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Home > Eco-Friendly Synthesis of Thiazolidinone Derivatives and Their Biological Studies

Eco-Friendly Synthesis of Thiazolidinone Derivatives and Their Biological Studies

Thesis Info

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Author

Naeem, Muhammad

Program

PhD

Institute

University of the Punjab

City

Lahore

Province

Punjab

Country

Pakistan

Thesis Completing Year

2010

Thesis Completion Status

Completed

Subject

Social sciences

Language

English

Link

http://prr.hec.gov.pk/jspui/handle/123456789/1033

Added

2021-02-17 19:49:13

Modified

2024-03-24 20:25:49

ARI ID

1676724640416

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Microwave heating, ionic liquids and solid phase catalysts were employed and studied for the preparation of various 4-thiazolidinone derivatives and for “in vitro” antibacterial and antifungal activity. These techniques revealed several advantages over the conventional methods. In combination with microwave radiation, ionic liquids were used as phase transfer catalysts (PTC) and montmorillonite clays (K10 and KSF types) were used as solid phase catalysts. The catalytic efficiency of montmorillonite KSF was marginally inferior to that of montmorillonite K10. Compounds pertaining to main six different series were synthesized. In the first series; two methods Microwave procedure-I: Multi-Component Reaction in DMF and Microwave procedure-II: Solvent free, Multi- Component Reaction were used and it was found that first was better in yield ranging from 82.4% to 96.0% while yield in procedure-II ranging from 42.6% to 84.6%. The compound 4,6-dimethylpyrimidin-2-amine was treated with disubstituted aromatic aldehydes in dimethylformamide to form a Schiff base and Schiff base was further treated with sulfanyl acetic acid under microwave radiation to obtain the compounds (88-97). The compounds of first series were synthesized and elucidated as 2-(2,4-dimethylphenyl)-3-(4,6-dimethylpyrimidin-2-yl)-thiazolidin-4-one (88), 3- (4,6-dimethylpyrimidin-2-yl)-2-(2-hydroxy-4-methylphenyl)-thiazolidin-4-one (89), 2- (2,4-dihydroxyphenyl)-3-(4,6-dimethylpyrimidin-2-yl)-thiazolidin-4-one (90), 2-(2,4- dichlorophenyl)-3-(4,6-dimethylpyrimidin-2-yl)-thiazolidin-4-one 3-(4,6- (91), dimethylpyrimidin-2-yl)-2-(2-hydroxy-4-methoxyphenyl)-thiazolidin-4-one (92), 2-(4- chloro-2-methylphenyl)-3-(4,6-dimethylpyrimidin-2-yl)-thiazolidin-4-one (93), 3-(4,6- dimethylpyrimidin-2-yl)-2-(4-fluorophenyl)-thiazolidin-4-one (94), 3-(4,6- dimethylpyrimidin-2-yl)-2-(4-nitrophenyl)-thiazolidin-4-one (95), 2-(2,4- difluorophenyl)-3-(4,6-dimethylpyrimidin-2-yl)-thiazolidin-4-one (96) and 2-(3- (dimethylamino)phenyl)-3-(4,6-dimethylpyrimidin-2-yl)- thiazolidin-4-one (97). In the second series (98-107); two methods Microwave procedure-I: Multi- Component Reaction using Montmorillonite Clays (K-10 and KSF) and Microwave procedure-II: Solvent free, Multi-Component Reaction were employed. First procedure was found better in yield ranging from (yield 78.4% to 94.1% with K-10 and 68.3% to 88.1% with KSF) while yield in second procedure ranging from 14.3% xii to 76.4%. In this procedure Schiff base was treated with mercaptoacetic acid under microwave radiation followed by the condensation reaction of aniline and substituted benzaldehydes. The compounds 2-(3,5-dimethylphenyl)-3-phenyl-thiazolidin-4-one (98), 2-(3-hydroxy-5-methoxyphenyl)-3-phenyl-thiazolidin-4-one (99), 2-(3-chloro-5- methylphenyl)-3-phenyl-thiazolidin-4-one (100), 2-(3,5-dichlorophenyl)-3-phenyl- thiazolidin-4-one (101), 2-(3-nitrophenyl)-3-phenyl-thiazolidin-4-one (102), 2-(3- ethoxyphenyl)-3-phenyl-thiazolidin-4-one thiazolidin-4-one (105), (104), (103), 2-(3-methoxyphenyl)-3-phenyl- 2-[3-(dimethylamino)phenyl]-3-phenyl-thiazolidin-4-one 2-(3,5-difluorophenyl)-3-phenyl-thiazolidin-4-one (106) and 2-(3,5- dihydroxyphenyl)-3-phenyl-thiazolidin-4-one (107) were obtained. For the compounds (108-117), two methods Microwave procedure-I: Ionic Liquids (PEG, TBAB and TEBAC) and Microwave procedure-II: Solvent free, Multi- Component Reaction were used. The second procedure was found better in yield and environmentally