Literature DB >> 26191372

Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents.

Jian Tang1, Bangxing Wang2, Tian Wu3, Junting Wan3, Zhengchao Tu3, Moses Njire1, Baojie Wan4, Scott G Franzblauc4, Tianyu Zhang3, Xiaoyun Lu3, Ke Ding3.   

Abstract

A series of pyrazolo[1,5-a]pyridine-3-carboxamide derivatives were designed and synthesized as new anti-Mycobacterium tuberculosis (Mtb) agents. The compounds exhibit promising in vitro potency with nanomolar MIC values against the drug susceptive H37Rv strain and a panel of clinically isolated multidrug-resistant Mtb (MDR-TB) strains. One of the representative compounds (5k) significantly reduces the bacterial burden in an autoluminescent H37Ra infected mouse model, suggesting its promising potential to be a lead compound for future antitubercular drug discovery.

Entities:  

Keywords:  Antitubercular agent; H37Rv; pyrazolo[1,5-a]pyridine; structure−activity relationship; tuberculosis

Year:  2015        PMID： 26191372      PMCID： PMC4499832          DOI： 10.1021/acsmedchemlett.5b00176

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  21 in total

Review 1.  Respiratory ATP synthesis: the new generation of mycobacterial drug targets?

Authors:  Dirk Bald; Anil Koul
Journal:  FEMS Microbiol Lett       Date:  2010-03-20       Impact factor: 2.742

2.  Synthesis of 3-substituted pyrazolo[1,5-a]pyridine derivatives with inhibitory activity on platelet aggregation. I.

Authors:  K Awano; S Suzue; M Segawa
Journal:  Chem Pharm Bull (Tokyo)       Date:  1986-07       Impact factor: 1.645

3.  Infectious disease. Approval of novel TB drug celebrated--with restraint.

Authors:  Jon Cohen
Journal:  Science       Date:  2013-01-11       Impact factor: 47.728

Review 4.  Advances in the development of new tuberculosis drugs and treatment regimens.

Authors:  Alimuddin Zumla; Payam Nahid; Stewart T Cole
Journal:  Nat Rev Drug Discov       Date:  2013-05       Impact factor: 84.694

5.  Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).

Authors:  S Löber; H Hübner; W Utz; P Gmeiner
Journal:  J Med Chem       Date:  2001-08-16       Impact factor: 7.446

6.  Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.

Authors:  Garrett C Moraski; Lowell D Markley; Philip A Hipskind; Helena Boshoff; Sanghyun Cho; Scott G Franzblau; Marvin J Miller
Journal:  ACS Med Chem Lett       Date:  2011-06-09       Impact factor: 4.345

7.  Autoluminescent Mycobacterium tuberculosis for rapid, real-time, non-invasive assessment of drug and vaccine efficacy.

Authors:  Tianyu Zhang; Si-Yang Li; Eric L Nuermberger
Journal:  PLoS One       Date:  2012-01-11       Impact factor: 3.240

8.  A dual read-out assay to evaluate the potency of compounds active against Mycobacterium tuberculosis.

Authors:  Juliane Ollinger; Mai Ann Bailey; Garrett C Moraski; Allen Casey; Stephanie Florio; Torey Alling; Marvin J Miller; Tanya Parish
Journal:  PLoS One       Date:  2013-04-04       Impact factor: 3.240

9.  Identification of novel imidazo[1,2-a]pyridine inhibitors targeting M. tuberculosis QcrB.

Authors:  Katherine A Abrahams; Jonathan A G Cox; Vickey L Spivey; Nicholas J Loman; Mark J Pallen; Chrystala Constantinidou; Raquel Fernández; Carlos Alemparte; Modesto J Remuiñán; David Barros; Lluis Ballell; Gurdyal S Besra
Journal:  PLoS One       Date:  2012-12-31       Impact factor: 3.240

10.  PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release.

Authors:  Ramandeep Singh; Ujjini Manjunatha; Helena I M Boshoff; Young Hwan Ha; Pornwaratt Niyomrattanakit; Richard Ledwidge; Cynthia S Dowd; Ill Young Lee; Pilho Kim; Liang Zhang; Sunhee Kang; Thomas H Keller; Jan Jiricek; Clifton E Barry
Journal:  Science       Date:  2008-11-28       Impact factor: 63.714
View more
  21 in total

1.  Identification of Pyrazolo[1,5-a]pyridine-3-carboxamide Diaryl Derivatives as Drug Resistant Antituberculosis Agents.

