Design, synthesis and biological evaluation of new substituted 5-benzylideno-2-adamantylthiazol[3,2- b][1,2,4]triazol-6(5H)ones. Pharmacophore models for antifungal activity
2018
Аутори:
Tratrat, ChristopheHaroun, Michelyne
Paparisva, Aliki
Geronikaki, Athina
Camoutsis, Charalabos
Ćirić, Ana
Glamočlija, Jasmina
Soković, Marina
Fotakis, Charalmpos
Zoumpoulakis, Panagiotis
Bhunia, Shome
Saxena, Anil
Тип документа:
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт:
As a part of our ongoing studies in developing new derivatives as antimicrobial agents we
describe the synthesis of novel substituted 5-benzylideno-2-adamantylthiazol[3,2-b][1,2,4]triazol-6
(5H)ones.The twenty-five newly synthesized compounds were tested for their antimicrobial and
antifungal activity. All compounds have shown antibacterial properties with compounds 1–9 showing
the lowest activity, followed by compounds 10–14 while compounds 15–25 the highest antibacterial
activity. Specific compounds appeared to be more active than ampicillin in most studied
strains and in some cases more active than streptomycin. Antifungal activity in most cases also
was better than that of reference drugs ketoconazole and bifonazole. Elucidating the relation of molecular properties to antimicrobial activity as well as generation of pharmacophore model for
antifungal activity of two fungal species Aspergillus fumigatus and Candida albicans were performed.
Кључне речи:
Adamantlythiazoles; Anti-inflammatory; Antibacterial; Antifungal; Pharmacophore; SARИзвор:
Arabian Journal of Chemistry, 2018, 11, 4, 573-590
DOI: 10.1016/j.arabjc.2016.06.007
ISSN: 1878-5352