Design and development of novel inhibitors for the treatment of latent tuberculosis | Zendy

Rudraraju Srilakshmi Reshma | Zendy; Perumal Yogeeswari | Zendy; Dharmarajan Sriram | Zendy

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Design and development of novel inhibitors for the treatment of latent tuberculosis

Author(s) -

Rudraraju Srilakshmi Reshma,

Perumal Yogeeswari,

Dharmarajan Sriram

Publication year - 2016

Publication title -

international journal of mycobacteriology

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.53

H-Index - 20

eISSN - 2212-554X

pISSN - 2212-5531

DOI - 10.1016/j.ijmyco.2016.09.006

Subject(s) - mycobacterium tuberculosis , bedaquiline , capreomycin , pharmacophore , tuberculosis , chemistry , small molecule , pharmacology , drug , ic50 , biology , stereochemistry , biochemistry , medicine , in vitro , ethambutol , pathology

"The captain of all these men of death", is the apt sobriquet for the age-old disease tuberculosis (TB). Despite the availability of many drugs, cases of increasing resistance in the forms of multi-drug and extensively drug-resistant TB and persistence [characteristic of Mycobacterium tuberculosis (MTB)] make the eradication of TB a nightmare. Approval of bedaquiline by the Food and Drug Administration focused attention on quinoline scaffolds for development of new anti-TB agents. Lysine ε-aminotransferase (LAT) in MTB plays a pivotal role in regulating amino acid synthesis, which in turn affects mycobacterial persistence. Here, developed quinoline inhibitors that targeted LAT with an objective to eliminate dormant forms of mycobacterium.

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