential limitation to their utility. In an effort to address this problem, a series of inhibitors were prepared which did not contain ortho bishydroxyls. None of these analogues exhibited significant inhibition. Therefore an alternate approach was taken, whose aim was to increase potency rather than eliminate catechol substructures. In this latter study, naphthyl nuclei were utilized as aryl components, since a previous report had indicated that fused bicyclic rings may afford higher affinity relative to monocyclic phenyl-based systems. In preliminary work with monomeric units, it was found that the 6,7-dihydroxy-2-naphthoic acid (17) (IC50 = 4.7 microM) was approximately 10-fold more potent than its 5,6-dihydroxy isomer 19 (IC50 = 62.4 microM). Of particular note was the dramatic difference in potency between free acid 17 and its methyl ester 21 (IC50 > 200 microM). The nearly total loss of activity induced by esterification strongly indicates that the free carboxylic -OH is important for high potency of this compound. This contrasts with the isomeric 5,6-dihydroxy species 19, where esterification had no effect on inhibitory potency (23, IC50 = 52.7 microM). These data provide evidence that the monomeric 6,7- and 5,6-dihydroxynaphthalenes may be interacting with the enzyme in markedly different fashions. However, when these naphthyl nuclei were incorporated into dimeric structures, significant enhancements in potencies each relative to the monomeric acids were observed, with bis-6,7-dihydroxy analogue 49 and bis-5,6-dihydroxy analogue 51 both exhibiting approximately equal potencies (IC50 values of 0.81 and 0.11 microM, respectively).

Integrase inhibitor

Linker

IC50

Structure–activity relationship

Catechol

Hydroxylation

10.1021/jm960449w

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Citations (85)

Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: A novel series of mixed dopamine D2/D4 receptor antagonist

Bioorganic & Medicinal Chemistry Letters (2003)

He Zhao Xiaoyan Zhang Kevin J. Hodgetts Andrew Thurkauf Jack Hammer

Tricyclic

10.1016/s0960-894x(02)01056-9

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Citations (16)

A combination of electro-enzymatic catalysis and electrocoagulation for the removal of endocrine disrupting chemicals from water

Journal of Hazardous Materials (2015)

He Zhao Di Zhang Penghui Du Haitao Li Chenming Liu

Electrocoagulation

Hypochlorite

10.1016/j.jhazmat.2015.04.063

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Citations (43)

N-dependent ozonation efficiency over nitrogen-containing heterocyclic contaminants: A combined density functional theory study on reaction kinetics and degradation pathways

Chemical Engineering Journal (2019)

Yujie Yao Yongbing Xie Binran Zhao Linbi Zhou Yanchun Shi

Hydroxylation

Degradation

Benzotriazole

10.1016/j.cej.2019.122708

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Citations (49)

ChemInform Abstract: Design and Synthesis of Photoactivatable Coumarin‐Containing HIV‐1 Integrase Inhibitors.

ChemInform (1998)

He Zhao Nouri Neamati Yves Pommier T. R. JUN. BURKE

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

10.1002/chin.199816131

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Citations (0)

Structure of the catalytic domain of avian sarcoma virus integrase with a bound HIV-1 integrase-targeted inhibitor

Proceedings of the National Academy of Sciences (1998)

J. Łubkowski Fan Yang Jerry Alexandratos Alexander Wlodawer He Zhao

The x-ray structures of an inhibitor complex of the catalytic core domain of avian sarcoma virus integrase (ASV IN) were solved at 1.9- to 2.0-Å resolution at two pH values, with and without Mn 2+ cations. This inhibitor (Y-3), originally identified in a screen for inhibitors of the catalytic activity of HIV type 1 integrase (HIV-1 IN), was found in the present study to be active against ASV IN as well as HIV-1 IN. The Y-3 molecule is located in close proximity to the enzyme active site, interacts with the flexible loop, alters loop conformation, and affects the conformations of active site residues. As crystallized, a Y-3 molecule stacks against its symmetry-related mate. Preincubation of IN with metal cations does not prevent inhibition, and Y-3 binding does not prevent binding of divalent cations to IN. Three compounds chemically related to Y-3 also were investigated, but no binding was observed in the crystals. Our results identify the structural elements of the inhibitor that likely determine its binding properties.

Divalent

Integrase inhibitor

Viral protein

10.1073/pnas.95.9.4831

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Citations (81)

Synergistic effect of charge transfer and short H-bonding on nanocatalyst surface for efficient oxygen evolution reaction

Nano Energy (2019)

Jinlong Yang Yinguo Xiao He Zhao Guangxing Zhang Rui Wang

Oxygen evolution

Overpotential

10.1016/j.nanoen.2019.02.053

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Citations (34)

Theoretical study on the two novel planar-type all-nitrogen N44− anions: Structures, stability, reaction rate and their stable mechanisms via protonation

Chemical Physics Letters (2021)

Yifan Feng Haiyan Zhu Qiyan Zhang Qinfu Zhao He Zhao

Zigzag

Tripod (photography)

10.1016/j.cplett.2021.138519

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Citations (4)

Characterization of flocs generated by preformed and in situ formed Al13 polymer

Chemical Engineering Journal (2012)

Chengzhi Hu Guixia Chen Huijuan Liu He Zhao Jiuhui Qu

Inorganic polymer

Particle (ecology)

10.1016/j.cej.2012.05.041

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Citations (32)

Simultaneous removal of SO2 and NOx from flue gas by low-temperature adsorption over activated carbon

Scientific Reports (2021)

Shiqing Wang Shisen Xu Shiwang Gao Ping Xiao Minhua Jiang

Abstract An exceptional phenomenon has been observed that SO 2 and NO x in flue gas can be effectively adsorbed over activated carbon with a surprising capacity at cold temperatures with the presence of oxygen. In this study, the adsorption characteristics of NO and SO 2 over activated carbon at 80, 20, 0, and − 20 is experimentally investigated. Without the presence of oxygen, adsorption of NO is negligible. In the presence of oxygen, NO can be oxidized to NO 2 over activated carbon which leads to the co-adsorption of NO/NO 2 within the adsorption bed. Catalytic oxidation of NO over activated carbon can be significantly enhanced at cold temperatures, leading to an extraordinary increase of adsorption capacity of NO. With an initial concentration of NO = 200 ppmv and a space velocity of 5000 h −1 , the average specific capacity increases from 3.8 to 169.1 mg/g when the temperature decreases from 80 to – 20 ℃. For NO–O 2 co-adsorption, the specific capacity increases along the adsorption bed due to the increasing NO 2 concentrations. The adsorption capacity of SO 2 is also significantly enhanced at cold temperatures. With an initial concentration of SO 2 = 1000 ppmv, the specific capacity increases from 12.9 to 123.1 mg/g when the temperature decreases from 80 to – 20 ℃. A novel low-temperature adsorption (LAS) process is developed to simultaneously remove SO 2 and NO x from flue gas with a target of near-zero emission. A pilot-scale testing platform with a flue gas flowrate of 3600 Nm 3 /h is developed and tested. Emission of both SO 2 and NO x is less than 1 ppmv, and the predicted energy penalty is about 3% of the net generation.

Carbon fibers

Space velocity

10.1038/s41598-021-90532-9

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Citations (38)