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Multitarget‐directed therapeutics: (Urea/thiourea) 2 derivatives of diverse heterocyclic‐Lys conjugates
Author(s) -
Pavan Kumar H.,
Kumara H. K.,
Suhas R.,
Channe Gowda D.
Publication year - 2021
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.202000468
Subject(s) - thiourea , chemistry , piperidine , piperazine , substituent , docking (animal) , urea , combinatorial chemistry , antimicrobial , stereochemistry , isoxazole , pyrazole , conjugate , organic chemistry , medicine , nursing , mathematical analysis , mathematics
The synthesis of a new small library of molecules containing bis ‐urea/thiourea pendants in lysine conjugated to three different heterocycles is described. The heterocycles used in this study have benzisoxazole/piperazine/piperidine units. After a detailed antimicrobial, antioxidant, and anti‐inflammatory evaluation, it was found that the most active compounds are 10 , 11 , 14 , 15 , 18 , 19 and 10 , 11 , 19 and 8 , 9 , 12 , 13 , 16 , 17 , respectively. Further, it was observed that the presence of all three entities, that is, urea/thiourea, the substituent (OMe/F), as well as the heterocycle, is highly essential for exerting potent activity. Among the heterocycles, the presence of isoxazole seems to be highly beneficial for exerting good potency. In continuation, docking studies have revealed extraordinary binding efficiency for some of the active compounds. Given their potent biological results and docking score, some of the title compounds could be potential drug candidates for microbial‐related diseases and provide a basis for future research into the development of molecules possessing multitask ability.

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