Preparation and properties of antitubercular 1-piperidino-3-arylthioureas

Hearn, Michael J.; Webster, Eleanor R.; Cynamon, Michael H.

doi:10.1002/jhet.5570420632

Cited by 7 publications

(4 citation statements)

References 17 publications

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“…In this perception, a series of 1piperidino-3-arylthioureas were evaluated for their anti-TB activity. Compound 64 has shown best potency of MIC 8μg/mL against the strain 303 (Hearn et al, 2005). A series of 2-Substituted derivatives of diphenylpyraline and their 1phenyl and 1-phenethyl analogues were evaluated against Mtb H37Rv as well as their cytotoxicity against human cells (HEK-293).…”

Section: Quinolonesmentioning

confidence: 99%

Anti-tubercular activity of some six membered heterocycle compounds

Asif¹

2019

Preprint

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The effectiveness in TB treatment is difficult because the structural composition of the mycobacterial cell wall is very complicated, which makes many drugs ineffective. Tuberculosis is still one of the most imperative infectious disease worldwide becouse its important reason is drug resistant, persistent or latent tuberculosis and synergism with HIV. Furthermore no any new chemical entity has come. The recently application of modern drug design promise to bring significant development in the fight against TB. In present review we discussed brief introduction of tuberculosis.

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Section: Quinolonesmentioning

confidence: 99%

Anti-tubercular activity of some six membered heterocycle compounds

Asif¹

2019

Preprint

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“…Thiourea is a simple and well-known chemical entity, and its derivatives represent another important class of organic molecules having broad spectrum of pharmacological activity. [11][12][13][14][15] Synthetic combinations of urea and thiourea connected with benzothiazole moiety resulted in DNA topoisomerases and HIV reverse transcriptase inhibitors. 16,17 Here, we present the synthesis, luminescence property investigation and cytotoxic potential evaluation of thiourea derivatives ( Figure 1).…”

Section: Introductionmentioning

confidence: 99%

Novel synthetic aromatic thiourea derivatives and investigations on their cytotoxic potential efficacy

Ray

John

Pooppadi

et al. 2020

Journal of Heterocyclic Chem

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Aromatic thiourea derivatives were synthesized by standard reactions from isothiocyanates in high yield. An efficient one‐pot synthesis of primary amine with carbon disulfide involving the intermediate dithiocarbamate conversion using T3P (propane phosphonic anhydride) to isothiocyanate is reported. Newly synthesized compounds showed excellent luminescence property. Cytotoxic investigation with different human cancer cell lines showed IC50 values varying from of 17 to 40 μM for N‐phenethyl‐3,4‐dihydroisoquinoline‐2(1H)‐carbothioamide (SCR172) among other molecules. Increase in Sub G1 population and increased depolarisation of mitochondria were evident in cells treated with SCR172, suggesting its role as a cancer therapeutic agent. This provides a lead structure for further synthetic modifications.

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“…As part of our ongoing investigation of the scope of antitubercular heterocyclic systems containing the thiourea moiety , we now report our results on the preparation and properties of new 1‐(4‐methylpiperazin‐1‐yl)thioureas, including preliminary findings on their activities against Mtb. In the event, the reaction of 1‐amino‐4‐methylpiperazine ( I ) with a variety of isothiocyanates ( II ) in ethanol or toluene formed the corresponding thioureas ( III ) as stable crystalline solids in good yield and purity (Scheme ).…”

Section: Introductionmentioning

confidence: 99%