نتایج جستجو برای: 2 aminobenzimidazole
تعداد نتایج: 2525262 فیلتر نتایج به سال:
In the present study, a quantitative structure activity relationship (QSAR) has been carried out on a series of 2-methyl and 2-aminobenzimidazole derivatives to identify the lipophilicity requirements for their inhibitory activity against bacteria Sarcina lutea. The tested compounds displayed in vitro antibacterial activity and minimum inhibitory concentration (MIC) was determined for all compo...
The enzyme pteridine reductase 1 (PTR1) is a potential target for new compounds to treat human African trypanosomiasis. A virtual screening campaign for fragments inhibiting PTR1 was carried out. Two novel chemical series were identified containing aminobenzothiazole and aminobenzimidazole scaffolds, respectively. One of the hits (2-amino-6-chloro-benzimidazole) was subjected to crystal structu...
Continuum solvation methods are frequently used to increase the efficiency of computational methods to estimate free energies. In this paper, we have evaluated how well such methods estimate the nonpolar solvation free-energy change when a ligand binds to a protein. Three different continuum methods at various levels of approximation were considered, viz., the polarized continuum model (PCM), a...
BACKGROUND Benzimidazoquinazolinones and related quinazolines are classes of heterocycles that are of considerable interest because of the diverse range of their biological properties. Although numerous classes of quinazolines have been conventionally synthesized, their syntheses have been suffered due to the multiple steps that sometimes have described in their preparation and also their chemi...
The antibacterial activities of cobalt(II) complexes with two series of benzimidazoles were evaluated in vitro against three Gram-positive bacterial strains (Bacillus cereus, Staphylococcus aureus, and Sarcina lutea) and one Gram-negative isolate (Pseudomonas aeruginosa). The minimum inhibitory concentration was determined for all the complexes. The majority of the investtigated complexes displ...
The structure activity relationships of 1H-benzimidazole-8-carboxylic acids (9a-9f), 1H-benzimidazole-8carboxylates (8a-8f) are described. Characteristic compounds showed improved demanding activity over a previously recognized 2-aminobenzimidazole series. In the lead optimization process and structure–activity relationship (SAR) of separate inhibitors based on modification of the lead molecule...
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