Review of the Sulfonamides and Trimethoprim

Smith, Connie L.; Powell, Keith R.

doi:10.1542/pir.21-11-368

Cited by 27 publications

(7 citation statements)

References 3 publications

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“…Sulphonamides are synthetic compounds based on the industrial dye sulfachrysoidine; 69 they are analogues of p-aminobenzoic acid (PABA) and inhibit folic acid biosynthesis via competitive inhibition of the enzyme dihydropteroate synthetase. 70,71 This competitive inhibition is bacteriostatic, disrupting DNA synthesis and bacterial growth.…”

Section: Sulphonamides (Two In Antibioticdb)mentioning

confidence: 99%

Revitalizing the drug pipeline: AntibioticDB, an open access database to aid antibacterial research and development

Farrell

Wanford

et al. 2018

Journal of Antimicrobial Chemotherapy

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The current state of antibiotic discovery, research and development is insufficient to respond to the need for new treatments for drug-resistant bacterial infections. The process has changed over the last decade, with most new agents that are in Phases 1-3, or recently approved, having been discovered in small- and medium-sized enterprises or academia. These agents have then been licensed or sold to large companies for further development with the goal of taking them to market. However, early drug discovery and development, including the possibility of developing previously discontinued agents, would benefit from a database of antibacterial compounds for scrutiny by the developers. This article describes the first free, open-access searchable database of antibacterial compounds, including discontinued agents, drugs under pre-clinical development and those in clinical trials: AntibioticDB (AntibioticDB.com). Data were obtained from publicly available sources. This article summarizes the compounds and drugs in AntibioticDB, including their drug class, mode of action, development status and propensity to select drug-resistant bacteria. AntibioticDB includes compounds currently in pre-clinical development and 834 that have been discontinued and that reached varying stages of development. These may serve as starting points for future research and development.

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Section: Sulphonamides (Two In Antibioticdb)mentioning

confidence: 99%

Revitalizing the drug pipeline: AntibioticDB, an open access database to aid antibacterial research and development

Farrell

Wanford

et al. 2018

Journal of Antimicrobial Chemotherapy

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“…All three drugs induce both dose-related toxicity and hypersensitivity, adverse effects on liver, brain, kidney, gastrointestinal and haemopoietic systems. 18–21 The risk of aplastic anemia with the use of other antiepileptic drug like sodium valproate 11 phenytoin 12 and felbamate 22 were found in several case reports. We did not find any significant association of Phenytoin with aplastic anemia.…”

Section: Discussionmentioning

confidence: 99%

The Relationship of Drug Therapy to Aplastic Anemia in Pakistan: A Hospital-Based Case Control Study

Syed¹,

Rahman²,

Syed³

et al. 2021

TCRM

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“…10 and 14) [88][89][90][91] and while they exhibited excellent ZBG properties for coordination, these moieties often suffer from permeability issues and were produced largely as tool compounds. As a result, more recent compounds utilise groups like hydroxamic acids (9, 11, and 12, this type of coordination is demonstrated in Figure 3B) [90][91][92][93][94][95] and geminal-diol (13) [96][97][98] for the coordination of Zn 2+ . Although targeting the Zn 2+ is essential, the approach raises challenges for selectivity of the parasite target over human homologuesparasite specific inhibitors therefore require the employment of specific interactions with the PfA-M1 S1 and S1 0 subsites [81].…”

Section: Pfa-m1 -Flexible Substrate Pockets Provide Key To Potencymentioning

confidence: 97%

“…Some of the earliest synthetic antimalarials targeted DHFR [11][12][13][14][15]. Cycloguanil (1) and pyrimethamine (Pyr) (2), date back to the 1940s [16,17] but long-term widespread use of these molecules has led to resistance through the evolution of multiple mutations in PfDHFR [18][19][20].…”

Section: Dihydrofolate Reductase -A Resistant Enzyme Made Sensitivementioning

confidence: 99%

Driving antimalarial design through understanding of target mechanism

Calic

Mansouri

Scammells

et al. 2020

Biochemical Society Transactions

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Malaria continues to be a global health threat, affecting approximately 219 million people in 2018 alone. The recurrent development of resistance to existing antimalarials means that the design of new drug candidates must be carefully considered. Understanding of drug target mechanism can dramatically accelerate early-stage target-based development of novel antimalarials and allows for structural modifications even during late-stage preclinical development. Here, we have provided an overview of three promising antimalarial molecular targets, PfDHFR, PfDHODH and PfA-M1, and their associated inhibitors which demonstrate how mechanism can inform drug design and be effectively utilised to generate compounds with potent inhibitory activity.

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Review of the Sulfonamides and Trimethoprim

Cited by 27 publications

References 3 publications

Revitalizing the drug pipeline: AntibioticDB, an open access database to aid antibacterial research and development

Revitalizing the drug pipeline: AntibioticDB, an open access database to aid antibacterial research and development

The Relationship of Drug Therapy to Aplastic Anemia in Pakistan: A Hospital-Based Case Control Study

Driving antimalarial design through understanding of target mechanism

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