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Synthesis and in Vitro Anti-Bacterial Activity of 2-(5-Nitro-2-Heteroaryl)-1,3,4-Thiadiazole Derivatives Publisher



Yazdanian M1 ; Zihayat B2 ; Moshafi MH3 ; Khodadadi A1 ; Peimani A1 ; Shamsaddini A1 ; Nourhashemi M4 ; Foroumadi A4, 5
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran
  2. 2. Student Research Committee, Kerman University of Medical Sciences, Kerman, Iran
  3. 3. Department of Pharmaceutics, Pharmaceutics Research Centre, Kerman University of Medical Sciences, Kerman, Iran
  4. 4. Drug Design and Development Research Center, Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran
  5. 5. Department of Medicinal Chemistry, Faculty of Pharmacy and Neuroscience Research Center, Kerman University of Medical Sciences, Kerman, Iran

Source: Journal of Sciences# Islamic Republic of Iran Published:2020


Abstract

A new series of 2-(5-nitro-2-heteroaryl)-1,3,4-thiadiazole derivatives, including nitro furan, nitro thiophene and nitro imidazole, were synthesized and screened in vitro for their inhibitory activity against eight bacterial strains. The results showed that most of the synthesized compounds were active against Gram-positive bacteria, determined by MIC method. Among them, compounds 6a, 6b and 6d exhibited strong anti-bacterial effects against the Gram-positive bacteria. The oxidation of synthesized compounds to sulfinyl and sulfonyl bearing analogues did not improve the activity. © 2020 National Research Center of Medical Sciences. All rights reserved.
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