Abstract
Background: Thiazole is a good pharmacophore nucleus due to its various pharmaceutical applications. Its derivatives have a wide range of biological activities such as antioxidant, analgesic, and antimicrobial including antibacterial, antifungal, antimalarial, anticancer, antiallergic, antihypertensive, anti-inflammatory, and antipsychotic. Indeed, the thiazole scaffold is contained in more than 18 FDA-approved drugs as well as in numerous experimental drugs. Objective: To summarize recent literature on the biological activities of thiazole ring-containing compounds Methods: A literature survey regarding the topics from the year 2015 up to now was carried out. Older publications were not included, since they were previously analyzed in available peer reviews. Results: Nearly 124 research articles were found, critically analyzed, and arranged regarding the synthesis and biological activities of thiazoles derivatives in the last 5 years.
Highlights
One of the main objectives of organic and medicinal chemistry is the design, synthesis, and development of molecules having therapeutic potential as human drugs
This thiazole derivative was found to be active against a wide range of multi-drug resistant Gram-negative bacteria, including Pseudomonas aeruginosa (P.aeruginosa) and used to treat complicated urinary tract infections in case when no other treatment is available [9,10,11]
Another example is cobicistat, which is a drug used for the treatment of human immunodeficiency virus infection (HIV) as a drug prolonging the half-life of some antivirotic drugs
Summary
One of the main objectives of organic and medicinal chemistry is the design, synthesis, and development of molecules having therapeutic potential as human drugs. Among them are cefiderocol, which was the first siderophore antibiotic approved by the FDA in 2019 under the brand name Fetroja® (Figure 1) This thiazole derivative was found to be active against a wide range of multi-drug resistant Gram-negative bacteria, including Pseudomonas aeruginosa (P.aeruginosa) and used to treat complicated urinary tract infections in case when no other treatment is available [9,10,11]. Lusutrombopag is a medication that was approved in 2018 for the stimulation of platelet formation used to treat thrombocytopenia such as thrombocytopenia associated with chronic liver disease Another example is cobicistat, which is a drug used for the treatment of human immunodeficiency virus infection (HIV) as a drug prolonging the half-life of some antivirotic drugs. Synthesis of 2-aminothiazoles from β-keto ester, tribromoisocyanuric acid, and thiourea. Component cascade cyclization of enaminones, cyanamide, and elemental sulfur (3S.chBeimoelo2g2)i.cal Activities of Thiazoles
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