Efficient and convenient synthesis of pyrido [2,1-b]benzothiazole, pyrimidopyrido[2,1-b]benzothiazole and benzothiazolo[3,2-a][1,8]naphthyridine derivatives

2015 ◽  
Vol 21 (4) ◽  
pp. 219-224 ◽  
Author(s):  
Hala M. Refat ◽  
Khaled S. Mohamed

AbstractNew 3-aryl-pyrido[2,1-b][1,3]benzothiazole derivatives 2a–e were synthesized in excellent yields via the reaction of benzothiazoleacetonitrile (1) with different aromatic aldehydes. The treatment of 2-(benzo[d]thiazol-2-yl)-3-(pyridin-4-yl)acrylonitrile (6) with malononitrile afforded 1-amino-3-(pyridin-4-yl)-3H-pyrido[2,1-b][1,3]benzothiazole-2,4-dicarbonitrile (7), which was allowed to react with a variety of reagents to provide pyrimido[5′,4′:5,6]pyrido[2,1-b][1,3]benzothiazole 8, 9 and [1,3]benzothiazolo[3,2-a][1,8]naphthyridine 10, 15 derivatives. All synthesized products were confirmed by elemental analysis, IR, 1H-NMR, 13C-NMR, and mass spectral data.

2008 ◽  
Vol 5 (s2) ◽  
pp. 1133-1143 ◽  
Author(s):  
Rajiv Dahiya ◽  
Anil Kumar

Present study describes the synthesis of a novel series of 3,5-diiodo-4-(5-nitro-1H-2-imidazolyl)benzoyl amino acids and di/tri/tetrapeptides using diisopropylcarbodiimide/dicyclohexylcarbodiimide (DIPC/DCC) as coupling agents andN-methylmorpholine/triethylamine (NMM/TEA) as bases. Structure elucidation of all the newly synthesized compounds was done by elemental analysis and IR,1H NMR,13C NMR and mass spectral data. Synthesized imidazolopeptides were screened for their anthelmintic activity and found to possess moderate to good bioactivity against earthwormsMegascoplex konkanensis, Pontoscotex corethruses and Eudrilus eugenieawhen compared to reference drugs - albendazole and mebendazole at dose level of 2 mg mL−1.


2007 ◽  
Vol 4 (3) ◽  
pp. 320-342 ◽  
Author(s):  
Vinod Mathew ◽  
J. Keshavayya ◽  
V. P. Vaidya

4-Amino-5-aryl/heteroaryl substituted-3-mercapto-1,2,4-triazoles 3(a-d) were prepared from the corresponding aromatic carboxylic acids through a multi-step sequence. Compounds 3(a-d) were made to react with various aromatic/hetero aromatic acids and hetero aromatic aldehydes to give 3,6-disubstituted-1,2,4-triazolo [3,4-b]-1,3,4-thiadizoles and 3,6-disubstituted-5,6-dihydro-1,2,4-triazolo [3,4-b]-1,3,4-thiadizoles respectively. Elemental analysis, IR,1H NMR and mass spectral data elucidated the structures of all newly synthesized compounds. Synthesized compounds are studied for their antibacterial, antifungal, anti-inflammatory and analgesic activities. Some of the tested compounds showed significant pharmacological activities.


Author(s):  
Haresh G. Kathrotiya ◽  
Yogesh T. Naliapara

A series of novel highly substituted pyrimidines bearing furanyl thiazole nucleous have been synthesized. In which reaction of guanidine nitrate with ketene dithioacetals 3c produced substituted pyrimidines 4d which further treated with various aromatic aldehydes to afford title compounds 5(a-t). The chemical structures of the synthesized compounds were elucidated by 1H NMR, 13C NMR, FT-IR, elemental analysis, and mass spectral data.


2009 ◽  
Vol 6 (3) ◽  
pp. 775-779 ◽  
Author(s):  
B. Rajeeva ◽  
N. Srinivasulu ◽  
S. M. Shantakumar

Some new 2-(5-substituted-1,3,4-oxadiazole-2-yl)-1,3- benzothiazole(3a-j)were synthesized by refluxing benzothiazolyl carboxyhydrazide with different aryl acids in phosphoryl chloride. Structures of the synthesized compounds were established on the basis of1H NMR and Mass spectral data. The anti microbial activity of the synthesized compounds was evaluated by disc diffusion method.


Author(s):  
J.V. Guna ◽  
V.N. Bhadani ◽  
H.D. Purohit ◽  
Dipak M. Purohit

2- Methoxy – 6 - {4' - [(4'''- Chlorophenyl) (phenyl) methyl amino] phenyl} - 4 - aryl nicotinonitrile (3a-3l) and 2-Amino-6-{4'-[(4'''-Chlorophenyl)(phenyl)methyl amino]phenyl}-4-aryl nicotinonitrile (4a-4l) have been synthesized. The products have been assayed for their antimicrobial activity against Gram +ve, Gram -ve bacteria and fungi. The structure of the products has been elucidated by IR, 1H-NMR, mass spectral data, elemental analysis and thin layer chromatography.


