Current Issue : July - September Volume : 2016 Issue Number : 3 Articles : 6 Articles
A series of cinchophen analogues of 2-(naphtha [2, 1-] furan-2-yl) quinoline-4-carboxylic acid 5(a-d) were synthesized by Pfitzinger method and further carboxylates of the corresponding acid 5(a-b) were synthesized by using different alcohols. The structure of synthesized compounds was confirmed by IR, 1H NMR, 13C NMR and mass spectral analysis and were screened for antitubercular activity on Mycobacterium tuberculi (Mtb) H37Rv strain, by Microplate Alamar Blue Assay (MABA) and their antibacterial activity by agar well diffusion method. In-silico molecular docking study was carried out on Auto Dock Vina. The antitubercular activity revealed that compounds 5b, 5d, 6a and 8a exhibited very good activity against M. tuberculi. The antibacterial activity results revealed that compounds 5d were found to be effective against Bacillus subtilus, Paracoccus denitrificans, Staphylococcus aureu sand Paracoccus sp. whereas, the compounds, 5a, 5b, 5d and 6b showed good activity against Paracoccus sp. The in-silico molecular docking studies were carried out on Mycobacterium translation initiation complex subunit S1 with the molecules 5a, 5b, 5c, 5d, 6a, 6b and 8a to identify the best docked conformation against the ribosomal protein S1. The synthesized compounds were found to exhibit good degree of antitubercular and antibacterial activity, this might be because of easy penetration of analogs into the cell membrane....
Acridine is an important nucleus in heterocyclic compounds which posses a wide spectrum of pharmacological activities. In this present work novel acridine derivatives containing pyrazole moiety like 3,4,6,7-tetrahydro-3,3,6,6-tetramethyl- 9-(3-(aryl)-1-phenyl-1H-pyrazol-4-yl) acridine-1,8(2H,5H,9H,10H)-diones were synthesized from 5,5-dimethylcyclohexane-1,3- dione with 3-(aryl)-1-phenyl-1H-pyrazole-4-carbaldehyde and ammonium acetate by microwave irradiation method. All the synthesized compounds have been characterized by using elemental analysis, FT-IR, 1H NMR, 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 analgesic and anti-inflammatory activities. These compounds can be further exploited to get the potent lead compounds. The detailed synthesis and the analgesic and anti-inflammatory screening of the new compounds are reported....
Indole 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 indole carboxylate derivatives were synthesized under green synthesis by microwave irradiation method according to the scheme. Methyl 6-chloro-1H-indole-5-carboxylate was treated with CH3I in presence of CS2CO3. Then Methyl 6-chloro-1H-indole-5-carboxylate was treated with oxalyl chloride in dry DCM and different secondary amines to get methyl 6-chloro-3-[(N,N-dialkylamino)(oxo)acetyl]-1-methyl-1H-indole-5-carboxylate derivatives (IND-1 to IND-10). IND-1 and IND-7 derivatives has been characterized by using elemental analysis, FT-IR, 1HNMR, 13C NMR spectroscopy and further supported by mass spectroscopy. Remaining derivatives were characterized by using elemental analysis, FT-IR 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 evaluated for anticonvulsant activity by maximal electroshock method (MES) by using phenytoin as standard at a concentration of 30 mg/kg. The anticonvulsant effect of the newly synthesized compounds was assessed by absence or reduction of hind limb tonic extensor phase. Among the synthesized derivatives compounds IND-5 and IND-10 were found to be the most potent compounds in the series....
Indole, the bicyclic ring system consists of pyrrole ring fused with benzene ring. Although indole moiety is very small but is fascinated by scientists because of the diverse biological activities by not only indole but its various substituted derivatives as well. In the present study some novel indole carboxamide derivatives like 6-Chloro-3-[(N,N-diethylamino)(oxo)acetyl]-1-methyl-N-aryl-1H-indole-5-carboxamide derivatives (IC-1 to IC-10) were synthesized according to the scheme. From all the synthesized novel indole carboxamide derivatives, IC-1 and IC-2 has been characterized by using elemental analysis, FT-IR, 1HNMR, 13C NMR spectroscopy and further supported by mass spectroscopy remaining are characterized by using elemental analysis, FT-IR, 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 evaluated for in-vivo diuretic activity by collecting total excreted urine (0-5 hrs) of rat kept in metabolic cage. All the compounds exhibited moderate to significant diuretic activity....
In the present study, a series of 1,3-thiazine derivatives were synthesized using Fe(III)-montmorillonite (Fe(III)- mont) as catalyst. The structures of newly synthesized compounds were confirmed by FTIR, 1H NMR, 13C NMR and LCMS. These compounds were screened for antimicrobial activity and in-silico molecular docking study....
Novel series of 5-Chloro-3-(3-substituted)-1,3-benzoxazol-2(3H)-one and 5-Chloro-3-[3-(cyclic amine)propyl]-1,3- benzoxazol-2(3H)-one derivatives were synthesized from 5-chloro-2(3H)-benzoxazolone with alkyl halides and 5-chloro-3-(3- substituted)-1,3-benzoxazol-2(3H)-one with 3-Cyclic amine substituted propyl chlorides. All the synthesized compounds have been characterized by using elemental analysis, FT-IR, 1H NMR, 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 streptomycin and amphotericin-B. The compounds exhibited significant antibacterial and moderate antifungal 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....
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