scholarly journals Biological Activity of Halogen-Containing Derivatives of N-Substituted Quinone Imines

2020 ◽  
Vol 10 (6) ◽  
pp. 7070-7076

The different halogen-containing derivatives of N-substituted quinone imines have been synthesized by the halogenation and hydrohalogenation of the corresponding quinone imines. N,N'-(Cyclohexa-2-en-1,4-diylidene)-diarylsulfonamides are good insecticides. They cause 89–97% of the insects to die. Compared with quinone imine, compounds having 4-oxocyclohexa-2,5-en-1-ylidene structure show higher fungicidal activity. N-(3,5-Dichloro-4-oxocyclohexa-2,5-dien-1-ylidene)-4-methylbenzene-1-sulfonamide and 4-chloro-N-[2,3,5,5,6,6-hexachloro-4-oxocyclohexa-2-en-1-ylidene]benzene-1-sulfonamide inhibit the growth and development of Phytophthora infestans by 82 and 81%, respectively. N-[2,3,5,5,6,6-Hexachloro-4-oxocyclohexa-2-en-1-ylidene]-4-methylbenzene-1-sulfonamide has a high herbicidal activity. The compounds with the largest number of chlorine atoms have the highest insecticidal, fungicidal, and herbicidal activity.

2021 ◽  
Vol 258 ◽  
pp. 04017
Author(s):  
K Giyasov ◽  
G. S. Turaeva ◽  
H T Turaeva

The article presents the herbicidal, defoliating, fungicidal properties of the synthesized derivatives of benzoxazolinones and benzoxazolinethions. It was shown that 3-alkylbenzoxazolinones, 3-alkyl-6-halobenzoxazolinones and 2-alkylthiobenzoxazoles exhibit herbicidal action during the growing season of plants, and they also cause cotton leaves to drop up to 70%. It was found that 3-alkylbenzoxazolinones and 2-alkylthiobenzoxazoles exhibited fungicidal activity against the pathogen, Fugarium oxyporum and Verticillum dahlia. Among them, 2-methylthiobenzoxazole inhibited spores of the fungi Verticillum dahlia by 96.4% and benzoxazolyl-2-carbamic acid butyl ester by 65%. These compounds exhibit fungicidal action against the pathogens of powdery mildew on cucumbers - Erysiphe cichoraceorum and powdery mildew on wheat - Erysiphe graminis, approaching the control Karatan. Apparently, these compounds are chemicals of contact action.


2019 ◽  
Vol 16 (7) ◽  
pp. 653-688 ◽  
Author(s):  
Leena Kumari ◽  
Salahuddin ◽  
Avijit Mazumder ◽  
Daman Pandey ◽  
Mohammad Shahar Yar ◽  
...  

Heterocyclic compounds are well known for their different biological activity. The heterocyclic analogs are the building blocks for synthesis of the pharmaceutical active compounds in the organic chemistry. These derivatives show various type of biological activity like anticancer, antiinflammatory, anti-microbial, anti-convulsant, anti-malarial, anti-hypertensive, etc. From the last decade research showed that the quinoline analogs plays a vital role in the development of newer medicinal active compounds for treating various type of disease. Quinoline reported for their antiviral, anticancer, anti-microbial and anti-inflammatory activity. This review will summarize the various synthetic approaches for synthesis of quinoline derivatives and to check their biological activity. Derivatives of quinoline moiety plays very important role in the development of various types of newer drugs and it can be used as lead compounds for future investigation in the field of drug discovery process.


2013 ◽  
Vol 9 (7) ◽  
pp. 920-925 ◽  
Author(s):  
Yi Bi ◽  
Jinyi Xu ◽  
Fei Sun ◽  
Xiaoming Wu ◽  
Wencai Ye ◽  
...  

1988 ◽  
Vol 53 (11) ◽  
pp. 2574-2582 ◽  
Author(s):  
Hedvig Medzihradszky-Schweiger ◽  
Helga Süli-Vargha ◽  
József Bódi ◽  
Kálmán Medzihradszky

A number of N-nitroso-2-chloroethyl-carbamoyl (Q(NO)) derivatives of α-melanotropin fragments have been synthesized and their effect on the frog skin melanocytes studied. Peptides substituted in this way possess the biological activity of the parent compounds, indicating that they preserved their receptor recognizing ability. These compounds can therefore serve as affinity labels. Some of these derivatives, related to the C-terminal sequence of α-melanotropin show prolonged darkening reaction, which does not influence the subsequent reaction of melanocytes with α-melanotropin. The Q(NO)-derivative of a fragment derived from the classical active site of the hormone shows, however, inhibition of the effect of α-melanotropin. It can be concluded that the latter peptide acts through the melanotropin receptor, while others, related to the C-terminal sequence of the hormone through another mechanism.


2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Takashi Ishida ◽  
Haruna Yoshimura ◽  
Masatsugu Takekawa ◽  
Takumi Higaki ◽  
Takashi Ideue ◽  
...  

AbstractThe discovery and useful application of natural products can help improve human life. Chemicals that inhibit plant growth are broadly utilized as herbicides to control weeds. As various types of herbicides are required, the identification of compounds with novel modes of action is desirable. In the present study, we discovered a novelN-alkoxypyrrole compound, kumamonamide fromStreptomyces werraensisMK493-CF1 and established a total synthesis procedure. Resulted in the bioactivity assays, we found that kumamonamic acid, a synthetic intermediate of kumamonamide, is a potential plant growth inhibitor. Further, we developed various derivatives of kumamonamic acid, including a kumamonamic acid nonyloxy derivative (KAND), which displayed high herbicidal activity without adverse effects on HeLa cell growth. We also detected that kumamonamic acid derivatives disturb plant microtubules; and additionally, that KAND affected actin filaments and induced cell death. These multifaceted effects differ from those of known microtubule inhibitors, suggesting a novel mode of action of kumamonamic acid, which represents an important lead for the development of new herbicides.


MedChemComm ◽  
2018 ◽  
Vol 9 (11) ◽  
pp. 1905-1909 ◽  
Author(s):  
Faustine d'Orchymont ◽  
Jeannine Hess ◽  
Gordana Panic ◽  
Marta Jakubaszek ◽  
Lea Gemperle ◽  
...  

The design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the antimalarial mefloquine is described.


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