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Triafur
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Five patients used either an ointment or suppositories containing 0.7% triafur for hemorrhoids or pruritus ani and developed contact dermatitis. Patch tests were positive in all to the medicament and to triafur 1% pet. By studying the cross-reaction patterns, it was established that the nitro group on the furan ring and the close bonding of the furan and thiadiazole rings were necessary to elicit a reaction. Tests with nitrofurantoin and nitrofurazone, which have no thiadiazole ring, were negative (2).
Lysosomal acid lipase deficiency: Wolman disease/cholesteryl ester storage disease
Published in William L. Nyhan, Georg F. Hoffmann, Aida I. Al-Aqeel, Bruce A. Barshop, Atlas of Inherited Metabolic Diseases, 2020
The measurement of lysosomal acid lipase in blood is complicated by the fact that there are other lipases in whole blood. A method has been developed that takes advantage of specific 3, 4-disubstituted thiadiazole carbamate inhibitors, the most effective of which was named Lalistat 2 [41]. The compound has no effect on pancreatic lipase. The method clearly distinguishes normal individuals, carriers and especially patients. Chemical analysis of tissues in both Wolman and cholesteryl ester storage diseases reveals increased quantities of cholesteryl esters and triglycerides [9, 10, 42]. This may be readily demonstrated by thin layer chromatography. A high-performance liquid chromatography (HPLC) method for the quantification of lipids is useful in the differentiation of Wolman disease, Niemann-Pick disease, and Gaucher disease [43]. It may be used with fibroblasts, lymphocytes, or leukocytes, as well as tissue samples. Lipid analysis has most commonly been reported of the liver and spleen, where the triglyceride content may be as much as 10 and 350 times the normal value, and the total cholesterol content is always increased [42]. An eight-fold elevation has been reported in adrenal [12]. Storage of cholesteryl ester has also been documented in fibroblasts [44]. Unusual oxygenated steryl esters such as those of 7-α-hydroxycholesterol have been found in tissues [42].
Physiology and Growth
Published in Paul Pumpens, Single-Stranded RNA Phages, 2020
Large sets of compounds were tested routinely on the effect on the RNA phage propagation. Thus, 26 plant growth regulators including herbicides were investigated for their effect on the bacterial growth and multiplication of phages including the phages M12 and Qβ (Menzel et al. 1975). Some of herbicides inhibited the phage M12 propagation at different stages (Touré and Stenz 1977). Some substituted thioureas were found to produce strong inhibitory effect on the phage M12 replication (Rehnig and Schuster 1978). The number of the M12 and Qβ plaques was diminished or increased depending on the kind of the 1,3,5-triazines tested (Stenz and Menzel 1978). Then, a set of morpholinium compounds was tested on the replication of the phages M12, f2, and Qβ, as well as on that of plant viruses: some drugs significantly enhanced plaque formation by the phages (Kluge et al. 1978). Some triazole compounds reduced plaque formation by the phages M12, f2, and Qβ and retarded the liberation of phages (Menzel and Kluge 1979, 1980). An 1,3,4-thiadiazole derivative inhibited the MS2 propagation (Varvaresou et al. 2000).
In vitro cytogenetic activity of 3-amino-4-[4-(dimethylamino)phenyl]-4,5-dihydro-1,2,5-thiadiazole 1,1-dioxide
Published in Drug and Chemical Toxicology, 2021
Zülal Atlı Şekeroğlu, Aliye Gediz Ertürk, Seval Kontaş Yedier, Vedat Şekeroğlu
Management of cancer still represents a major challenge in medicine despite significant progress achieved in anticancer therapy. Therefore, the development of novel effective anticancer drugs and strategies is eagerly being pursued (Rahman and Mohamed 2014). Heterocyclic organic compounds have several applications because of their structure (Grillo et al.2009). Thiadiazole is a versatile moiety that exhibits a wide variety of biological activities. Thiadiazole is a 5-membered ring system containing two nitrogen and one sulfur atom. They occur in nature in four isomeric forms: 1,2,3-thiadiazole, 1,2,5-thiadiazole, 1,2,4-thiadiazole and 1,3,4-thiadiazole (Bhuva et al.2011, Dawood and Farghaly 2017). It has been stated that compounds bearing thiadiazole rings exhibit antitumor, anti-inflammatory, antibacterial, antifungal, antiviral, anticonvulsant and antiparasitic activities. Therefore, a number of thiadiazole-containing drugs and medicinal agents are currently on the market (Li et al.2013, Dawood and Farghaly 2017).
Towards discovery of new leishmanicidal scaffolds able to inhibit Leishmania GSK-3
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Paula Martínez de Iturrate, Victor Sebastián-Pérez, Montserrat Nácher-Vázquez, Catherine S. Tremper, Despina Smirlis, Julio Martín, Ana Martínez, Nuria E. Campillo, Luis Rivas, Carmen Gil
After these initial studies, eleven showed a good inhibition of LdGSK-3 and some of them also phenotypic activities. From the initial set, eight were selected as representative members of the different chemical families according to their binding modes to the human enzyme as well as to their biological activities. As shown in Table 1, all the selected compounds inhibited LdGSK-3, except quinoline 11 and maleimide 13. Thiadiazolidinones (TDZDs) 1 and 2, and halomethylketones (HMKs) 5 and 14, inhibited LdGSK-3, and also showed a higher leishmanicidal activity on axenic amastigotes than on promastigotes. Compounds 3 and 4, both 5-imino-1,2,4-thiadiazoles (ITDZs), showed nil antiparasitic activities, despite their significant in vitro inhibition of the enzyme.
An updated patent review of glutaminase inhibitors (2019–2022)
Published in Expert Opinion on Therapeutic Patents, 2023
Danni Wang, Xiaohong Li, Guangyue Gong, Yulong Lu, Ziming Guo, Rui Chen, Huidan Huang, Zhiyu Li, Jinlei Bian
Computer-simulated binding maps of the GAC tetramer and BPTES show that the intermediate aliphatic chain has a direct effect on the interaction of the compound with key residues at the KGA metastable site. The esterophilic diethyl sulfide fraction primarily contributes to the low solubility of BPTES. To optimize its pharmacological properties and improve its hydrophilicity, studies have reported the modification of the diethyl sulfur portion into a ring structure or replaced the sulfur atom with other atoms. The thiadiazole portion containing a combination of symmetric and asymmetric five-membered heterocyclic or six-membered heterocyclic structures and different functional groups was substituted and modified. In a patent (CN110396089) [81] filed by Ruan et al. from Hangzhou Jiannifu Biotechnology Co., Ltd., a series of compounds with low or no toxicity and efficient targeting of KGA were synthesized by modifying the diethyl sulfide structure to Se–Se, S–S, or C–C and replacing the thiadiazole portion with different cyclic structures, and a representative superior compound 40 (CPD36) was obtained (Figure 5B). Replacing the thiadiazole structure with a benzene ring reduced its KGA inhibitory activity. However, the structural end modification with 3,5-dimethyl-1 H-pyrazole and isoindoline-1,3-dione enhanced the KGA inhibitory effect. It is important to note that the substitution of Se–Se in compound 40 (CPD36) by S–S to obtain compound 41 (CPD35) resulted in a ten-fold decrease in the KGA inhibitory activity and A549 cell inhibition effect, which suggests that Se–Se compounds inhibit KGA and tumor cells better than S–S compounds or C–C compounds. Further studies [82] revealed that diselenium compounds strongly inhibit the growth of breast (MCF-7) cells.