2006 ◽  
Vol 10 (07) ◽  
pp. 996-1002 ◽  
Author(s):  
Ayhan Nazli ◽  
Ergün Gonca ◽  
Ahmet Gül

Magnesium porphyrazinate substituted with eight (1-naphthyl) groups on the peripheral positions has been synthesized by cyclotetramerization of 3,4-(1-naphthyl)pyrroline-2,5-diimine, 4-(1-naphthyl)pyrroline-2,5-diimine in the presence of magnesium butanolate. Its demetalation by treatment with trifluoroacetic acid, resulted in a partially oxidized product, namely, octakis(1-naphthyl)-2-seco-porphyrazine-2,3-dione. Further reaction of this product with copper(II) acetate, zinc(II) acetate and cobalt(II) acetate led to the metallo derivatives, [octakis(1-naphthyl)-2-seco-2,3-dioxoporphyrazinato]M(II) ( M = Cu , Zn or Co ). These new compounds have been characterized by elemental analysis, together with FT-IR, 1 H NMR, UV-vis and mass spectral data.


2015 ◽  
Vol 19 (06) ◽  
pp. 753-768 ◽  
Author(s):  
Ahmed A. Fadda ◽  
Rasha E. El-Mekawy ◽  
Ahmed I. El-Shafei

This manuscript describes the synthesis of a new series of porphyrin structures 4a–4m, 7, 9, 12 and 14. These structures were investigated against two types of viruses such as HIV-1 and HSV-1. Also they were screened for their antitumor activity. Among all tested compounds, it was found that compound 4b showed a high activity against HIV-1 and HSV-1 and against four different tumor cell lines. Most of the tested compounds showed a moderate degree of a potent antimicrobial activity. The structure of these compounds was confirmed on the basis of their analytical and spectral data such as UV-vis, IR, 13 C NMR, 1 H NMR spectroscopy and mass spectral data.


2008 ◽  
Vol 12 (02) ◽  
pp. 116-122 ◽  
Author(s):  
Ergün Gonca ◽  
Ümmü Gülsüm Baklaci ◽  
Hatice Akin Dinçer

Magnesium porphyrazinates substituted with eight (p-tolyl) and (o-tolyl) units on the peripheral positions have been synthesized for the first time by cyclotetramerization of 1,2-bis(p-tolyl)maleonitrile and 1,2-bis(o-tolyl)maleonitrile in the presence of magnesium butanolate. Their demetalation by the treatment with trifluoroacetic acid resulted in partially oxidized products, namely, octakis(p-tolyl)-2-seco-porphyrazine-2,3-dione and octakis(o-tolyl)-2-seco-porphyrazine-2,3-dione. Further reactions of these products with copper(II) acetate, zinc(II) acetate and cobalt(II) acetate have led to the metallo derivatives, [octakis(p-tolyl)-2-seco-2,3-dioxoporphyrazinato] M(II) and [octakis(o-tolyl)-2-seco-2,3-dioxoporphyrazinato] M(II) ( M = Cu , Zn , Co ). These novel compounds have been characterized by elemental analysis, together with FT-IR, 1H NMR, UV-vis and mass spectral data.


1986 ◽  
Vol 51 (12) ◽  
pp. 2810-2816 ◽  
Author(s):  
Jozef Gonda ◽  
Pavol Kristian

2-Bromomethylphenyl isothiocyanate reacts with pyridine to yield 2-isothiocyanatobenzylpyridinium bromide, which afforded N-aryl-N'-(2-benzylpyridinium)thiourea bromides. Deprotonization of the latter with aqueous NaOH gave N-aryl-N'-(2-benzylpyridinium) thioureates; these freed pyridine upon heating to give 2-arylamino-4H-benzo[d][1,3]thiazines. Structure of these compounds was evidenced by IR, 1H, 13C NMR and mass spectral data and backed by elemental analysis.


INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (11) ◽  
pp. 40-44
Author(s):  
.Aishwarya T.C ◽  
◽  
James Jainey ◽  
Vijay Kumar M. ◽  
B.C. Revanasiddappa

2 Oxo-2h-chromene-3-carbohydrazide (1) reacts with various aromatic aldehydes to give corresponding 2-oxo-2h-chromene-3-carbohydrazide arylidene hydrazides (SB1-8). Oxidative cyclization of (SB1-8) with mercuric oxide and iodine in DMF medium furnishes the title compounds 3-(5-aryl-1,3,4-oxadiazol2-yl)-2h-chromen-2-ones (2a-h). All the synthesized compounds were assigned structures on the basis of IR, 1 H-NMR and Mass spectral data. Some of the selected compounds were evaluated for In vivo anticonvulsant activity by MES and PTZ models.


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