TY - JOUR
T1 - Synthesis and biological evaluation of newer 1,3,4-oxadiazoles incorporated with benzothiazepine and benzodiazepine moieties
AU - Navin, Patel
AU - Sarvil, Patel
AU - Amit, Purohit
AU - Divyesh, Patel
AU - Dhansukh, Rajani
AU - Moo-Puc, Rosa
AU - Rivera, Gildardo
N1 - Publisher Copyright:
© 2017 Walter de Gruyter GmbH, Berlin/Boston.
PY - 2017/3/1
Y1 - 2017/3/1
N2 - A series of thiazepines and diazepines having 1,3,4-oxadiazole moiety were synthesized, and they were analyzed for their in vitro antimicrobial activity against several bacteria (Staphylococcus aureus, Staphylococcus pyogenes, Escherichia coli, and Pseudomonas aeruginosa) and fungi (Candida albicans, Aspergillus Niger, and Aspergillus Clavatus) and protozoa (Entamoeba histolytica, Giardia lamblia, Trypanosoma cruzi and Leishmania mexicana). Few of the selected compounds were tested for their antitubercular activity. However, it was noticed that the potency of final analogs against each strain placed reliance on the type of substituent present on aryl ring of oxadiazole as well as presence of thiophene, pyridine, and furan at benzothiazepines and benzodiazepines. The biological screening identified that some of the compounds were found to possess good antimicrobial and antitubercular (62.5-100 μg/mL of MIC) activity.
AB - A series of thiazepines and diazepines having 1,3,4-oxadiazole moiety were synthesized, and they were analyzed for their in vitro antimicrobial activity against several bacteria (Staphylococcus aureus, Staphylococcus pyogenes, Escherichia coli, and Pseudomonas aeruginosa) and fungi (Candida albicans, Aspergillus Niger, and Aspergillus Clavatus) and protozoa (Entamoeba histolytica, Giardia lamblia, Trypanosoma cruzi and Leishmania mexicana). Few of the selected compounds were tested for their antitubercular activity. However, it was noticed that the potency of final analogs against each strain placed reliance on the type of substituent present on aryl ring of oxadiazole as well as presence of thiophene, pyridine, and furan at benzothiazepines and benzodiazepines. The biological screening identified that some of the compounds were found to possess good antimicrobial and antitubercular (62.5-100 μg/mL of MIC) activity.
KW - 1,3,4-Oxadiazole
KW - antimicrobial activity
KW - antituberculosis activity
KW - benzodiazepines
KW - benzothiazepines
UR - http://www.scopus.com/inward/record.url?scp=85016043006&partnerID=8YFLogxK
U2 - 10.1515/znc-2016-0129
DO - 10.1515/znc-2016-0129
M3 - Artículo
C2 - 28182579
SN - 0939-5075
VL - 72
SP - 133
EP - 146
JO - Zeitschrift fur Naturforschung - Section C Journal of Biosciences
JF - Zeitschrift fur Naturforschung - Section C Journal of Biosciences
IS - 3-4
ER -