Reach Us +441414719275
Synthesis and Evaluation of Anti-HIV-1 Activities of Novel 7-Hydroxy-1,3- dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-4-carboxylate Derivatives | OMICS International | Abstract
ISSN: 2161-0444

Medicinal Chemistry
Open Access

Like us on:

OMICS International organises 3000+ Global Conferenceseries Events every year across USA, Europe & Asia with support from 1000 more scientific Societies and Publishes 700+ Open Access Journals which contains over 50000 eminent personalities, reputed scientists as editorial board members.

Open Access Journals gaining more Readers and Citations
700 Journals and 15,000,000 Readers Each Journal is getting 25,000+ Readers

This Readership is 10 times more when compared to other Subscription Journals (Source: Google Analytics)

Research Article

Synthesis and Evaluation of Anti-HIV-1 Activities of Novel 7-Hydroxy-1,3- dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-4-carboxylate Derivatives

Guan-Nan LIU1,2, Rong-Hua LUO3, Xing-Jie ZHANG3, Yu ZHOU2, Jian LI2, Yong-Tang ZHENG3 and Hong LIU2*

1College of Life Sciences, China Jiliang University, Hangzhou, Zhejiang, China

2State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai, China

3Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China

*Corresponding Author:
Hong LIU
State Key Laboratory of Drug Research
Shanghai Institute of Material Medica
Chinese Academy of Sciences
555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park
Shanghai 201203, China
Tel: +86-21-50807042
Fax: +86-21-50807042
E-mail: [email protected]

Received date: July 03, 2014; Accepted date: July 27, 2014; Published date: July 29, 2014

Citation: LIU GN, LUO RH, ZHANG XJ, ZHOU Y, LI J, et al. (2014) Synthesis and Evaluation of Anti-HIV-1 Activities of Novel 7-Hydroxy-1,3-dioxo-2,3-dihydro- 1H-pyrrolo[3,4-c]pyridine-4-carboxylate Derivatives. Med chem 4:573-580. doi:10.4172/2161-0444.1000196

Copyright: © 2014 LIU GN, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.


Aim: To design and synthesize a series of novel 7-hydroxy-1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-4- carboxylate derivatives and evaluate their anti-HIV-1 activities. Methods: Holding the same triad of metal-chelating heteroatoms for the catalytic site of IN and introducing a new hydroxyl group into the adjacent position of the amide to form another three-heteroatoms group for metal chelation, a series of novel 7-hydroxy-1,3-dioxo-2,3-dihydro-1Hpyrrolo[ 3,4-c]pyridine-4-carboxylate derivatives were designed and synthesized through multi-step chemical reactions. All the synthesized compounds were evaluated for their inhibitory activities against HIV-1 replication. Results: Thirtyfive new compounds (5–13) have been designed, synthesized and bioassayed. Their structural features were determined by 1H-NMR spectra, and low- and high-resolution mass spectra. Most of the synthesized compounds showed moderate to potent activities against HIV-1. Among the analogs, compounds 7d, 7f, 7i-7j, 8d and 9c exhibited potent anti-HIV-1 activities (EC50<10 μM). In particular, 7d exhibited significant anti-HIV-1 activities with EC50 values of 1.65 μM. Conclusion: This study provides a new template for further development of potent anti-HIV-1 drugs, and the preliminary SAR among the newly synthesized analogs provided useful indications for guiding further rational design of potent anti-HIV-1 agents.


Peer Reviewed Journals
Make the best use of Scientific Research and information from our 700 + peer reviewed, Open Access Journals
International Conferences 2019-20
Meet Inspiring Speakers and Experts at our 3000+ Global Annual Meetings

Contact Us

Agri and Aquaculture Journals

Dr. Krish

[email protected]

+1-702-714-7001Extn: 9040

Biochemistry Journals

Datta A

[email protected]

1-702-714-7001Extn: 9037

Business & Management Journals


[email protected]

1-702-714-7001Extn: 9042

Chemistry Journals

Gabriel Shaw

[email protected]

1-702-714-7001Extn: 9040

Clinical Journals

Datta A

[email protected]

1-702-714-7001Extn: 9037

Engineering Journals

James Franklin

[email protected]

1-702-714-7001Extn: 9042

Food & Nutrition Journals

Katie Wilson

[email protected]

1-702-714-7001Extn: 9042

General Science

Andrea Jason

[email protected]

1-702-714-7001Extn: 9043

Genetics & Molecular Biology Journals

Anna Melissa

[email protected]

1-702-714-7001Extn: 9006

Immunology & Microbiology Journals

David Gorantl

[email protected]

1-702-714-7001Extn: 9014

Materials Science Journals

Rachle Green

[email protected]

1-702-714-7001Extn: 9039

Nursing & Health Care Journals

Stephanie Skinner

[email protected]

1-702-714-7001Extn: 9039

Medical Journals

Nimmi Anna

[email protected]

1-702-714-7001Extn: 9038

Neuroscience & Psychology Journals

Nathan T

[email protected]

1-702-714-7001Extn: 9041

Pharmaceutical Sciences Journals

Ann Jose

ankara escort

[email protected]

1-702-714-7001Extn: 9007

Social & Political Science Journals

Steve Harry

pendik escort

[email protected]

1-702-714-7001Extn: 9042

© 2008- 2019 OMICS International - Open Access Publisher. Best viewed in Mozilla Firefox | Google Chrome | Above IE 7.0 version