Top PDF ONE-POT SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF 2-AMINO-5-ARYL-5H-THIAZOLO [4,3-b]-1,3,4-THIADIAZOLES

ONE-POT SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF 2-AMINO-5-ARYL-5H-THIAZOLO [4,3-b]-1,3,4-THIADIAZOLES

ONE-POT SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF 2-AMINO-5-ARYL-5H-THIAZOLO [4,3-b]-1,3,4-THIADIAZOLES

Chemistry The synthesis of the finished products from aromatic aldehydes, thiosemicarbazide, and thioglycolic acid involves three steps. We followed the Shukurov et al 16 procedure for one-pot synthesis of 2-amino-5-aryl-5 H- thiazolo[4,3-b]-1,3,4-thiadiazoles (5a-5j) (Scheme 1) from equimolar quantities of an aromatic aldehyde, thioglycolic acid, and thiosemicarbazide. The interaction between equimolar quantities of aromatic aldehydes and thioglycolic acid proceeds with heat liberation and probably results in semithioacetals of thioglycolic acid (1), which further react with thiosemicarbazide to give functionalized N,S-acetals (2). Thioureas 3 are obtained as a result of cyclodehydration of the latter in concentrated H 2 SO 4 medium; they transform into compounds 5a-5j through intermediates 4. The structure of compounds 5a-5j was confirmed by IR, 1 H NMR and Mass spectroscopy. The IR spectra of these compounds have no absorption band in the region of 1680-1630 cm - 1 , characteristic of the stretching vibrations of the
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 ONE-POT SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF 2-AMINO-5-ARYL-5H-THIAZOLO [4,3-b]-1,3,4-THIADIAZOLES

 ONE-POT SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF 2-AMINO-5-ARYL-5H-THIAZOLO [4,3-b]-1,3,4-THIADIAZOLES

Tuberculosis is a common and often deadly infectious disease caused by Mycobacterium tuberculosis in humans, and it is estimated that one-third of the world’s population is currently infected with TB bacillus and annually 2.0 million deaths were found 13 . The treatment of mycobacterial infections especially the tuberculosis, has become an important problem due to the emergence of monodrug and multidrug-resistant strains of M. tuberculosis 14 . In this context, there is a need for new drugs to fight against this disease. Recently, N-substituted-2-amino-5-aryl-5H-thiazolo[4,3-b]-1,3,4-thiadiazoles, active against pathogenic fungi of agricultural crops, have become substances, among other 1,3,4-thiadiazoles, that have drawn the attention of researchers 15-17 . The only known method giving rise to that heterocyclic system is based on cyclodehydration of (4-oxothiazolidine-3-yl)thioureas (in concentrated H 2 SO 4
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One- Pot synthesis and reactions of Novel 5-(4-fluoro-phenyl)-3-(8-hydroxyquinolin-5- yl)-7-phenyl-5H-thiazolo[3,2-a]pyrimidine-6- carbonitrile as antimicrobial agents

One- Pot synthesis and reactions of Novel 5-(4-fluoro-phenyl)-3-(8-hydroxyquinolin-5- yl)-7-phenyl-5H-thiazolo[3,2-a]pyrimidine-6- carbonitrile as antimicrobial agents

15. Pan, B.; Huang, R.; Zheng, L.; Chen, C.; Han, S.; Qu, D.; Zhu, M.; Wei, P. Thiazolidione derivatives as novel antibiofilm agents: Design, synthesis, bi- ological evaluation, and structure–activity rela- tionships. Eur. J. Med. Chem. 2011, 46, 819-824. 16. Abu-Hashem, A. A.; Youssef, M. M.; Hussein, H. A. R. Synthesis, Antioxidant, Antituomer Activi- ties of Some New Thiazolopyrimidines, Pyrrolo- thiazolopyrimidines and Triazolopyrrolothiazo- lopyrimidines Derivatives. J. Chin. Chem. Soc.

