scholarly journals Discovery of Novel Dihydrolipoamide S-Succinyltransferase Inhibitors Based on Fragment Virtual Screening

2021 ◽  
Vol 22 (23) ◽  
pp. 12953
Author(s):  
Chengqian Wei ◽  
Junjie Huang ◽  
Yu Wang ◽  
Yifang Chen ◽  
Xin Luo ◽  
...  

A series of new oxadiazole sulfone derivatives containing an amide moiety was synthesized based on fragment virtual screening to screen high-efficiency antibacterial agents for rice bacterial diseases. All target compounds showed greater bactericidal activity than commercial bactericides. 3-(4-fluorophenyl)-N-((5-(methylsulfonyl)-1,3,4-oxadiazol-2-yl)methyl)acrylamide (10) showed excellent antibacterial activity against Xanthomonas oryzae pv. oryzae and Xanthomonas oryzae pv. oryzicola, with EC50 values of 0.36 and 0.53 mg/L, respectively, which were superior to thiodiazole copper (113.38 and 131.54 mg/L) and bismerthiazol (83.07 and 105.90 mg/L). The protective activity of compound 10 against rice bacterial leaf blight and rice bacterial leaf streak was 43.2% and 53.6%, respectively, which was superior to that of JHXJZ (34.1% and 26.4%) and thiodiazole copper (33.0% and 30.2%). The curative activity of compound 10 against rice bacterial leaf blight and rice bacterial leaf streak was 44.5% and 51.7%, respectively, which was superior to that of JHXJZ (32.6% and 24.4%) and thiodiazole copper (27.1% and 28.6%). Moreover, compound 10 might inhibit the growth of Xanthomonas oryzae pv. oryzae and Xanthomonas oryzae pv. oryzicola by affecting the extracellular polysaccharides, destroying cell membranes, and inhibiting the enzyme activity of dihydrolipoamide S-succinyltransferase.

2014 ◽  
Vol 81 (2) ◽  
pp. 688-698 ◽  
Author(s):  
L. Poulin ◽  
P. Grygiel ◽  
M. Magne ◽  
L. Gagnevin ◽  
L. M. Rodriguez-R ◽  
...  

ABSTRACTMultilocus variable-number tandem-repeat analysis (MLVA) is efficient for routine typing and for investigating the genetic structures of natural microbial populations. Two distinct pathovars ofXanthomonas oryzaecan cause significant crop losses in tropical and temperate rice-growing countries. Bacterial leaf streak is caused byX. oryzaepv. oryzicola, and bacterial leaf blight is caused byX. oryzaepv. oryzae. For the latter, two genetic lineages have been described in the literature. We developed a universal MLVA typing tool both for the identification of the threeX. oryzaegenetic lineages and for epidemiological analyses. Sixteen candidate variable-number tandem-repeat (VNTR) loci were selected according to their presence and polymorphism in 10 draft or complete genome sequences of the threeX. oryzaelineages and by VNTR sequencing of a subset of loci of interest in 20 strains per lineage. The MLVA-16 scheme was then applied to 338 strains ofX. oryzaerepresenting different pathovars and geographical locations. Linkage disequilibrium between MLVA loci was calculated by index association on different scales, and the 16 loci showed linear Mantel correlation with MLSA data on 56X. oryzaestrains, suggesting that they provide a good phylogenetic signal. Furthermore, analyses of sets of strains for different lineages indicated the possibility of using the scheme for deeper epidemiological investigation on small spatial scales.


2021 ◽  
Vol 905 (1) ◽  
pp. 012068
Author(s):  
Hadiwiyono ◽  
S H Poromarto ◽  
S Widono ◽  
R F Rizal

Abstract Bacterial leaf blight (BLB) caused by Xanthomonas oryzae pv. oryzae (Xoo) is one of the limiting factors in rice production. A local cultivar, rice “Pandanwangi” is a superior variety much preferred and cultivated by the farmers in Cianjur, West Java, Indonesia. The information about the response of “Pandangwangi” to Xoo is still poorly understood. This paper reports the results of the evaluation of “Pandanwangi” response against BLB. This research was conducted in a greenhouse with artificial inoculation using Xoo strains III, IV, and VIII with bacterial suspension at 108 cfu.mL−1. The results showed that the response of cv Pandanwangi to Xoo infection was different from the strain of Xoo. “Pandanwangi” cultivar was susceptible to Xoo strain III and VIII and very susceptible to strain IV.


2018 ◽  
Vol 45 (12) ◽  
pp. 1251 ◽  
Author(s):  
Shasmita ◽  
Harekrushna Swain ◽  
Anuprita Ray ◽  
Pradipta K. Mohapatra ◽  
Ramani K. Sarkar ◽  
...  

Bacterial leaf blight (BLB) is a serious threat for rice (Oryza sativa L.) cultivation caused by the bacterial pathogen Xanthomonas oryzae pv. oryzae. The pathogen mainly damages the leaf chlorophyllous tissue, resulting in poor photosynthesis and causing up to 50% reductions in grain yield. In the present work, we have compared the structural and functional ability of the chloroplast of three varieties of rice with different degrees of susceptibility (TN1, highly susceptible; IR-20, moderately resistant; DV-85, resistant to BLB) treated with riboflavin (1 and 2 mM) and infected with BLB, with chlorophyll fluorescence as a tool. As indicated by the chlorophyll fluorescence technique, the disease progress curve and yield data, riboflavin acted as an effective vitamin for inducing resistance against BLB. Plants treated with riboflavin showed improved PSII activity, more chlorophyll content and higher yield than the diseased plants.


2016 ◽  
Vol 100 (11) ◽  
pp. 5059-5067 ◽  
Author(s):  
Wei Shi ◽  
Caiyun Li ◽  
Man Li ◽  
Xicui Zong ◽  
Dongju Han ◽  
...  

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