Synthesis and biological evaluation of novel 4-(6-substituted quinolin-4-yl)-N-aryl thiazol-2-amine derivatives as potential antimicrobial agents |
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| Authors: | Prashant Thakare Abhijit Shinde Sagar Dakhane Abhijit Chavan Vivek D Bobade Pravin C Mhaske |
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| Institution: | 1. Department of Chemistry, S. P. Mandali's Sir Parashurambhau College (Affiliated to Savitribai Phule Pune University), Pune, India;2. Department of Chemistry, Abasaheb Garware College (Affiliated to Savitribai Phule Pune University), Pune, India;3. Department of Chemistry, H. P. T. Arts and R. Y. K. Science College (Affiliated to Savitribai Phule Pune University), Nashik, India |
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| Abstract: | 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. |
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