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Synthesis and antimicrobial activity of 2 {4' [(3" aryl) 2" propene 1" N (1,2,4  triazole) amino]} 6 [bis(2"' chloro ethyl) amino] 4 methoxy 1,3,5 triazine

Synthesis and antimicrobial activity of 2 {4' [(3" aryl) 2" propene 1" N (1,2,4 triazole) amino]} 6 [bis(2"' chloro ethyl) amino] 4 methoxy 1,3,5 triazine

Triazoles (5a-5k) were evaluated in vitro for antimicrobial activity against B. Mega, B. Subtillis, E. Coli, P. Fluoresences and for antifungal activity against A. awamori using DMF as solvent at 50 µg concentration by cup- plate method 7 . After 24 hrs. of incubation at 37 0 C temp., the zone or inhibition were measured in mm. The activity was compared with the known antibiotics viz. Ampicillin chloramphenicol, Norfloaxacin, Greseofulvin at same concentration which is represented in Table-I and comparable anti microbial activity represented in Table no. II
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Synthesis, Antimicrobial, Antioxidant and Molecular Docking Study of Some Novel Bis-1, 2, 4-Triazolo [3, 4-b]-1, 3, 4-Thiadiazoles

Synthesis, Antimicrobial, Antioxidant and Molecular Docking Study of Some Novel Bis-1, 2, 4-Triazolo [3, 4-b]-1, 3, 4-Thiadiazoles

A novel series of 1-aryl-3,4-bis-(3-alkyl/phenyl-[1,2,4] triazolo[3,4-b][1,3,4]thiadiazol)-1H-pyrazole (5a-i) are synthesized by the cyclocondensation of 1-(aryl)-1H-pyrazol-3,4-dicarboxylic acids with 3-alkyl/aryl-4-amino-5-mercapto-1,2,4-triazoles. Pyrazole dicarboxylic acids were prepared by the 1, 3-dipolar cyclo addition of 3-aryl sydnones with dimethylacetylenedicarboxylate (DMAD). The newly synthesized compounds were studied for their antibacterial, antifungal and antioxidant activities. Particularly compounds 5a and 5g showed considerable antibacterial activity against the standard drug, while all the tested compounds displayed poor inhibitory effect against fungi. Compound 5d exhibited good antioxidant activity. The docking study was performed with Acinetobacter baumannii penicillin- binding protein target using AutoDock 4.2, which proved H-bond interaction and strong binding affinity.
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Synthesis and antioxidant, antimicrobial activity o
f 6 cyano 5 imino 2 methyl 
7 (methylthio) 5H thiazolo [3, 2 
a
] pyrimidines

Synthesis and antioxidant, antimicrobial activity o f 6 cyano 5 imino 2 methyl 7 (methylthio) 5H thiazolo [3, 2 a ] pyrimidines

New heterocyclic compound 6-cyano-5-imino-2-methyl-7-(methylthio)-5H-thiazolo [3, 2-a] pyrimidines (3) reported by reacting of 2-amino-5-methyl thiazole (1) with bis(methylthio) methylene malanonitrile (2). Further the compound (3) was treated with aryl amines, substituted phenols, active methylene compounds and heteryl amines to obtain its 7-substituted derivatives. Newly synthesized thiazolo [3, 2-a] pyrimidines derivatives were screened for their antimicrobial and antioxidant activity.
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Synthesis of 5-arylidine-2-(3, 4, 5-trimethoxyphenyl)-3-(4-phenylthiazol-2-yl) Thiazolidin-4-one Derivatives as a Novel Class of Antimicrobial Agents

Synthesis of 5-arylidine-2-(3, 4, 5-trimethoxyphenyl)-3-(4-phenylthiazol-2-yl) Thiazolidin-4-one Derivatives as a Novel Class of Antimicrobial Agents

8. [a] Ber lin KD and Herd MD. Novel 2~Amino~4~Aryl~Substituted~ and 2~Amino~4,5~Disubstituted~Thiazoles. Proc Okla Acad Sci, 71: 29~33 and references there in (1991). [b] Agarwal N, Kumar S, Shrivastava AK and Sarkar PC. Synthesis and Biological Evaluation of some 2~amino~4~arylthiazoles and thiazolylamides. Indian Journal of Heterocyclic Chemistry, 6: 291~294 (1997). [c] Alessandro DL and Manuela S. In vitro activityof 2~cyclohexy-lidenhydrazo- 4~phenyl~thiazole compared with those of amphotericin B and fluconazole against clinical isolates of Candida spp and fluconazole~resistant Candida albicans. Journal of Antimicrobial Chemotherapy, 55(5): 692~698 (2005). [d] Pandeya SN, Sriram D, Nath G and DeClerq E. Synthesis, antibacterial, antifungal and anti~HIV activities of Schiff and mannich bases derived from isatin derivatives and N ~ [ 4 ~ ( 4 ’ c h l o r o p h e n y l ) t h i a z o l ~ 2~yl]thiosemicarbazide. European Journal of Pharmaceutical Sciences. 9: 25~31 ( 1999). [e] PattWC, Hamilton HW and Taylor MD. Structure~activity relationships of a series of 2~amino~4~thiazole~containing renin inhibitors. J Med Chem, 35: 2562–2572 (1992). [f] Dodson RM and Harr yWT. α ~Cyanoalkyl Sulfonates. I. The Reactions of α ~Cyanobenzyl Benzenesulfonate.JAmer 1. Verma A and Saraf SK. 4~thiazolidinone ~a
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SYNTHESIS AND BIOLOGICAL SCREENING OF 2 AMINO 6 ARYL  4 {[(3′ DIFLUOROMETHOXY) 5′ (3″ METHYL) 4″ (2‴,2‴,2‴  TRIFLUOROETHOXY)PYRIDIN 2″ YL]METHOXYPHENYL}  NICOTINONITRILES

