ChemInform Abstract: Aminothiazoles. Part 1. Syntheses and Pharmacological Evaluation of 4‐[Isobutylphenyl]‐2‐substituted‐aminothiazoles.

Giridhar, Thota; Reddy, R. B.; Prasanna, B.; Mouli, G. V. P. C.

doi:10.1002/chin.200216144

Cited by 5 publications

(4 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Owing to its promising pharmacological properties, the thiophene skeleton has been well recognized as a potential entity in medicinal chemistry. 124 The thiophene derivatives are well recognized to demonstrate diverse pharmacological activities, such as antioxidant, 125 anti-HIV, 126 bactericidal, 127 antifungal, 128 anti-inflammatory, 125,129 antitubercular, 130 and, antitumor. [131][132][133] Combretastatin (CA-4) is a very well-known naturally occurring molecule that binds at the colchicine site and inhibits the polymerization of tubulin.…”

Section: Thiophenementioning

confidence: 99%

Expedition of sulfur‐containing heterocyclic derivatives as cytotoxic agents in medicinal chemistry: A decade update

Laxmikeshav

Kumari

Shankaraiah

2021

Medicinal Research Reviews

View full text Add to dashboard Cite

This review article proposes a comprehensive report of the design strategies engaged in the development of various sulfur-bearing cytotoxic agents. The outcomes of various studies depict that the sulfur heterocyclic framework is a fundamental structure in diverse synthetic analogs representing a myriad scope of therapeutic activities. A number of five-, six-and seven-membered sulfur-containing heterocyclic scaffolds, such as thiazoles, thiadiazoles, thiazolidinediones, thiophenes, thiopyrans, benzothiazoles, benzothiophenes, thienopyrimidines, simple and modified phenothiazines, and thiazepines have been discussed. The subsequent studies of the derivatives unveiled their cytotoxic effects through multiple mechanisms (viz. inhibition of tyrosine kinases, topoisomerase I and II, tubulin, COX, DNA synthesis, and PI3K/Akt and Raf/MEK/ERK signaling pathways), and several others. Thus, our concise illustration explains the design strategy and anticancer potential of these five-and six-membered sulfur-containing heterocyclic molecules along with a brief outline on seven-membered sulfur heterocycles. The thorough assessment of antiproliferative activities with the reference drug allows a proficient assessment of the structure-activity relationships (SARs) of the diversely synthesized molecules of the series.

show abstract

Section: Thiophenementioning

confidence: 99%

Expedition of sulfur‐containing heterocyclic derivatives as cytotoxic agents in medicinal chemistry: A decade update

Laxmikeshav

Kumari

Shankaraiah

2021

Medicinal Research Reviews

View full text Add to dashboard Cite

show abstract

“…Thiazole ring system is an important class of compounds in medicinal chemistry. This structure has found applications in drug development for the treatment of cardiotonic [20] , fungicidal [21] , HIV infection [22] , mental retardation in children, age-related and neurodegenerative brain damage (Alzheimer's disease, Parkinsonism disease) [23] .…”

Section: Introductionmentioning

confidence: 99%

Synthesis of novel thiazole derivative of Di-substituted N-aryl maleimides and characterized by spectral and analytical techniques

Chaudhari,

Patil,

Chavan

et al. 2023

J. Res. Chem.

View full text Add to dashboard Cite

The compound 1 was reacted with bromine in DMF to obtain dibromo succinimide 2. Compound 2 was reacted with piperidine as a base followed by dehydrohalogenation to obtained monobromo compound 3 through a common enaminone intermediate, further compound 3 on Vilsmeier Haack formylation afforded compound 4 with good yield. The condensation of 2,5-dihydro-2,5-dioxo-1-phenyl-4-(piperidin-1-yl)-1H-pyrrole-3-carbaldehyde 4 with thiosemicarbazide hydrochloride in ethanol in presence of acetic acid furnished compound 5 with 82% yield. The compound 5 react with disubstituted phenacyl bromide 6 a-e to obtained thiazole derivative of Di-substituted N-aryl maleimides 7 a-e with good yield. All the synthesized compounds were well characterised by spectral and analytical techniques.

show abstract

“…Thiazole, thiadiazole, and oxadiazole derivatives are also display a wide range of pharmacological activities such as anaesthetic (Geronikaki and Theophilidis, 1992) and anti-inflammatory (Giridhar et al, 2001) properties. Oxadiazole and thiadiazole derivatives have been evaluated and proved for a wide range of pharmacological and clinical uses (Tawfeeq et al, 2012), particularly the activity focused by antibacterial, antifungal (Liu et al, 2008), and analgesic (Almasirad et al, 2014) activities.…”

Section: Introductionmentioning

confidence: 99%

Antimicrobial, anticoagulant, and cytotoxic evaluation of multidrug resistance of new 1,4-dihydropyridine derivatives

Ahamed

Arif

Mateen

et al. 2018

Saudi Journal of Biological Sciences

View full text Add to dashboard Cite

A new series of 1,4-dihydropyridine derivatives ( and were systematically designed and synthesized via ultrasound irradiation methods with easy work-up and good yields. Compounds structures were confirmed by IR,H NMR, C NMR, and mass spectra. The synthesized compounds were screened for both antimicrobial and anticoagulant activities. Compound (MIC: 0.25 μg/mL) was highly active against and compound (MIC: 0.5 μg/mL) was also highly active against compared with ciprofloxacin. (MIC: 1 μg/mL) The antifungal activity of (MIC: 0.5 μg/mL) against was high relative to that of clotrimazole (MIC: 1 μg/mL). Anticoagulant activity was determined by activated partial thromboplastin time (APTT) and prothrombin time (PT) coagulation assays. Compound 4-(4-hydroxyphenyl)-2,6-dimethyl-,-bis(5-phenyl-1,3,4-thiadiazol-2-yl)-1,4-dihydropyridine-3,5-dicarboxamide (>1000 s in APTT assays) was highly active in anticoagulant screening compared with the reference of heparin. Cytotoxicity was evaluated using HepG2 (liver), HeLa (cervical), and MCF-7 (breast) cancer cell lines, with high toxicities observed for (GI = 0.02 μm) against HeLa cell line and (GI = 0.03 μm) equipotant against MCF-7 cell line. Therefore, the compounds and can serve as lead molecules for the development of new classes of antimicrobial and anticoagulant agent.

show abstract

ChemInform Abstract: Aminothiazoles. Part 1. Syntheses and Pharmacological Evaluation of 4‐[Isobutylphenyl]‐2‐substituted‐aminothiazoles.

Cited by 5 publications

References 0 publications

Expedition of sulfur‐containing heterocyclic derivatives as cytotoxic agents in medicinal chemistry: A decade update

Expedition of sulfur‐containing heterocyclic derivatives as cytotoxic agents in medicinal chemistry: A decade update

Synthesis of novel thiazole derivative of Di-substituted N-aryl maleimides and characterized by spectral and analytical techniques

Antimicrobial, anticoagulant, and cytotoxic evaluation of multidrug resistance of new 1,4-dihydropyridine derivatives

Contact Info

Product

Resources

About