scholarly journals Inhibitors of pantothenate synthetase of Mycobacterium tuberculosis – a medicinal chemist perspective

RSC Advances ◽  
2020 ◽  
Vol 10 (61) ◽  
pp. 37098-37115
Author(s):  
Amaroju Suresh ◽  
Singireddi Srinivasarao ◽  
Yogesh Mahadu Khetmalis ◽  
Shashidhar Nizalapur ◽  
Murugesan Sankaranarayanan ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Drug Discovery ◽  
Antitubercular Drugs ◽  
New Drug ◽  
Current Review ◽  
Pantothenate Synthetase

Tuberculosis, leads to numerous deaths worldwide. New drug discovery strategies are need of the hour. In the current review, we focused on the discovery of new antitubercular drugs targeting pantothenate synthetase.

scholarly journals Targeting Genome Integrity in Mycobacterium Tuberculosis: From Nucleotide Synthesis to DNA Replication and Repair

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1205 ◽  
Author(s):  
Riccardo Miggiano ◽  
Castrese Morrone ◽  
Franca Rossi ◽  
Menico Rizzi
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Drug Discovery ◽  
Genome Stability ◽  
Current Knowledge ◽  
Genome Integrity ◽  
Dna Integrity ◽  
Dna Metabolism ◽  
Nucleotide Synthesis ◽  
Antitubercular Drugs ◽  
Molecular Events

Mycobacterium tuberculosis (MTB) is the causative agent of tuberculosis (TB), an ancient disease which still today causes 1.4 million deaths worldwide per year. Long-term, multi-agent anti-tubercular regimens can lead to the anticipated non-compliance of the patient and increased drug toxicity, which in turn can contribute to the emergence of drug-resistant MTB strains that are not susceptible to first- and second-line available drugs. Hence, there is an urgent need for innovative antitubercular drugs and vaccines. A number of biochemical processes are required to maintain the correct homeostasis of DNA metabolism in all organisms. Here we focused on reviewing our current knowledge and understanding of biochemical and structural aspects of relevance for drug discovery, for some such processes in MTB, and particularly DNA synthesis, synthesis of its nucleotide precursors, and processes that guarantee DNA integrity and genome stability. Overall, the area of drug discovery in DNA metabolism appears very much alive, rich of investigations and promising with respect to new antitubercular drug candidates. However, the complexity of molecular events that occur in DNA metabolic processes requires an accurate characterization of mechanistic details in order to avoid major flaws, and therefore the failure, of drug discovery approaches targeting genome integrity.

Current Approaches to Drug Discovery for Chagas Disease: Methodological Advances

2019 ◽  
Vol 22 (8) ◽  
pp. 509-520
Author(s):  
Cauê B. Scarim ◽  
Chung M. Chin
Keyword(s):  
Drug Discovery ◽  
Chagas Disease ◽  
Drug Candidates ◽  
Lead Compounds ◽  
New Drug ◽  
Compound Libraries ◽  
Screening Assays ◽  
Cruzi Infection

Background: In recent years, there has been an improvement in the in vitro and in vivo methodology for the screening of anti-chagasic compounds. Millions of compounds can now have their activity evaluated (in large compound libraries) by means of high throughput in vitro screening assays. Objective: Current approaches to drug discovery for Chagas disease. Method: This review article examines the contribution of these methodological advances in medicinal chemistry in the last four years, focusing on Trypanosoma cruzi infection, obtained from the PubMed, Web of Science, and Scopus databases. Results: Here, we have shown that the promise is increasing each year for more lead compounds for the development of a new drug against Chagas disease. Conclusion: There is increased optimism among those working with the objective to find new drug candidates for optimal treatments against Chagas disease.

scholarly journals ONRLDB—manually curated database of experimentally validated ligands for orphan nuclear receptors: insights into new drug discovery

Database ◽  
2015 ◽  
Vol 2015 ◽  
pp. bav112 ◽  
Author(s):  
Ravikanth Nanduri ◽  
Isha Bhutani ◽  
Arun Kumar Somavarapu ◽  
Sahil Mahajan ◽  
Raman Parkesh ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Nuclear Receptors ◽  
Orphan Nuclear Receptors ◽  
New Drug

HTRF Applications in New Drug Discovery

2013 ◽  
Vol 33 (13) ◽  
pp. 21-21
Author(s):  
John Sterling
Keyword(s):  
Drug Discovery ◽  
New Drug

scholarly journals Open Science Meets Stem Cells: A New Drug Discovery Approach for Neurodegenerative Disorders

2018 ◽  
Vol 12 ◽  
Author(s):  
Chanshuai Han ◽  
Mathilde Chaineau ◽  
Carol X.-Q. Chen ◽  
Lenore K. Beitel ◽  
Thomas M. Durcan
Keyword(s):  
Stem Cells ◽  
Drug Discovery ◽  
Neurodegenerative Disorders ◽  
Open Science ◽  
New Drug

Drug discovery in tuberculosis. New drug targets and antimycobacterial agents

2018 ◽  
Vol 150 ◽  
pp. 525-545 ◽  
Author(s):  
André Campaniço ◽  
Rui Moreira ◽  
Francisca Lopes
Keyword(s):  
Drug Discovery ◽  
Drug Targets ◽  
New Drug ◽  
Antimycobacterial Agents

Collateral efficacy as a pharmacological problem applied to new drug discovery

2006 ◽  
Vol 1 (7) ◽  
pp. 635-652 ◽  
Author(s):  
Terry Kenakin
Keyword(s):  
Drug Discovery ◽  
New Drug
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