36107-11-6Relevant academic research and scientific papers
Expedient discovery for novel antifungal leads: 1,3,4-Oxadiazole derivatives bearing a quinazolin-4(3H)-one fragment
Chai, Jianqi,Chen, Min,Jin, Fei,Kong, Xiangyi,Wang, Xiaobin,Xue, Wei,Yang, Chunlong
, (2021/08/03)
Developing novel fungicide candidates are intensively promoted by the rapid emergences of resistant fungi that outbreak on agricultural production. Aiming to discovery novel antifungal leads, a series of 1,3,4-oxadiazole derivatives bearing a quinazolin-4(3H)-one fragment were constructed for evaluating their inhibition effects against phytopathogenic fungi in vitro and in vivo. Systematically structural optimizations generated the bioactive molecule I32 that was identified as a promising inhibitor against Rhizoctonia solani with the in vivo preventative effect of 58.63% at 200 μg/mL. The observations that were captured by scanning electron microscopy and transmission electron microscopy demonstrated that the bioactive molecule I32 could induce the sprawling growth of hyphae, the local shrinkage and rupture on hyphal surfaces, the extreme swelling of vacuoles, the striking distortions on cell walls, and the reduction of mitochondria numbers. The above results provided an indispensable complement for the discovery of antifungal lead bearing a quinazolin-4(3H)-one and 1,3,4-oxadiazole fragment.
Synthesis, characterization and antioxidant activity of bis (arylsulfonylmethyl/arylaminosulfonylmethylazolyl) pyridines
Gunthanakkala, Anil Kumar,Mangali, Madhu Sekhar,Venkatapuram, Padmavathi,Adivireddy, Padmaja
, p. 4164 - 4174 (2020/09/07)
A new class of bis(arylsulfonylmethylazolyl)pyridines and bis(arylaminosulfonylmethyl-azolyl)pyridines were synthesized from the synthetic intermediates methyl arylsulfonylacetic acid hydrazide and methyl arylaminosulfonylacetic acid hydrazide adopting a green methodology-ultrasonication. All the synthesized compounds were resulted in higher yield and in shorter reaction times. The spectral parameters such as IR, 1H NMR, 13C NMR, mass and microanalyzes were used to determine the structures of all the synthesized compounds and were assayed for antioxidant activity. The bis(arylaminosulfonylmethylazolyl)pyridines showed higher radical scavenging activity than the bis(arylsulfonylmethylazolyl)pyridines. Besides, unsubstituted, and methyl substituted compounds exhibited greater activity. Among all the tested compounds 8b and 11b were identified as potential antioxidants.
Synthesis and biological evaluation of 2-(4-substituted benzene-1-sulfonyl)-N'-(substituted-1-sulfonyl)acetohydrazide as antibacterial agents
Li, Pei,Zhou, Junliang,Liu, Yan,Wang, Xiang
, p. 4559 - 4565 (2020/07/10)
In this study, a series of new sulfone derivatives containing a sulfonohydrazide moiety were synthesized and their structures were determined using 1H NMR, 13C NMR, and HRMS. Then, the in vitro antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas axonopodis pv. citri (Xac) were evaluated by performing turbidimeter test. Bioactivity results showed that compound 2-(4-fluorobenzene-1-sulfonyl)-N′-(4-fluorobenzene-1-sulfonyl)acetohydrazide (5g) revealed the best antibacterial activities against Xoo and Xac, with the 50percent effective concentration (EC50) values of 25 and 36?μg/mL, respectively, which were superior to those of thiodiazole copper (110 and 230?μg/mL, respectively) and bismerthiazol (84 and 146?μg/mL, respectively).
Design, Synthesis, and Evaluation of New Sulfone Derivatives Containing a 1,3,4-Oxadiazole Moiety as Active Antibacterial Agents
Li, Pei,Hu, Deyu,Xie, Dandan,Chen, Jixiang,Jin, Linhong,Song, Baoan
, p. 3093 - 3100 (2018/04/05)
This study aimed to synthesize some new sulfone derivatives containing a 1,3,4-oxadiazole moiety and investigate their in vitro antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas axonopodis pv. citri (Xac), the pathogens
2,5-substituent-1,3,4-oxadiazole sulfone derivative as well as preparation method and application thereof
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Paragraph 0097; 0098; 0109; 0110; 0121; 0122; 0133; 0134, (2018/06/16)
The invention discloses a 2,5-substituent-1,3,4-oxadiazole sulfone derivative as well as a preparation method and application thereof. The 2,5-substituent-1,3,4-oxadiazole sulfone derivative has a general formula shown in a formula (I), wherein R1 is 4-chlorine or 4-fluorine; and R2 is methyl, ethyl, propyl, n-butyl, n-pentyl, benzyl, 4-chlorobenzyl or 4-fluorobenzyl. The 2,5-substituent-1,3,4-oxadiazole sulfone derivative disclosed by the invention has good activity on rice bacterial leaf blight and xanthomonas citri and is simple in structure, simple in preparation technology and low in production cost. (The formula (I) is described in the specification).
2. 5 - Substituted - 1, 3, 4 - oxadiazoles double-sulfones derivatives, preparation method and application thereof (by machine translation)
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Paragraph 0074; 0075; 0089; 0103; 0117; 0131, (2018/07/30)
The invention discloses a 2, 5 - substituted - 1, 3, 4 - oxadiazoles double-sulfones derivatives, preparation method and application thereof, having formula (I) of the general formula, wherein: R1 For the 4 - chloro or 4 - fluoro; R2 For hydroxy, methyl, ethyl, benzyl, 4 - benzylic or 4 - fluorobenzyl. The invention relates to a rice BLB and citrus ulcer bacteria has better activity, the structure is simple, the preparation process is simple, the production cost is low. (by machine translation)
Synthesis and antimicrobial activity of pyrazolyl 1,3,4-oxadiazoles
Padmavathi, Venkatapuram,Reddy, Gali Sudhakar,Reddy, Guda Dinneswara,Payani, Thalari
scheme or table, p. 482 - 493 (2010/04/06)
The pyrazolyl oxadiazoles are synthesized from arylsulfonylacetic acid methyl ester and benzylsulfonylacetic acid methyl ester. Preliminary antimicrobial screening of the compounds showed that bis heterocycles with a chloro-substituted benzyl moiety exhibited high activity. Copyright Taylor & Francis Group, LLC.
Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles
Padmavathi,Sudhakar Reddy,Padmaja,Kondaiah,Ali-Shazia
experimental part, p. 2106 - 2112 (2009/09/25)
A new class of 1,3,4-oxadiazoles were prepared from acid hydrazides on treatment with different carboxylic acids in the presence of phosphorus oxychloride. Interconversion of oxadiazoles to thiadiazoles and triazoles was carried out with appropriate reagents. The antimicrobial and cytotoxic activities of compounds 7a-d to 12a-d were tested. Compounds 10d and 12d showed pronounced antimicrobial activity. Further, compound 10d exhibited maximum cytotoxicity.
Synthesis of thiadiazoles, triazoles and oxadiazoles from sulfonyl acetic acids via a common route
Padmavathi, Venkatapuram,Thriveni, Pinnu,Reddy, Boggu Jagan Mohan,Padmaja, Adivireddy
, p. 113 - 116 (2007/10/03)
A new class of five membered heterocycles, thiadiazoles, triazoles and oxadiazoles were prepared from sulfonyl acetic acids via acid hydrazides.
