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含苯并咪唑环的1,3,4-噻二唑酰胺衍生物的合成与抑菌活性
Synthesis and fungicidal activity of 1,3,4-thiadiazole amide derivatives containing benzimidazole moiety
郑广进,黄欢
- , 2017,
Abstract: 为寻找新型活性杂环化合物，通过活性亚结构拼接，以取代苯酚和氯乙酸为起始原料，经醚化、缩合、烃基化和氨解反应，设计并采用微波辅助合成了6种未见文献报道的含苯并咪唑环的1，3，4-噻二唑酰胺衍生物，其结构经红外和核磁共振氢谱确证。初步抑菌活性测试结果表明，所有目标化合物对5种供试病原菌都表现出一定的抑菌活性，其中，化合物7c、7d、7e和7f在50 mg/L下对5种供试病原菌的抑制率均达到80%以上。
In order to discover novel heterocyclic compounds with biological activity, six novel 1,3,4-thiadiazole amide derivatives containing benzimidazole moiety were synthesized under microwave assisted condition via etherification, condensation, hydrocarbylation and the ammonolysis reactions with substituted phenol and chloracetic acid as raw materials. The structures were confirmed by IR and 1H NMR. Fungicidal activity test showed that all the compounds exhibit fungicidal activity against the five fungi tested at the concentration of 50 mg/L, among them, the inhibition rate of 7c, 7d, 7e and 7f against the fungi tested were above 80%.
Determination of Metal Ions in Fuel Ethanol after Preconcentration on 5-Amino-1,3,4-Thiadiazole-2-Thiol Modified Silica Gel
Gomes, Luis A. de Melo;Padilha, Pedro de Magalh？es;Moreira, José Celso;Dias Filho, Newton L.;Gushikem, Yoshitaka;
Journal of the Brazilian Chemical Society , 1998, DOI: 10.1590/S0103-50531998000500015
Abstract: this work describes the synthesis and characterization of 5-amino-1,3,4-thiadiazole-2-thiol modified silica gel (siatt), and the results of a study of the adsorption and preconcentration (in batch, and in flow using a column technique) of cd(ii), co(ii), cu(ii), fe(iii), ni(ii), pb(ii) and zn(ii) in ethanol medium. the adsorption capacities for each metal ion were (in mmol g-1): cd(ii) = 0.11, co(ii) = 0.10, cu(ii) = 0.20, fe(iii) = 0.20, ni(ii) = 0.16, pb(ii) = 0.08 and zn(ii) = 0.12. the results obtained in the flow experiments, showed a recovery of ca. 100% of the metal ions adsorbed in a column packed with 2 g of siatt, using 5 ml of 2.0 mol l-1 hcl solution as eluent. the sorption-desorption of the metal ions made possible the development of a preconcentration method and quantification by flame aas of metal ions at trace level in fuel ethanol.
Determination of Metal Ions in Fuel Ethanol after Preconcentration on 5-Amino-1,3,4-Thiadiazole-2-Thiol Modified Silica Gel
Gomes Luis A. de Melo,Padilha Pedro de Magalh？es,Moreira José Celso,Dias Filho Newton L.
Journal of the Brazilian Chemical Society , 1998,
Abstract: This work describes the synthesis and characterization of 5-amino-1,3,4-thiadiazole-2-thiol modified silica gel (SiATT), and the results of a study of the adsorption and preconcentration (in batch, and in flow using a column technique) of Cd(II), Co(II), Cu(II), Fe(III), Ni(II), Pb(II) and Zn(II) in ethanol medium. The adsorption capacities for each metal ion were (in mmol g-1): Cd(II) = 0.11, Co(II) = 0.10, Cu(II) = 0.20, Fe(III) = 0.20, Ni(II) = 0.16, Pb(II) = 0.08 and Zn(II) = 0.12. The results obtained in the flow experiments, showed a recovery of ca. 100% of the metal ions adsorbed in a column packed with 2 g of SiATT, using 5 mL of 2.0 mol L-1 HCl solution as eluent. The sorption-desorption of the metal ions made possible the development of a preconcentration method and quantification by Flame AAS of metal ions at trace level in fuel ethanol.
