Structure guided lead generation for M. Tuberculosis thymidylate kinase (Mtb TMK): Discovery of 3-cyanopyridone and 1,6-naphthyridin-2-one as potent inhibitors

DOI: 10.1021/jm5012947

Source and publish data:

Journal of Medicinal Chemistry p. 753 - 766 (2015)

Update date:2022-08-03

Topics:

Authors:

Naik, Maruti

Raichurkar, Anandkumar

Bandodkar, Balachandra S.

Varun, Begur V.

Bhat, Shantika

Kalkhambkar, Rajesh

Murugan, Kannan

Menon, Rani

Bhat, Jyothi

Paul, Beena

Iyer, Harini

Hussein, Syeed

Tucker, Julie A.

Vogtherr, Martin

Embrey, Kevin J.

McMiken, Helen

Prasad, Swati

Gill, Adrian

Ugarkar, Bheemarao G.

Venkatraman, Janani

Read, Jon

Panda, Manoranjan

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Article abstract of DOI:10.1021/jm5012947

M. tuberculosis thymidylate kinase (Mtb TMK) has been shown in vitro to be an essential enzyme in DNA synthesis. In order to identify novel leads for Mtb TMK, we performed a high throughput biochemical screen and an NMR based fragment screen through which

Full text of DOI:10.1021/jm5012947

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