29546-25-6Relevant academic research and scientific papers
Efficient formation of C–S bond using heterocyclic thiones and arynes
An, Yu,Xu, Gang,Cai, Menglu,Wang, Shihui,Wang, Xiao zhong,Chen, Yingqi,Dai, Liyan
, (2020/12/23)
Phenylthio heterocyclic compounds are widely used because of their diverse biological activities and medicinal prospects. Here, a facile method was reported. An arylation of 1,3,4-oxa(thia)diazol-2-thiones reacting with arynes to build C(aryl)-S bonds in the presence of CsF had good yields and excellent selectivity. The reaction was completed in short time without using expensive reagents and catalysts. Present reaction system is an efficient procedure to process phenylthio heterocyclic compounds and reveals a sustainable method and better application prospects in future organic synthesis.
Antibacterial drug for targeted therapy of staphylococcal infection by synergizing with antibiotic as well as synthesis method and application of antibacterial drug
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Paragraph 0033; 0035, (2018/12/05)
The invention designs and synthesizes a novel antibacterial drug ASC for staphylococcus aureus based on a beta-lactam ring of a parent nucleus structure of beta-lactam antibiotic molecules, wherein the ASC is an antibacterial reagent and is also a broad-spectrum inhibitor of beta-lactam antibiotic drug-resistant target protein metal beta-lactamase; the ASC can synergize with three kinds of 7 to 8antibiotics such as beta-lactams, aminoglycosides and tetracyclines to carry out targeted therapy on the staphylococcal infection. The vitality of the antibiotics is increased by 4 to 128 times by combining with 1 [mu]g/ml dosage of ASC.
Azolylthioacetamides as a potent scaffold for the development of metallo-β-lactamase inhibitors
Xiang, Yang,Chang, Ya-Nan,Ge, Ying,Kang, Joon S.,Zhang, Yi-Lin,Liu, Xiao-Long,Oelschlaeger, Peter,Yang, Ke-Wu
supporting information, p. 5225 - 5229 (2017/11/13)
In an effort to develop new inhibitors of metallo-β-lactamases (MβLs), twenty-eight azolylthioacetamides were synthesized and assayed against MβLs. The obtained benzimidazolyl and benzioxazolyl substituted 1–19 specifically inhibited the enzyme ImiS, and 10 was found to be the most potent inhibitor of ImiS with an IC50 value of 15 nM. The nitrobenzimidazolyl substituted 20–28 specifically inhibited NDM-1, with 27 being the most potent inhibitor with an IC50 value of 170 nM. Further studies with 10, 11, and 27 revealed a mixed inhibition mode with competitive and uncompetitive inhibition constants in a similar range as the IC50 values. These inhibitors resulted in a 2–4-fold decrease in imipenem MIC values using E. coli cells producing ImiS or NDM-1. While the source of uncompetitive (possibly allosteric) inhibition remains unclear, docking studies indicate that 10 and 11 may interact orthosterically with Zn2 in the active site of CphA, while 27 could bridge the two Zn(II) ions in the active site of NDM-1 via its nitro group.
Antibacterial activities against rice bacterial leaf blight and tomato bacterial wilt of 2-mercapto-5-substituted-1,3,4-oxadiazole/thiadiazole derivatives
Li, Pei,Shi, Li,Gao, Man-Ni,Yang, Xia,Xue, Wei,Jin, Lin-Hong,Hu, De-Yu,Song, Bao-An
supporting information, p. 481 - 484 (2015/02/18)
In this study, a series of 2-mercapto-5-substituted-1,3,4-oxadiazole/thiadiazole derivatives were synthesized and evaluated for their antibacterial activities against rice bacterial leaf blight and tomato bacterial wilt caused by Xanthomonas oryzae pv. oryzae (Xoo) and Ralstonia solanacearum (R. solanacearum) via the turbidimeter test in vitro. Antibacterial bioassays indicated that most compounds demonstrated appreciable antibacterial bioactivities against Xoo and R. solanacearum. Among the title compounds, compound 4i demonstrated the best inhibitory effect against Xoo and R. solanacearum with half-maximal effective concentration (EC50) values of 14.69 and 15.14 μg/mL, respectively, which were even better than those of commercial agents Bismerthiazol and Thiodiazole Copper. In vivo antibacterial activities tests under greenhouse conditions revealed that the control efficiency of compound 4i against rice bacterial leaf blight and tobacco bacterial wilt were better than those of Bismerthiazol and Thiodiazole Copper. Meanwhile, field trials also indicated that compound 4i demonstrated appreciable control efficiency against rice bacterial leaf blight and tomato bacterial wilt.
