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Synthesis and Biological Evaluation of some novel chrome-2-one derivatives for antipsychotic activity
... Benzothiazole are an important class of bioactive and industrially important organic compounds. From the recent literature, these derivatives are also known to possess anti-tubercular, [3] local anesthetic, [4] antidiabetic, [5] antiulcer, [6] antipsychotic, [7] anti-tumor, [8] anti-oxidant, [9] analgesic, [10] schistosomicidal, [11] antileishmanial, [12] anti-convulsant, [13] anti-parasitic, [14] diuretic, [15] plant growth regulator [16] activities, anthelmintic, [17] Acaricidal. [18] Quinoline or 1-aza-naphthalene is one of the most important N-based heterocyclic aromatic compounds. ...
As part of ongoing studies in developing new antibacterial agent, a novel series of N-(benzo[d]thiazol-2-yl)-2-(2-(6-chloroquinolin-4-yl)hydrazinyl)acetamide derivatives was synthesized by sequencing reaction of 2-aminobenzothiazole with chloroacetylchloride, hydrazine hydrate and 4,7-dichloroquinoline. The novel heterocycles were characterized by elemental analyses and various spectroscopic techniques. The synthesized compounds were tested in-vitro antibacterial activity against two Gram-positive and two Gram-negative bacteria with standard drugs. Microbiological results showed that the synthesized compounds possessed a broad spectrum of antibacterial activity against the tested microorganisms.
... In recent years heterocyclic compounds analogues and derivatives have attracted strong interest due to their biological and pharmacological properties. Benzothiazole derivatives possess a wide spectrum of biological applications such as antitumor [17] , antimicrobial [18] ,schictosomicidal [19] , anti-inflammatory [20] , anticonvulsants [21] , antidiabetic [22] , antipsychotic and diuretic etc [23] . It is one of the most widely used anticancer agents, with indications and established protocols in a range of childhood and adult cancers. ...
The aim of the present work is to synthesize four new antimony compounds containing Methotrexate (MTX) and Benzothiazole (BZT) as ligands, in the mole ratio 1:1 and 1:2 .Antimony complexes were characterized by FTIR, UV, CHNS analysis, Atomic Absorption and conductivity measurements. The biological activity of MTX, BZT, SbCl 3 and the new compounds was evaluated against Leishmania parasite. All compounds were effective, while compound (4) was the best in inhibition.
... Gull and coworkers reported synthesis of 6-tolylbenzo-[d]thiazole-2-amine (77) obtained by Suzuki cross coupling reactions between 2-bromobenzothiazole and aryl boronic acids and these compounds exhibited potent and selective antiurease activity showing effective inhibitory action against plant urease [105]. Novel chromene derivatives, N-(6-substituted benzothiazol-2-yl)-(4-methyl-2-oxochromene-7-yloxy) acetamide (78) were synthesized by conventional method and have shown antipsychotic activity with muscle relaxant property [106]. Synthesis of 3-alkoxycarbonylmethyl-6nitro-2-benzothiazolones (79) were described by Loos et al. and the plant growth regulating activity of synthesized compounds has been evaluated on wheat (Triticum aestivum L) by measuring the primary roots [107]. ...
Background: Heterocycles are the gold mines in medicinal chemistry. Most drugs used in today's medicinal period possess a heterocyclic nucleus. One of the interesting heterocycles, benzothiazole, a potent phamacophore, is highly important in the medicinal chemistry due to its association with diverse pharmacological properties. Development in biological evaluation of heterocyclic molecule has undergone manifold changes and the advancement in molecular biology has eased the design of new molecule based on their mechanism of action. Methods: A structured search of bibliographic databases for peer-reviewed research literature has been done using different database. The quality of retrieved papers was appraised using standard tools. The details of important papers were described to focus on the potency of derivatives of benzothiazole. Results: One hundred fourteen papers were included in the review indicating importance of benzothiazole derivatives. The review has been focussed on papers highlighting anticancer and antimicrobial activities. Several papers have been searched for anticonvulsant, anti-inflammatory, antitubercular and other miscellaneous activities. Conclusion: The findings of this review confirm the importance of a conceptual framework for widespread use of heterocyclic compounds containing nitrogen, sulfur and oxygen compounds. It is basically focused on the medicinal applications of benzothiazole derivatives in the recent years that are currently attributed to exploitation of drug design and discovery of biologically active compounds across a wide range of therapeutic areas on a reasonable time scale.