Authors:  Xianglong Hu; Baojie Wan; Yang Liu; Jiayi Shen; Scott G Franzblau; Tianyu Zhang; Ke Ding; Xiaoyun Lu
Journal:  ACS Med Chem Lett       Date:  2019-02-21       Impact factor: 4.345

Review 2.  Molecule Property Analyses of Active Compounds for Mycobacterium tuberculosis.

Authors:  Vadim Makarov; Elena Salina; Robert C Reynolds; Phyo Phyo Kyaw Zin; Sean Ekins
Journal:  J Med Chem       Date:  2020-04-20       Impact factor: 7.446

3.  Assessment of Clofazimine and TB47 Combination Activity against Mycobacterium abscessus Using a Bioluminescent Approach.

Authors:  Yang Liu; Yaoju Tan; M Mahmudul Islam; Yuanyuan Cao; Xiaoyun Lu; Sheng Zeng; H M Adnan Hameed; Peipei Zhou; Xingshan Cai; Shuai Wang; Julius N Mugweru; Guoliang Zhang; Huancai Yin; Jianxiong Liu; Eric Nuermberger; Tianyu Zhang
Journal:  Antimicrob Agents Chemother       Date:  2020-02-21       Impact factor: 5.191

4.  Design, synthesis, and biological evaluation of m-amidophenol derivatives as a new class of antitubercular agents.

Authors:  Niu-Niu Zhang; Zhi-Yong Liu; Jie Liang; Yun-Xiang Tang; Lu Qian; Ya-Min Gao; Tian-Yu Zhang; Ming Yan
Journal:  Medchemcomm       Date:  2018-06-07       Impact factor: 3.597

5.  Alcohols as Latent Coupling Fragments for Metallaphotoredox Catalysis: sp3-sp2 Cross-Coupling of Oxalates with Aryl Halides.

Authors:  Xiaheng Zhang; David W C MacMillan
Journal:  J Am Chem Soc       Date:  2016-10-17       Impact factor: 15.419

Review 6.  Targeting the cytochrome bc1 complex for drug development in M. tuberculosis: review.

Authors:  Mushtaq Ahmad Wani; Devendra Kumar Dhaked
Journal:  Mol Divers       Date:  2021-11-11       Impact factor: 3.364

Review 7.  Thiazole Ring-A Biologically Active Scaffold.

Authors:  Anthi Petrou; Maria Fesatidou; Athina Geronikaki
Journal:  Molecules       Date:  2021-05-25       Impact factor: 4.411

8.  Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant Mycobacterium tuberculosis.

Authors:  Xiaoyun Lu; Xianglong Hu; Zhiyong Liu; Tianyu Zhang; Ruibing Wang; Baojie Wan; Scott G Franzblau; Qidong You
Journal:  Medchemcomm       Date:  2017-04-28       Impact factor: 3.597

9.  Sterilizing Effects of Novel Regimens Containing TB47, Clofazimine, and Linezolid in a Murine Model of Tuberculosis.

Authors:  Wei Yu; Buhari Yusuf; Shuai Wang; Xirong Tian; H M Adnan Hameed; Zhili Lu; Gift Chiwala; Md Shah Alam; Gregory M Cook; Dmitry A Maslov; Nanshan Zhong; Tianyu Zhang
Journal:  Antimicrob Agents Chemother       Date:  2021-07-19       Impact factor: 5.191

Review 10.  Chemical Classes Presenting Novel Antituberculosis Agents Currently in Different Phases of Drug Development: A 2010-2020 Review.

Authors:  Klaudia T Angula; Lesetja J Legoabe; Richard M Beteck
Journal:  Pharmaceuticals (Basel)       Date:  2021-05-13
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.