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Mechanisms of action
Published in Fazal-I-Akbar Danish, Ahmed Ehsan Rabbani, Pharmacology in 7 Days for Medical Students, 2018
Fazal-I-Akbar Danish, Ahmed Ehsan Rabbani
It is pertinent to mention here that BDZs are not GABA-mimetic (meaning they do not have effects like GABA) and the presence of GABA in the CNS is necessary for the actions of BDZs. If we inhibit the synthesis of GABA with thiosemicarbazide, BDZs become ineffective. Similarly if we block post-synaptic receptors of GABA with bicuculline, BDZs again will become ineffective.
T
Published in Anton Sebastian, A Dictionary of the History of Medicine, 2018
Thioactazone [Greek: theion, sulfur] Thiosemicarbazide was shown to be active against Mycobacterium tuberculosis in vitro by Peak and co-workers in 1944. Work was continued by Gerhard Johannes Paul Domagk (1895–1964) in Germany and led to its introduction as a mainline drug against tuberculosis.
Cancer
Published in Stephen P. Coburn, The Chemistry and Metabolism of 4′-Deoxypyridoxine, 2018
Mihich and Nichol324 demonstrated that their deoxypyridoxine contained less than 0.01% pyridoxine. In the presence of normal B6, intraperitoneal administration of 50 and 100 mg/kg/day had little effect on tumor sarcoma 180 growth in mice. Combining the treatment with a B6-deficient diet did cause inhibition of tumor growth but not regression, probably because the antagonist simultaneously interfered with host defenses. Isonicotinic acid hydrazide alone had no effect. However, deoxypyridoxine combined with isonicotinic acid hydrazide did produce inhibition of tumor growth even on a normal B6 diet but again failed to produce the regression seen with the B6 deficiency alone. Inhibition of tumor growth was observed if dietary depletion was started 2 weeks prior to tumor implantation but not if the deficient diet was started on the day of implantation. Inhibition of tumor growth was observed if treatment with a B6-deficient diet containing 10 to 50 mg deoxypyridoxine per kilogram was started on the day of implantation, However, tumors in the deoxypyridoxine group failed to regress like the tumors in mice which had been depleted for 2 weeks prior to implantation. Solid tumors were less responsive to the effects of the drugs or B6 deficiency. B6 deficiency alone had no effect on ascitic S-180 inoculated subcutaneously. However, combining the deficient diet with deoxypyridoxine did produce inhibition. Thiosemicarbazide inhibited tumor growth without affecting tumor regression. The authors concluded that clinical trials in humans are warranted.
4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Daniela Secci, Simone Carradori, Anél Petzer, Paolo Guglielmi, Melissa D’Ascenzio, Paola Chimenti, Donatella Bagetta, Stefano Alcaro, Gokhan Zengin, Jacobus P. Petzer, Francesco Ortuso
4–(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives (1–36) were synthesised in high yields as reported in our previous communications (Scheme 1)26. The appropriate carbonyl compound was reacted with thiosemicarbazide in ethanol at room temperature and in presence of acetic acid as the catalyst (Scheme 1, a). The Hantzsch reaction between the resulting thiosemicarbazone and 2-bromo-3′-nitroacetophenone in the same conditions of solvent and temperature gave the corresponding 4–(3-nitrophenyl)thiazol-2-ylhydrazone derivatives (Scheme 1, b). For the synthesis of the thiophene-containing 4-(3-amino)thiazol-2-ylhydrazone derivative (37), reduction of the nitro group was performed using sodium dithionite previously solubilised in a basic aqueous solution and added dropwise to a stirring suspension of compound 3 in tetrahydrofuran at room temperature (Scheme 1, c). All the synthesised products were washed with petroleum ether and diethyl ether and purified by chromatography using silica gel as stationary phase and the appropriate mixtures of ethyl acetate and petroleum ether as mobile phase. Characterisation and purity assessment of the synthesised compounds were carried out by melting point determination, spectroscopic methods (IR, 1H and 13C NMR) and elemental analysis.
Identification of 3-(piperazinylmethyl)benzofuran derivatives as novel type II CDK2 inhibitors: design, synthesis, biological evaluation, and in silico insights
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Wagdy M. Eldehna, Raed M. Maklad, Hadia Almahli, Tarfah Al-Warhi, Eslam B. Elkaeed, Mohammed A. S. Abourehab, Hatem A. Abdel-Aziz, Ahmed M. El Kerdawy
The thiosemicarbazide derivatives 9a-i showed CDK2 inhibitory concentration (IC50) range of 40.91–322.1 nM. The m-trifluoromethyl derivative 9h showed potent inhibitory activity relative to that of staurosporine (IC50 = 40.91 vs 56.76 nM, respectively). Compounds 9b, 9d, 9e, 9 g and 9i showed comparable CDK2 inhibitory activity to that of staurosporine (the used reference standard) with IC50 less than 100 nM. Compounds 9a, 9c and 9f showed weak inhibitory activity compared to that of staurosporine (IC50 = 322.10, 214.00 and 119.00 nM, respectively, vs 56.76 nM) (Table 1).
Novel thiazolidinone-containing compounds, without the well-known sulphonamide zinc-binding group acting as human carbonic anhydrase IX inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Özlen Güzel-Akdemir, Andrea Angeli, Kübra Demir, Claudiu T. Supuran, Atilla Akdemir
The chemical synthesis of 3a-o and 4a-k compounds is outlined in Scheme 1. The synthesis of several intermediate thiosemicarbazide derivatives except 2g and 2h were previously reported elsewhere32,39. 4-Thiazolidinones were prepared starting from 2-hydroxy-2-phenylacetohydrazide (1) which afforded intermediate thiosemicarbazides (2) on reaction with aryl isothiocyanates. The thiosemicarbazides in turn furnished 3 and 4 with ethyl α-bromoacetate and ethyl α-bromopropionate, respectively.