... Benzothiazole is a unique example of a heterocyclic compound with a thiazole ring fused to a benzene ring and has received a lot of interest due to its diversified molecular design and remarkable optical, liquid, and electronic properties [8]. The compound and its derivatives have been reported to possess a wide spectrum of biological applications such as antitumor [9,10], antimicrobial [11,12], schictosomicidal [13], anti-inflammatory [14,15], anticonvulsant [16,17], antidiabetic [18], antipsychotic [19,20], and diuretic [8,21]. Interestingly, the nature of the substituent on the benzothiazole moiety plays an important role in the overall biological properties of the compound. ...
Two Schiff bases, HL1 and HL2, were synthesized in two different reactions involving 2-hydroxynaphthaldehyde with 2-amino-6-methylbenzothiazole and 2-amino-6-florobenzothiazole respectively. Copper(II) and nickel(II) complexes of the Schiff bases were subsequently prepared in 1:1 metal-to-ligand stoichiometric reactions. The compounds were characterized extensively by ¹H NMR, ¹³C NMR, Dept-90, UV–Vis, and IR spectroscopic techniques, magnetic susceptibility, TGA, DTG, and molar conductivity analysis. The spectroscopic results confirm bidentate nature of the Schiff bases and a four coordinate geometry for all the complexes: [CuL1ClH2O], [NiL1ClH2O], [Cu(L2)2], and [NiL2ClH2O]. Quantum chemical studies gave fully optimized geometries of the Schiff bases and metal complexes using the 6-31+g(d,p) basis set. The compounds were studied for their in vitro antibacterial activities against some selected Gram-positive and Gram-negative bacteria, using agar well diffusion. The metal complexes exhibited better antibacterial activities compared to the free ligand due to the effects of chelation, which improved the lipophilicity. Furthermore, the antioxidant potentials of the compounds were ascertained using DPPH radical scavenging and ferrous chelating assay. The copper complexes had the best antioxidant properties of all the tested compounds. The results of the biological analysis were in agreement with the theoretical data from quantum chemical calculations. The study presented biologically active coordination compounds with benzothiazole moiety that could be used as compounds of interest in the drug discovery processes.
... Benzothiazole is a unique example of a heterocyclic compound with a thiazole ring fused to a benzene ring and has received a lot of interest due to its diversified molecular design and remarkable optical, liquid, and electronic properties [8]. The compound and its derivatives have been reported to possess a wide spectrum of biological applications such as antitumor [9,10], antimicrobial [11,12], schictosomicidal [13], anti-inflammatory [14,15], anticonvulsant [16,17], antidiabetic [18], antipsychotic [19,20], and diuretic [8,21]. Interestingly, the nature of the substituent on the benzothiazole moiety plays an important role in the overall biological properties of the compound. ...