SYNTHESIS AND BIOLOGICAL SCREENING OF 2 AMINO 6 ARYL 4 {[(3′ DIFLUOROMETHOXY) 5′ (3″ METHYL) 4″ (2‴,2‴,2‴ TRIFLUOROETHOXY)PYRIDIN 2″ YL]METHOXYPHENYL} NICOTINONITRILES

Cyanopyridine derivatives shows good biological and therapeutic activities, With a view of getting to synthesized 2-Amino-6-aryl-4- {[(3′-difluoromethoxy)-5′-(3′′-methyl)-4′′-(2′′′,2′′′,2′′′-trifluoroethoxy) pyridin-2′′-yl]methoxyphenyl}-nicotinonitriles (3a-3k) by the condensation of (E)-3-{[(3′-difluoromethoxy)-5′-(3″-methyl)-4″- (2‴,2‴,2‴-trifluoroethoxy) pyridine-2-yl] methoxy phenyl}-1-aryl-prop- 2-ene-1-ones with malononitrile in presence of ammonium acetate. All Synthesized compounds characterized by TLC, IR, 1 HNMR, Mass spectra and Physical constants. All the synthesized compounds screened for their antimicrobial activity against Gram +ve bacteria (B.mega, B.Subtillis) Gram -ve bacteria (E.coli, P.fluorescens) and fungi (A.awamori).
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Synthesis and Antimicrobial Activity of Some 2-[(4-Substituted-Phenyl-3-Chloro-Azetidin-2-One)-5-(2'-Methylamino-4-Phenyl-1', 3'-Thiazolyl-]-1, 3,4-Thiadiazoles

Synthesis and Antimicrobial Activity of Some 2-[(4-Substituted-Phenyl-3-Chloro-Azetidin-2-One)-5-(2'-Methylamino-4-Phenyl-1', 3'-Thiazolyl-]-1, 3,4-Thiadiazoles

All the synthesized compounds 4(a-n) and 5(a-n) have been screened in vitro for their antibacterial activity against B. subtilis (Bs), E. coli (Ec), S. aureus (Sa) and K. pneumoniae (Kp) at two concentrations (50 and 100 ppm) and antifungal activity against A. niger (An), A. flavus (Af), F. oxisporium (Fo) and T. viride (Tv) at two concentrations (50 and 100 ppm). Standard antibacterial Streptomycin and fungicide Griseofulvin were also screened under the similar conditions for comparison. The following compounds were found active against the tested becteria: 4d(Ec, Sa), 4f(Bs, Kp), 4g(Ec), 4h(Bs, Ec, Sa), 4i, 4j(Kp), 5b, 5c, 5d, 5e, 5f, 5g(Bs, Ec, Kp, Sa), 5i(Ec, Kp, Sa), 5h(Kp), 5k (Ec), 5n(Kp, Sa) and fungi: 5f(Af, Tv), 5g(An), 4n(Fo), 5b(Tv), 5c(Af, Fo), 5d(An), 5e, 5f, 5g(An, Af, Fo, Tv), 5i(Af, Fo), 5j(An, Af), 5h(Fo, Tv), 5k(An, Af), 5l, 3m, 5n(An). On the basis of structural activity relationship it has been observed that among the substituents present on the phenyl ring, halo derivatives were found to be highly active against in the series. Further study reveals that bromo derivatives are highly active.
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SYNTHESIS AND CHARACTERIZATION OF SOME NOVEL 2-[(5-ARYL)-4, 5-DIHYDRO-1H-PYRAZOLE-3-YL]-1H-BENZIMIDAZOLES WITH ANTIMICROBIAL ACTIVITY