Synthesis and Antiviral Activity of 5？(4？Chlorophenyl)-1,3,4-Thiadiazole Sulfonamides
Zhuo Chen,Weiming Xu,Keming Liu,Song Yang,Huitao Fan,Pinaki S. Bhadury,De-Yu Huang,Yuping Zhang
Molecules , 2010, DOI: 10.3390/molecules15129046
Abstract: Starting from 4-chlorobenzoic acid, 10 new 5-(4-chlorophenyl)-N-substituted-N-1,3,4-thiadiazole-2-sulfonamide derivatives were synthesized in six-steps. Esterification of 4-chlorobenzoic acid with methanol and subsequent hydrazination, salt formation and cyclization afforded 5-(4-chlorophen-yl)-1,3,4-thiadiazole-2-thiol (5). Conversion of this intermediate into sulfonyl chloride 6, followed by nucleophilic attack of the amines gave the title sulfonamides 7a-7j whose structures were confirmed by NMR, IR and elemental analysis. The bioassay tests showed that compounds 7b and 7i possessed certain anti-tobacco mosaic virus activity.
Synthesis and biological activity of 5-nitrofuran-containing (1,3,4-thiadiazol-2-yl)piperazine moieties as a new type of anti-Helicobacter pylori heterocycles
MOHAMMAD HASSAN MOSHAFI,AZADEH YAHYA-MEYMANDI,SEYED ESMAEIL SADAT-EBRAHIMI,SAEED EMAMI
Journal of the Serbian Chemical Society , 2011,
Abstract: In order to find new and potent drug candidates for the treatment of Helicobacter pylori infections in this study attention was focused on the synthesis and anti-H. pylori activity of a series of 5-(5-nitrofuran-2-yl)-1,3,4-thiadiazoles containing piperazinyl functionality at the C-2 position of the 1,3,4--thiadiazole ring. The synthesis of 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2--yl]piperazine derivatives 3a–h and pyrrolidine derivative 3i was achieved with a versatile and efficient synthetic route via 2-chloro-5-(5-nitrofuran-2-yl)-1,3,4--thiadiazole. The inhibitory activity of the new derivatives 3a–i against twenty clinical H. pylori strains was evaluated by the disc diffusion method and compared with the commercially available standard drug metronidazole. Resulting biological data indicated that most compounds exhibited strong inhibitory activity even at doses lower than 2 μg/disc (average zone of inhibition >20 mm) while metronidazole had little or no growth inhibition at this dose. Compound 3c containing the N-benzoylpiperazin-1-yl moiety showed the most potent inhibitory activity.
Design of New Thiadiazole Derivatives with Improved Antidiabetic Activity  [PDF]
Chiépi Nadège Dominique Dou, Georges Stéphane Dembele, Mamadou Guy-Richard Kone, Nanou Tiéba Tuo, Fandia Konate, Adama Niare, Panaghiotis Karamanis, Nahossé Ziao
Computational Chemistry (CC) , 2023, DOI: 10.4236/cc.2023.113005
Abstract: Diabetes is a serious, long-term (or chronic) disease that occurs when a person’s blood sugar levels are high because their body cannot produce enough insulin, or does not produce enough insulin or that it cannot effectively use the insulin it produces. According to the literature, this disease has several causes, but certain types of diabetes such as type 2 diabetes are most closely linked to a metabolic disorder due to abdominal obesity. Thus, the number of individuals with type 2 diabetes is increasing. It is with this in mind that we work to improve human health. The aim of this study is to design new derivatives of 1,3,4-thiadiazole with improved antidiabetic activity by the mathematical model of multiple linear regression (MLR) established previously. The analysis of the effect on the substituents influencing the antidiabetic activity, fourteen (14) new molecules coded CDTH were generated and presenting values of the potential of inhibitory concentration higher than that of the base compound (pIC50 = 2.526). But thirteen (13) of these new compounds belong to the domain of applicability of the MLR model established previously. In addition, the thermodynamic quantities of formation formed at 298K have been calculated. Lipinski’s rule and pharmacokinetic properties proved that five (5) (TH4, TH9, TH10, TH13 and TH14) new molecules can be used as diabetes medicine.
