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Synthesis and biological evaluation of novel 4‐(6‐substituted quinolin‐4‐yl)‐ N ‐aryl thiazol‐2‐amine derivatives as potential antimicrobial agents
Author(s) -
Thakare Prashant,
Shinde Abhijit,
Dakhane Sagar,
Chavan Abhijit,
Bobade Vivek D.,
Mhaske Pravin C.
Publication year - 2021
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.4317
Subject(s) - aspergillus niger , chemistry , antimicrobial , bacillus subtilis , aryl , amine gas treating , proteus mirabilis , antibacterial activity , bromide , candida albicans , escherichia coli , bacteria , organic chemistry , microbiology and biotechnology , biochemistry , alkyl , biology , gene , genetics
Cyclocondensation reaction of 4‐(2‐bromoacetyl)quinolin‐1‐ium bromide ( 4a–d ) with substituted arylthiourea, ( 5a–g ) afforded 4‐(6‐substituted quinolin‐4‐yl)‐ N ‐aryl/pyridyl thiazol‐2‐amine ( 6a‐ab ). These newly synthesized derivatives were evaluated for in vitro antibacterial activity against Escherichia coli (NCIM 2574), Proteus mirabilis (NCIM 2388) (Gram‐negative strains), Bacillus subtilis (NCIM 2063), Staphylococcus albus (NCIM 2178) (Gram‐positive strains) and in vitro antifungal activity against Aspergillus niger (ATCC 504) and Candida albicans (NCIM 3100). Compounds 6a , 6b , 6d , 6f , 6k , and 6l showed moderate to good antibacterial activity against S. albus . Ten derivatives 6c , 6q , 6r , 6s , 6t , 6v , 6w , 6x , 6y , and 6aa , showed moderate to good activity against A. niger . N ‐[4‐(Quinolin‐4‐yl)‐1,3‐thiazol‐2‐yl]pyridin‐2‐amine presented comparable activity against A. niger with respect to standard drug Rouconazole.