SYNTHESIS AND CHARACTERIZATION OF SOME NOVEL 2-[(5-ARYL)-4, 5-DIHYDRO-1H-PYRAZOLE-3-YL]-1H-BENZIMIDAZOLES WITH ANTIMICROBIAL ACTIVITY

intermediate 4a-d was treated with the various aryl aldehydes in ethanol solvent in alkaline medium (60% KOH) at ambient temperature for 4-5 h to obtain the final intermediate 5a-h in good yields. Subsequently condensation followed by cyclization of compound 5a- h with guanidine in acetic acid under reflux for 4-5 h gave the title compounds 6a-h in good to excellent yields. The chemical structures of the newly prepared compounds were confirmed by their IR, 1 H NMR and

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One-pot Synthesis of Some Novel 2-[(Z)-1-(Aryl)]-6,7-dihydro-2H-istohiazolo[2,3-a]pyrimidine-3(5H)-one Derivatives

One-pot Synthesis of Some Novel 2-[(Z)-1-(Aryl)]-6,7-dihydro-2H-istohiazolo[2,3-a]pyrimidine-3(5H)-one Derivatives

assignments and integral of the peaks are consistent with the proposed structure of 3,4,5, 6-tetrahydro-2-pyrimidinethiol. Further reaction of 2 with ethyl chloroacetate and corresponding aromatic aldehyde in the presence of sodium acetate and acetic acid afforded 3(a-j), as shown in Scheme 1. The reaction was preceded under reflux condition for 5-7 h. The yield of products after recrystallization from

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Synthesis and antimicrobial activity of 2 [1 phenyl 3 arylpyrazol 4 yl]benzothiazolines

Synthesis and antimicrobial activity of 2 [1 phenyl 3 arylpyrazol 4 yl]benzothiazolines

A convenient and solventless synthesis of 2-[1-phenyl-3-arylpyrazol-4-yl]benzothiazolines is reported. The procedure does not involve the use of any additional reagent/catalyst, produces no waste, and represents a green synthetic protocol. The structures of newly synthesized compounds were confirmed by IR, 1 H NMR, 13 C NMR, mass and elemental analyses. All the seven compounds were evaluated for in vitro antibacterial activity against Gram-positive Bacillus subtilis, Staphylococcus aureus, Gram-negative Escherichia coli and in vitro antifungal activity against Candida albicans and Aspergillus niger.
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SYNTHESIS OF 3  (1 – BENZYL – 1H – BENZO [D] IMIDAZOL – 2 – L AMINO) – 2 – (3 – ARYL – 1  PHENYL – 1H – PYRAZOL – 4 – YL) THIAZOLIDIN – 4  ONES AND THEIR ANTIMICROBIAL ACTIVITIES

SYNTHESIS OF 3 (1 – BENZYL – 1H – BENZO [D] IMIDAZOL – 2 – L AMINO) – 2 – (3 – ARYL – 1 PHENYL – 1H – PYRAZOL – 4 – YL) THIAZOLIDIN – 4 ONES AND THEIR ANTIMICROBIAL ACTIVITIES

activities were performed by cup plate method. The sample was dissolved in DMF at the concentration of 1000 µg/ml. Antibacterial activity screened against P. aeruginosa, S. aureus and P. vulgaris. Antifungal activity was carried out against A. niger and A. flavus under aseptic conditions. Gentamycin and fluconazole were used as standard drug for antibacterial and antifungal activities respectively. The zone of inhibition was compared with standard drug after 24 hours of

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SYNTHESIS, CHARECTERIZATION AND ANTIMICROBIAL ACTIVITY OF 5 METHYL  2, 4 DIHYDRO 3H PYRAZOL 3 ONE 4 (4 SUBTITUTED) BENZYLPIPERAZINE DERIVATIVES

SYNTHESIS, CHARECTERIZATION AND ANTIMICROBIAL ACTIVITY OF 5 METHYL 2, 4 DIHYDRO 3H PYRAZOL 3 ONE 4 (4 SUBTITUTED) BENZYLPIPERAZINE DERIVATIVES

INTRODUCTION: Benzylpiperazines and its derivatives are versatile type of ligands have attracted considerable pharmaceutical interest due to their antibacterial 1, 2, 3 antifungal 4, 5, 6 antitumor and anthelmintic 7 activities. Benzylpiperazines have drawn great interests for their high potential biological activity especially for their antitumor activity when linked with thiosemicarbazides increases their antimicrobial and antitumor activity

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Synthesis and Antimicrobial Activity of 1 (4 aryl 2 thiazolyl)   and 1 (4 aryl 2 oxazolyl) 3,5 diaryl 2 pyrazoline derivatives