Design, synthesis, and antibacterial activity against rice bacterial leaf blight and leaf streak of 2,5-substituted-1,3,4-oxadiazole/thiadiazole sulfone derivative
Li, Pei,Shi, Li,Yang, Xia,Yang, Lei,Chen, Xue-Wen,Wu, Fang,Shi, Qing-Cai,Xu, Wei-Ming,He, Ming,Hu, De-Yu,Song, Bao-An
, p. 1677 - 1680 (2014/04/17)
A series of 2,5-substituted-1,3,4-oxadiazole/thiadiazole sulfone derivatives were synthesized and evaluated for their antibacterial activities against rice bacterial leaf blight and leaf streak caused by Xanthomonas oryzae pv. oryzae and Xanthomonas oryzae pv. oryzicolaby via the turbidimeter test in vitro. Antibacterial bioassay results indicated that most compounds demonstrated good inhibitory effect antibacterial bioactivities against rice bacterial leaf blight and leaf streak. Among the title compounds, compound 6c demonstrated the best inhibitory effect against rice bacterial leaf blight and leaf streak with half-maximal effective concentration (EC50) values of 1.07 and 7.14 μg/mL, respectively, which were even better than those of commercial agents such as Bismerthiazol and Thiediazole Copper. In vivo antibacterial activities tests at greenhouse conditions demonstrated that the controlling effect of compounds 6c (43.5%) and 6g (42.4%) against rice bacterial leaf blight were better than those of Bismerthiazol (25.5%) and Thiediazole Copper (37.5%).
Thiadiazole-based Thioglycosides as Sodium-glucose Co-transporter 2 (SGLT2) Inhibitors
Gao, Yunlong,Zhao, Guilong,Liu, Wei,Wang, Yuli,Xu, Weiren,Wang, Jianwu
scheme or table, p. 605 - 612 (2010/10/19)
A series of thiadiazole-based thioglycosides were synthesized as SGLT2 inhibitors from D-glucose, D-galactose and a variety of phenylacetic acids via a convenient protocol in 8 steps and evaluated in vivo with an oral glucose tolerance test (OGTT), and 5-benzyl-1,3,4-thiadiazol-2-yl 1-thio-β-D-glucopyranoside (1a) was the most efficacious to suppress the blood glucose excursion during OGTT.
Acetazolamide-related compounds, process for their preparation, and pharmaceutical composition containing the same
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, (2008/06/13)
Compounds related to acetazolamide and to its N-methyl derivatives, of the formulae: STR1 wherein Y is one of the following groups: STR2 R1 being a straight or branched alkylene or arylalkylene, or a phenylene, and the processes for their preparation; the compounds so obtained are inhibitors of carbonic anhydrase like acetazolamide but, in addition, they are well absorbed topically so that they can be used as drugs for treating glaucoma.
Acetazolamide-related compounds, process for their preparation, and pharmaceutical composition containing the same
-
, (2008/06/13)
Compounds related to acetazolamide and to its N--methyl derivatives, of the formulae: wherein Y is one of the following groups: R1 being a straight or branched alkylene or arylalkylene, or a phenylene, and the processes for their preparation; the compounds so obtained are inhibitors of carbonic anhydrase like acetazolamide but, in addition, they are well absorbed topically so that they can be used as drugs for treating glaucoma.