Two Schiff bases, HL1 and HL2, were synthesized in two different
reactions involving 2-hydroxynaphthaldehyde with 2-amino-6-methylbenzothiazole
and 2-amino-6-florobenzothiazole respectively. Copper(II) and nickel(II) complexes
of the Schiff bases were subsequently prepared in 1:1 metal-to-ligand stoichiometric
reactions. The compounds were characterized extensively by 1
H NMR, 13C NMR,
Dept-90, UV–Vis, and IR spectroscopic techniques, magnetic susceptibility, TGA,
DTG, and molar conductivity analysis. The spectroscopic results confirm bidentate
nature of the Schiff bases and a four coordinate geometry for all the complexes:
[CuL1ClH2O], [NiL1ClH2O], [Cu(L2)2], and [NiL2ClH2O]. Quantum chemical
studies gave fully optimized geometries of the Schiff bases and metal complexes
using the 6-31?g(d,p) basis set. The compounds were studied for their in vitro
antibacterial activities against some selected Gram-positive and Gram-negative
bacteria, using agar well diffusion. The metal complexes exhibited better antibacterial activities compared to the free ligand due to the effects of chelation,
which improved the lipophilicity. Furthermore, the antioxidant potentials of the
compounds were ascertained using DPPH radical scavenging and ferrous chelating
assay. The copper complexes had the best antioxidant properties of all the tested
compounds. The results of the biological analysis were in agreement with the
theoretical data from quantum chemical calculations. The study presented biologically
active coordination compounds with benzothiazole moiety that could be used
as compounds of interest in the drug discovery processes.
... The benzothiazole ring system in numerous biologically active molecules has been recognized, which shows important pharmacological activities. Various benzothiazole bearing compounds possess activities such as antitumor (Shi et al., 1996), antimicrobial (Catalano et al., 2013), schistosomicidal (Mahran et al., 2007), anti-inflammatory (Gupta and Rawat, 2010), anticonvulsants (Siddiqui et al., 2007), antidiabetic (Navarrete-Vazquez et al., 2009), antipsychotic (Arora et al., 2010), neuroprotective (Anzini et al., 2010) and diuretic (Yar and Ansari, 2009). 2-(4-Aminophenyl) benzothiazole moiety is present in various bioactive molecules such as antitumor I, II (Singh and Singh, 2014), orexin receptor antagonist III (Bergman et al., 2006) and the Gram-positive selective antibacterial IV (Ali et al., 2001) (Fig. 1). ...
A novel series of substituted benzothiazoles, bearing semicarbazone and thiosemicarbazone moieties, was designed, synthesized and evaluated for their antimicrobial activity and possible mode of action. Structures of the synthesized compounds were elucidated by H-1 NMR, C-13 NMR, IR and Mass spectral data. The results revealed that compounds SC06, SC09, TS05 and TS07 have potent antibacterial activity against both Gram-positive and Gram-negative strains. Compound TS05 displayed most potent activity with MIC values of 3.91, 7.81 and 1.56 A mu g/ml against S. aureus, E. coli and P. aeruginosa, respectively. The results from cytoplasmic membrane permeabilization assay, FACS study as well as DNA-binding assays, evaluated against clinically relevant pathogens S. aureus and E. coli, suggest membrane perturbing as well as intracellular mode of action of this class of compounds. In addition, hemolytic activity of the compounds was measured which indicated their low cytotoxicity.
... Benzothiazole are an important class of bioactive and industrially important organic compounds. From the recent literature, these derivatives are also known to possess anti-tubercular, [3] local anesthetic, [4] antidiabetic, [5] antiulcer, [6] antipsychotic, [7] anti-tumor, [8] anti-oxidant, [9] analgesic, [10] schistosomicidal, [11] antileishmanial, [12] anti-convulsant, [13] anti-parasitic, [14] diuretic, [15] plant growth regulator [16] activities, anthelmintic, [17] Acaricidal. [18] Quinoline or 1-aza-naphthalene is one of the most important N-based heterocyclic aromatic compounds. ...
As part of ongoing studies in developing new antibacterial agent, a novel series of N-(benzo[d]thiazol-2-yl)-2-(2-(6-chloroquinolin-4-yl)hydrazinyl)acetamide derivatives was synthesized by sequencing reaction of 2-aminobenzothiazole with chloroacetylchloride, hydrazine hydrate and 4,7-dichloroquinoline. The novel heterocycles were characterized by elemental analyses and various spectroscopic techniques. The synthesized compounds were tested in-vitro antibacterial activity against two Gram-positive and two Gram-negative bacteria with standard drugs. Microbiological results showed that the synthesized compounds possessed a broad spectrum of antibacterial activity against the tested microorganisms.
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