Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry and Computational Chemistry

Abstract

Synthesis and anti-fungal screening of fluoro benzothiazolo imidazole derivatives

Author(s): Bhushankumar Sathe, Jaychandran E, Vijay Jagtap and Swati Deshmukh

Literature revealed that vast majority of benzothiazoles and imidazole compounds are known to possess pharmacologically proven therapeutic potentials. Though extensive research work is reported on benzothiazoles, very little is known so for about fluorobenzothiazole fused imidazolines with fluorine at 6th position.The reaction of 6- fluro-7-chloroaniline1 with potassium thiocynate (KSCN) in presence of bromine and glacial acetic acid and ammonia to get 2-amino 6- fluro-7-chloro(1,3) benzothiazoles2-5 (1) which was further treated with hydrazine hydrate in presence of ethylene glycol and sulphuric acid to yield 2-hydrazino-6- fluoro-7-chloro(1,3) benzothiazoles(2). It was reacted with prepared Oxazolone i.e.2-phenyl- 4-benzylidine-5-oxazolone (3) to yield 2[2’- Phenyllidinyl- 5’- oxo- imidazoline- 1yl- amino] -6 fluoro- 7- chloro(1,3) benzothiazole(4), which was treated with variety of aromatic anilines in presence of DMF to yield different derivatives (5a-5i). Purity of compounds was checked by TLC. Melting points were determined by open capillaries method and uncorrected. IR spectra (NaCl) are recorded on FTIR (Schimadzu-84005) spectrophotometer using nujol mull technique. 1HNMR spectra are recorded on a spectrophotometer (Bruker AMX) at 500MHz, using TMS as internal reference. Griseofulvin was used as standard reference anti-fungal drug. All the results related to above data are given as MIC values in Table No. II.


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