than Ionic Liquids (PEG, TBAB and TEBAC). The yield ranged from 33.4%-48.8% with TBAB, 33.5%-52.2% with PEG and 20.4%-32.4% with TEBAC while in solvent free procedure-II 66.8% to 92.8%. The compounds 1,3- dipyridin-2-ylthiourea, chloroacetic acid and different aromatic aldehydes were used for the preparation of compounds (108-117) of third series named as 5-benzylidene- 3-(pyridin-2-yl)-2-(pyridin-2-ylimino)-thiazolidin-4-one (108), 5-(4- methoxybenzylidene)-3-(pyridin-2-yl)-2-(pyridin-2-ylimino)-thiazolidin-4-one (109), 5- (2-hydroxy-4-methoxybenzylidene)-3-(pyridin-2-yl)-2-(pyridin-2-ylimino)-thiazolidin-4- one (110), 5-[4-(dimethylamino)benzylidene]-3-(pyridin-2-yl)-2-(pyridin-2-ylimino)- thiazolidin-4-one (111), 5-(2,4-dichlorobenzylidene)-3-(pyridin-2-yl)-2-(pyridin-2- ylimino)-thiazolidin-4-one (112), 5-(4-nitrobenzylidene)-3-(pyridin-2-yl)-2-(pyridin-2- ylimino)-thiazolidin-4-one (113), 5-(4-ethoxybenzylidene)-3-(pyridin-2-yl)-2-(pyridin- 2-ylimino)-thiazolidin-4-one (114), 5-(2,4-difluorobenzylidene)-3-(pyridin-2-yl)-2- (pyridin-2-ylimino)-thiazolidin-4-one (115), 5-(4-ethylbenzylidene)-3-(pyridin-2-yl)-2- (pyridin-2-ylimino)-thiazolidin-4-one (116) and 5-(1,3-benzodioxol-5-ylmethylidene)- 3-(pyridin-2-yl)-2-(pyridin-2-ylimino)-thiazolidin-4-one (117). In the forth series; two methods Microwave procedure-I: Multi-Component Reaction using Montmorillonite Clays (KSF and K-10) and Microwave procedure-II: Solvent free, Multi-Component Reaction were used and it was found that first was better in yield ranging from 78.8% to 96.1% with K-10 and 70.8% to 84.2% with KSF xiii while yield in second ranging from 34.6% to 78.8%. In this series compounds (118- 127) were synthesized by adopting environmentally safe procedure. (4-substituted- phenyl)methylidene]aniline was treated with sulfanyl(thioxo)acetic acid in the presence of montmorillonite clays under microwave radiation for ten to twelve minutes. The compounds (118-127) (5-benzylidene-3-phenyl-2-thioxo-thiazolidin-4- one (118), 5-(4-methylbenzylidene)-3-phenyl-2-thioxo-thiazolidin-4-one (119), 5-(4- methoxybenzylidene)-3-phenyl-2-thioxo-thiazolidin-4-one 5-(3-hydroxy-4- (120), methoxybenzylidene)-3-phenyl-2-thioxo-thiazolidin-4-one (121), (dimethylamino)benzylidene]-3-phenyl-2-thioxo-thiazolidin-4-one nitrobenzylidene)-3-phenyl-2-thioxo-thiazolidin-4-one yl)benzylidene]-3-phenyl-2-thioxo-thiazolidin-4-one 5-(4- (124), 5-[2-(furan-2- (125), (126) 5-(4- 5-(2,4- (123), dichlorobenzylidene)-3-phenyl-2-thioxo-thiazolidin-4-one ethoxybenzylidene)-3-phenyl-2-thioxo-thiazolidin-4-one (122), 5-[4- and 5-(2,4- difluorobenzylidene)-3-phenyl-2-thioxo-thiazolidin-4-one) (127) were synthesized. The compounds (128-137) of fifth series were prepared by using environmentally benign procedure and reaction time was also dramatically reduced. In this series two methods Microwave procedure-I: Multi-Component Reaction using Montmorillonite Clays (KSF and K-10) and Microwave procedure-II: Solvent free, Multi-Component Reaction were employed and procedure-I was found better in yield ranging yields ranging from 78.8% to 94.4% with K-10 and 68.9-% to 88.6% with KSF while yield in procedure-II ranging from 34.4% to 65.3%. Sulfanylacetic acid was reacted with (2,5-disubstituted-phenyl)methylidene-4-methoxypyrimidin-2-amine followed by the condensation between 4-methoxypyrimidin-2-amine and various aldehydes. The compounds 2-(2,5-dimethylphenyl)-3-(4-methoxypyrimidin-2-yl)- thiazolidin-4-one (128), 2-(4-ethylphenyl)-3-(4-methoxypyrimidin-2-yl)-thiazolidin-4- one (129), 2-(4-methoxyphenyl)-3-(4-methoxypyrimidin-2-yl)-thiazolidin-4-one (130), 2-(2-hydroxy-5-methoxyphenyl)-3-(4-methoxypyrimidin-2-yl)-thiazolidin-4-one (131), 2-(4-ethoxyphenyl)-3-(4-methoxypyrimidin-2-yl)-thiazolidin-4-one (132), 2-[4- (dimethylamino)phenyl]-3-(4-methoxypyrimidin-2-yl)-thiazolidin-4-one (133), 2-(2,5- dichlorophenyl)-3-(4-methoxypyrimidin-2-yl)-thiazolidin-4-one difluorophenyl)-3-(4-methoxypyrimidin-2-yl)-thiazolidin-4-one (134), (135), 2-(2,5- 2-(2,5- dihydroxyphenyl)-3-(4-methoxypyrimidin-2-yl)-thiazolidin-4-one (136), 2-[3-(furan-2- yl)phenyl]-3-(4-methoxypyrimidin-2-yl)-thiazolidin-4-one (137) were thus achieved.

