Biarylmethoxy Nicotinamides As Novel and Specific Inhibitors of <i>Mycobacterium tuberculosis</i>

Kedari, Chaitanya Kumar; Choudhury, Nilanjana Roy; Sharma, Sreevalli; Kaur, Parvinder; Guptha, Supreeth; Panda, Manoranjan; Mukerjee, Kakoli; Ramachandran, Vasanthi; Bandodkar, Balachandra; Ramachandran, Sreekanth; Tantry, Subramanyam J.

doi:10.1021/ml4004815

Cited by 4 publications

(3 citation statements)

References 12 publications

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“…Alkem initiated drug discovery efforts in 2012 in the area of infectious diseases 251. A more recent focus has been on the development of cathepsin K inhibitors for the treatment of osteoporosis, with Alkem‐43 as a potential candidate compound (Supporting Information Table 6a, entry 168) 252, 253, 254.…”

Section: Drug Discovery In Indiamentioning

confidence: 99%

“…[250] Alkem initiated drug discovery efforts in 2012 in the area of infectious diseases. [251] Am ore recent focus has been on the development of cathepsin Ki nhibitors for the treatment of osteoporosis, with Alkem-43 as ap otentialc andidate compound (Supporting In-formationT able 6a, entry 168). [252][253][254] Alkemc losed its drug discovery efforts in preparation of its successful initial public offering in 2015, and has attempted to license the project.…”

Section: Initiation Of Drug Discovery At Large Pharmaceutical Companiesmentioning

confidence: 99%

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The Drug Discovery and Development Industry in India—Two Decades of Proprietary Small‐Molecule R&D

Differding¹

2017

ChemMedChem

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This review provides a comprehensive survey of proprietary drug discovery and development efforts performed by Indian companies between 1994 and mid‐2016. It is based on the identification and detailed analysis of pharmaceutical, biotechnology, and contract research companies active in proprietary new chemical entity (NCE) research and development (R&D) in India. Information on preclinical and clinical development compounds was collected by company, therapeutic indication, mode of action, target class, and development status. The analysis focuses on the overall pipeline and its evolution over two decades, contributions by type of company, therapeutic focus, attrition rates, and contribution to Western pharmaceutical pipelines through licensing agreements. This comprehensive analysis is the first of its kind, and, in our view, represents a significant contribution to the understanding of the current state of the drug discovery and development industry in India.

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Section: Drug Discovery In Indiamentioning

confidence: 99%

Section: Initiation Of Drug Discovery At Large Pharmaceutical Companiesmentioning

confidence: 99%

The Drug Discovery and Development Industry in India—Two Decades of Proprietary Small‐Molecule R&D

Differding¹

2017

ChemMedChem

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“…35 Medicinal chemistry optimization from the weak active compound 76 resulted in about 200 fold improvement of anti TB activity to provide compound 77, which exhibited MIC of …”

Section: Biarylmethoxy Nicotinamidementioning

confidence: 99%

Recent Progress on the Development of Novel Antitubercular Agents from Whole-Cell Screening Hits

Yokokawa

2014

J. Synth. Org. Chem. Jpn.

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Tuberculosis (TB) caused by Mycobacterium tuberculosis (Mtb) continues to be a serious major global health risk. More than one third of the world s human population is infected, resulting in 1.4 2.0 million deaths per year. The rst line therapy using a multidrug regimen has existed since the 1970s, however, there has been an alarming increase in the number of patients with multi (MDR) and extensive (XDR) drug resistant TB in recent years. Hence, there is an urgent need to develop novel drugs with new mechanisms of action and new chemotypes in order to combat drug resistant TB. A target based approach to nding new anti TB agents has been widely used, however this approach has not led to the identi cation of clinical candidates. The recent trend has been to go back to whole cell screens, in which compounds are identi ed based on their anti TB activity. Consequently, various groups have reported structurally diverse active compounds against Mtb, which were originally identi ed from phenotypic screens. This review will cover recent scienti c accounts published from these groups that have described medicinal chemistry optimization studies from whole cell screening hits. In vivo pharmacokinetics and ef cacy of optimized compounds as well as their potential molecular targets will be also discussed.

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Synthesis and Antiproliferative Activity of 2-Oxo-4-Cyano-1,2-Dihydropyridine-3-Carboxamides

Fedoseev,

Lipin

2023

Pharm Chem J

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Biarylmethoxy Nicotinamides As Novel and Specific Inhibitors of Mycobacterium tuberculosis

Cited by 4 publications

References 12 publications

The Drug Discovery and Development Industry in India—Two Decades of Proprietary Small‐Molecule R&D

The Drug Discovery and Development Industry in India—Two Decades of Proprietary Small‐Molecule R&D

Recent Progress on the Development of Novel Antitubercular Agents from Whole-Cell Screening Hits

Synthesis and Antiproliferative Activity of 2-Oxo-4-Cyano-1,2-Dihydropyridine-3-Carboxamides

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