含1,3,4-噻二唑的吡啶联吡唑乙酰胺类化合物的合成及除草活性
Synthesis and herbicidal activity of substituted 2-(1-(3-chloropyridin-2-yl)-3,5-dimethyl-1H-pyrazol-4-yl) acetic acid derivatives containing 1, 3, 4-thiadiazole
胡燕红,何海琴,刘幸海,翁建全,谭成侠
- , 2017,
Abstract: 以乙酰丙酮、溴乙酸乙酯和2，6-二氯吡啶为起始原料，经取代、肼基化、环合、水解、酸化及缩合等反应，得到9个未见文献报道的吡啶联吡唑乙酰基类化合物B1~B9。其结构均经核磁共振氢谱和质谱表征。初步生物活性测定表明：在150 g/hm2的处理剂量下，大部分目标化合物表现出一定的除草活性，其中化合物B2、B3、B6和B8对苘麻Abutilon theophrasti Medicus、反枝苋Amaranthus retroflexus和凹头苋Amaranthus lividus L.生长的抑制率接近100%。
Nine novel 2-(1-(3-chloro pyridin-2-yl)-3,5-dimethyl-1H-pyrazol-4-yl) acetic acid derivatives B1-B9 were synthesized from acetylacetone, ethyl bromoacetate and 2,6-dichloropyridine. The synthesis route included a series of reactions such as substitution, alkylation, cyclization, hydrolysis, and acidification condensation. The chemical structures were characterized by 1H NMR and MS. Preliminary bioassay showed that most of the above compounds displayed herbicidal activities at the concentration of 150 g/hm2. The inhibition rates of B2, B3, B6 and B8 against Abutilon theophrasti Medicus, Amaranthus retroflexus and Amaranthus lividus L. were nearly 100%.
1,3,4-THIADIAZOLE AS ANTIMICROBIAL AGENT: A REVIEW
Mehnaz Kamal,Ashok K. Shakya,Talha Jawaid
International Journal of Biomedical Research , 2013, DOI: 10.7439/ijbr.v2i1.80
Abstract: 1,3,4-Thiadiazole nucleus exhibited remarkable pharmacological activities. Literature indicates that compounds having 1,3,4-Thiadiazole nucleus have wide range of pharmacological activities that include antibacterial, antifungal, antitubercular, antiviral, antileishmanial, anti-inflammatory, analgesic, CNS depressant, anticonvulsant, anticancer, antioxidant, antidiabetic, molluscicidal, antihypertensive, diuretic. The present review provides a broad view of the antimicrobial activity possessed by compounds having a 1,3,4-Thiadiazole nucleus.
1,3,4-THIADIAZOLE AS ANTIMICROBIAL AGENT: A REVIEW
Mehnaz Kamal,Ashok K. Shakya,Talha Jawaid
International Journal of Biomedical Research , 2011, DOI: 10.7439/ijbr.v2i1.80
Abstract: 1,3,4-Thiadiazole nucleus exhibited remarkable pharmacological activities. Literature indicates that compounds having 1,3,4-Thiadiazole nucleus have wide range of pharmacological activities that include antibacterial, antifungal, antitubercular, antiviral, antileishmanial, anti-inflammatory, analgesic, CNS depressant, anticonvulsant, anticancer, antioxidant, antidiabetic, molluscicidal, antihypertensive, diuretic. The present review provides a broad view of the antimicrobial activity possessed by compounds having a 1,3,4-Thiadiazole nucleus.
SYNTHESIS AND ANTICONVULSANT ACTIVITY OF NOVEL 2-AMINO-5-[4-CHLORO-2-(2-CHLOROPHENOXY) PHENYL]-1,3,4-THIADIAZOLE DERIVATIVES
Foroumadi A.,Sheibani V.,Sakhteman A.,Rameshk M
DARU : Journal of Pharmaceutical Sciences , 2007,
Abstract: Several novel 2-amino-5-[4-chloro-2-(2-chlorophenoxy)phenyl]-1,3,4-thiadiazole derivatives 4a-d were synthesized and their anticonvulsant activity was determined by evaluation of the ability of theses compounds to protect mice against convulsion induced by a lethal doses of pentylentetrazole (PTZ) and maximal electroshock (MES). The result of anticonvulsant data shows that among the synthesized compounds, 5-[4-chloro-2-(2-chlorophenoxy)phenyl]-N-ethyl-1,3,4-thiadiazol-2-amine 4c was the most active compound in both MES and PTZ tests with an ED50 of 20.11 and 35.33 mg/kg, respectively.
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