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استفہام بمعنی امر

استفہام بمعنی امر

بسااوقات استفہام امر کے معنوں میں استعمال ہوتا ہے ۔ ذیل کی آیت:

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"شیطان تو یہی چاہتا ہے کہ شراب اور جوئے کے ذریعے تمہارے درمیان دشمنی اور بغض کے بیج ڈال دے اور تمہیں اللہ کی یاد اور نماز سے روک دے ، اب بتاؤ کہ کیا تم ان چیزوں سے باز آ جاؤ گے"۔

اس آیت میں ’’فھل انتم منتھون ‘‘ در اصل ’’انتھوا عنھا‘‘ کے معنی میں مستعمل ہے ۔

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"اس کے بعد اگر یہ تمہاری بات قبول نہ کریں تو (اے لوگو) یقین کر لو کہ یہ وحی صرف اللہ کےحکم سے اتری ہےاور یہ کہ اللہ کے سوا کوئی عبادت کے لائق نہیں، تو کیا اب تم فرما بردار بنو گے"۔

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" قُلْ أَرَأَيْتُمْ إِنْ أَهْلَكَنِيَ اللَّهُ وَمَنْ مَعِيَ أَوْ رَحِمَنَا”[[4]]

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Islam is a holistic and comprehensive system of life because the Creator of universe has given the instructions that are eternal and are perfect guide for humanity in all ages and circumstances. Islamic teachings are consistent with the comprehensive nature. Those instructions that human being has given for all walks of life in that the elements of morality is distinct and dominant and prohibited every act that is harmful to others. This fact is quite clear that the moral aspect of Islam is so important to consider the ethics of Islam has taken into consideration and there is no command to be out of the realm of ethics and particularly matters of life which is part of religion and are important aspect of society. Islamic teachings are so clear that there is no example of it in any economic system the world. Today we have different economic systems in the world which essentially teach us that the purpose of human life is to make money and collect goods even if affects the lives of others. But in Islamic economic world it is emphasized that this world is not the original house and satisfactory zone of human being and his purpose is not to collect wealth but the worship of Almighty. Human being is gifted fair system of order in every aspect of which there is clearly ethics thus human is strictly prohibited to collect money through unfair means and in cruel manners. In this article we will discuss the ethical consideration of Islamic economical system. So it is quite clear that the guarantor of peace, love and harmony in the world is Islamic system.

Data Driven Modelling for Improved Water Management in Indus Basin

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