About: Trimethoprim and other nonclassical antifolates an excellent template for searching modifications of dihydrofolate reductase enzyme inhibitors

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About: Trimethoprim and other nonclassical antifolates an excellent template for searching modifications of dihydrofolate reductase enzyme inhibitors Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Trimethoprim and other nonclassical antifolates an excellent template for searching modifications of dihydrofolate reductase enzyme inhibitors
Creator	Arciszewska, Karolina Drozdowska, Danuta Wróbel, Agnieszka Dawid Maliszewski, •
Source	PMC
abstract	The development of new mechanisms of resistance among pathogens, the occurrence and transmission of genes responsible for antibiotic insensitivity, as well as cancer diseases have been a serious clinical problem around the world for over 50 years. Therefore, intense searching of new leading structures and active substances, which may be used as new drugs, especially against strain resistant to all available therapeutics, is very important. Dihydrofolate reductase (DHFR) has attracted a lot of attention as a molecular target for bacterial resistance over several decades, resulting in a number of useful agents. Trimethoprim (TMP), (2,4-diamino-5-(3′,4′,5′-trimethoxybenzyl)pyrimidine) is the well-known dihydrofolate reductase inhibitor and one of the standard antibiotics used in urinary tract infections (UTIs). This review highlights advances in design, synthesis, and biological evaluations in structural modifications of TMP as DHFR inhibitors. In addition, this report presents the differences in the active site of human and pathogen DHFR. Moreover, an excellent review of DHFR inhibition and their relevance to antimicrobial and parasitic chemotherapy was presented.
has issue date	2019-10-02(xsd:dateTime)
bibo:doi	10.1038/s41429-019-0240-6
bibo:pmid	31578455
has license	no-cc
sha1sum (hex)	87d7f11e7825e53841a3c77c3f705c1f5f0baa93
schema:url	https://doi.org/10.1038/s41429-019-0240-6
resource representing a document's title	Trimethoprim and other nonclassical antifolates an excellent template for searching modifications of dihydrofolate reductase enzyme inhibitors
has PubMed Central identifier	PMC7102388
has PubMed identifier	31578455
schema:publication	J Antibiot (Tokyo)
resource representing a document's body	covid:87d7f11e7825e53841a3c77c3f705c1f5f0baa93#body_text
is schema:about of	named entity 'TMP' named entity 'inhibition' named entity 'DHFR' named entity 'antifolates' named entity 'ANTIBIOTIC' named entity 'NEW' named entity 'INSENSITIVITY' named entity 'RESPONSIBLE' named entity 'PATHOGEN' named entity 'DRUGS' named entity 'STRAIN' named entity 'PRESENTED' named entity 'USED' named entity 'DEVELOPMENT' named entity 'WORLD' named entity 'HUMAN' named entity 'MOLECULAR TARGET' named entity 'RESISTANT TO' named entity 'STANDARD' named entity 'RESISTANCE' named entity '283' named entity 'MAY BE' named entity 'This' named entity 'bacterial resistance' named entity 'antibiotic' named entity 'antibiotics' named entity 'number' named entity 'structural' named entity 'Dihydrofolate reductase' named entity 'antimicrobial' named entity 'dihydrofolate reductase inhibitor' named entity 'DHFR' named entity 'DHFR' named entity 'antifolates' named entity 'urinary tract infections' named entity 'chemotherapy' named entity 'pathogens' named entity 'pyrimidine' named entity 'molecular target' named entity 'antibiotics' named entity '80%' named entity 'PATHOGENS' named entity 'ACTIVE' named entity 'INHIBITION' named entity 'pyrimidine' named entity 'parasitic' named entity 'antibiotic' named entity 'DHFR' named entity 'UTIs' named entity '282' named entity 'THEIR' named entity 'SYNTHESIS' named entity 'A LOT OF' named entity 'VERY IMPORTANT' named entity 'ONE OF' named entity 'INTENSE' named entity 'PRESENTS' named entity 'ADDITION' named entity '2C4' named entity 'RESULTING IN' named entity 'REVIEW OF' named entity 'CANCER' named entity 'GENES' named entity 'PROBLEM' named entity 'DESIGN' named entity 'CHEMOTHERAPY' named entity 'LEADING' named entity 'ACTIVE SITE' named entity 'DIHYDROFOLATE REDUCTASE' named entity 'SEARCHING' named entity 'ANTIBIOTICS' named entity 'MECHANISMS' named entity 'DIHYDROFOLATE REDUCTASE INHIBITOR' named entity '2C5' named entity 'REPORT' named entity 'Trimethoprim' named entity 'CLINICAL' named entity 'URINARY TRACT INFECTIONS'

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