Synthesis and Biological Screening of Benzothiazole Derivatives with Pyrazole Moiety

Main Article Content

Gollapalli Raju
Tallapaneni Prasanna
Medipalli Surekha
Rama Nadendla

Abstract

Benzothiazole is one of the most important heterocyclic compound, weak base, having varied biological activities and still of great scientific interest now a days. They are widely found in bioorganic and medicinal chemistry with application in drug discovery. In the present study some novel benzothiazole derivatives were synthesized according to the scheme. All the synthesized benzothiazole derivatives have been characterized by using elemental analysis, FT-IR, 1HNMR, 13C NMR spectroscopy and further supported by mass spectroscopy. Purity of all the compounds has been checked on thin layer chromatographic plate and HPLC technique. All the synthesized compounds were tested for their antibacterial and antifungal activity (MIC) in vitro by broth dilution method with two Gram-positive bacteria, two Gram-negative bacteria and two fungal strains. The biological activities of the synthesized compounds have been compared with standard drugs Ciprofloxacin and Flucanazole. Analgesic activities were tested by Tail-flick method and Writhing method. The anti-pyretic activity was evaluated using Brewer's yeast induced pyrexia in rats. The compounds exhibited significant and moderate antibacterial, antifungal, analgesic and anti-pyretic activities. These compounds can be further exploited to get the potent lead compounds. The detailed synthesis and the antimicrobial screening of the new compounds are reported.

Downloads

Download data is not yet available.

Metrics

Metrics Loading ...

Article Details

Section
Journal of Basic And Applied Research

References

Achaiah, Garlapati et al; Synthesis and anti-inflammatory activity of novel pyrimidino benzothiazole amine derivatives; Pharmacophore, 2014, Vol. 5 (2), 331-342.

Balaji.P.N et al, Anthelmintic and Anti-microbial activities of synthesized heterocyclic pyrazole and its derivatives from fluoro substituted hydrazino benzothiazole; Int.J. PharmTech Res.2014,6(7),pp 1970-1975

Delmas F, Synthesis and antileishmanial activity of (1,3-benzothiazol-2-yl) amino-9-(10H)-acridinone derivatives; Synthesis and antileishmanial activity of (1,3-benzothiazol-2-yl) amino-9-(10H)-acridinone derivatives; Eur J Med Chem. 2004 Aug;39(8):685-90.

Geronikaki A; Evaluation of the local anaesthetic activity of 3-aminobenzo[d]isothiazole derivatives using the rat sciatic nerve model; Eur J Med Chem; 2009 Feb;44(2):473-81

Gollapalli Naga Raju et al; Benzothiazole - Versatile heterocyclic nucleus in medicinal chemistry: A review; IJPC (2015) 05 (04).

Gollapalli Naga Raju et al; Benzothiazole: Unique and versatile scaffold in the field of cancer; J. Chem. Pharm. Res., 2015, 7(4):286-293

Govinda et al; Synthesis, characterization and analgesic activity of some novel substituted 2-amino benzothiazole derivatives; WJPR; Vol 4, Issue 05, 2015.

Hasain. A; Synthesis and in vivo diuretic activity of some new benzothiazole sulfonamides containing quinoxaline ring system; J Enzyme Inhib Med Chem; 2016 Jan 7:1-8.

Herrera Cano N; New synthesis and biological evaluation of benzothiazole derivates as antifungal agents; J Agric Food Chem; 2015 Apr 15;63(14):3681-6.

Nadeem Siddiqui et al, Design, Synthesis and Anticonvulsant Screening of Newer Benzothiazole-Semicarbazones; Asian Journal of Biomedical and Pharmaceutical Sciences, 2(10) 2012,8-17

Nagaraju G, Sai KB, Chandana K, Gudipati M, Suresh P, Ramarao N. Synthesis, evaluation of antioxidant and antimicrobial study of 2-substituted benzothiazole derivatives. IAJPR. 2015; 5(3): 1288-1296.

Telvekar VN et al; Novel 2-(2-(4-aryloxybenzylidene) hydrazinyl)benzothiazole derivatives as anti-tubercular agents; Bioorg Med Chem Lett. 2012 Jan 1;22(1):649-52.

Vikas S. Padalkar et al; Synthesis and antimicrobial activity of novel 2-substituted benzimidazole, benzoxazole and benzothiazole derivatives; Arabial Journal of Chemistry, 2011.

Yin GL et al, Synthesis and biological evaluation of 2-(3-butynoicamidophenyl) benzothiazole derivatives as antitumor agents; Yao Xue Xue Bao; 2014 Jun;49(6):888-95.