Synthesis and Antimicrobial Activity of 1 (4 aryl 2 thiazolyl) and 1 (4 aryl 2 oxazolyl) 3,5 diaryl 2 pyrazoline derivatives

The new compounds (6a-i) and (8a-f) were screened for their antibacterial activity by disk- diffusion technique [29,30] against two Gram – positive bacteria namely, Staphylococcus aureus and Pseudomonas acruginosa, two Gram-negative bacteria namely, Bacillis subtillis and Escherichia coli and four pathogenic fungi namely, Syncephalastrum racemosum, Aspergillus fumigatus, Candida albicans and Geotrichum candidum at three concentrations 5,2.5 and 1.25 µg/ml. Chloramphenicol was used as standard antibacterial agent and flucanazole was used as standard antifugal agent. The minimal inhibitory concentrations (MIC) of the compounds are listed in Table 3. MIC'S were recorded as the minimum concentration of a compound that inhibits the growth of tested microorganisms. All of the compounds tested have shown significant antibacterial and antifungal activity as compared with the reference drugs. The antibacterial assessment revealed that most of the tested compounds possess weak to moderate activity. The MIC values are generally within the range 3.9-250 µg/ml against all the tested strains.
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An efficient one pot synthesis of 2, 4, 6 triaryl pyridines and their in
vitro antimicrobial activity

An efficient one pot synthesis of 2, 4, 6 triaryl pyridines and their in vitro antimicrobial activity

Pyridine derivatives have occupied a unique position in medicinal chemistry. The naturally occurring B6-vitamins pyridoxine, pyridoxal, pyridoxamine and codecarboxylase contain a pyridine nucleus. Due to their Л-stacking ability, some pyridines are used in supramolecular chemistry. In addition, many pyridines are reported as antimalerial, anesthetic, anticonvulsant, antiepileptic, antioxidant, fungicidal, antibacterial, antiparasitic activities [1-4].

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Eco-friendly synthesis of 1-Aryl-8-methoxythiazolo [2’, 3’ : 3, 4] [1, 2, 4] triazino [5, 6-b] indoles under microwave ir-radiations

Eco-friendly synthesis of 1-Aryl-8-methoxythiazolo [2’, 3’ : 3, 4] [1, 2, 4] triazino [5, 6-b] indoles under microwave ir-radiations

Similar ly, 6-Methoxyisatin-3-(4-p- bromopheny1-2-thiazoly1) hydrazone hydrobromide (IIb; Ar = p-BrC 6 H 4 ) and 6- Methoxyisatin-3-(pheny1-2-thiazoly1) hydrazone hydrobromide (IIa; Ar = p-C1C 6 H 4 ) (IIc; Ar = C 6 H 5 ) were also irradiated in a mixture of POCl 3 under

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ANTIMICROBIAL ACTIVITY OF 6-ARYL-4-METHYL-2-OXO-1, 2, 3, 6-TETRAHYDROPYRIMIDINE-5-(N-ARYL) CARBOXAMIDES: A STRUCTURE-REACTIVITY STUDY

ANTIMICROBIAL ACTIVITY OF 6-ARYL-4-METHYL-2-OXO-1, 2, 3, 6-TETRAHYDROPYRIMIDINE-5-(N-ARYL) CARBOXAMIDES: A STRUCTURE-REACTIVITY STUDY

In this study, four bacteria and two fungi were used. The result of the present study showed a broad range of antimicrobial activity (Figure 1). Table 1 and 2 show that the antimicrobial activity depends upon substituent only. Compound ‘7’ exhibited excellent antimicrobial activity. The chlorine derivative is characterized by greater antimicrobial activity than that of the methyl and methoxy derivatives. According to Mohamed et al., 12 this may be attributed to the

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Synthesis and anti inflammatory activity of some [4, 6 (4 substituted aryl) 2  oxo 1, 2, 3, 4 tetrahydropyrimidin  5 yl] acetic acid derivatives

Synthesis and anti inflammatory activity of some [4, 6 (4 substituted aryl) 2 oxo 1, 2, 3, 4 tetrahydropyrimidin 5 yl] acetic acid derivatives

Synthesis of 4-(4-substituted phenyl)-4-oxo butanoic acid derivatives (IIa-IId) In RBF provided with a reflux condenser protected by calcium chloride guard tube, placed 0.5 mol of substituted benzene and 7.5 gm (0.75 mol) of I. Stirred the mixture & added 22 gm (0.165 mol) of powdered anhydrous AlCl 3 all at once. The reaction started immediately. HCl was evolved

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Synthesis of some new 2 amino 3 cyano 4 aryl 6 (1 napthyl amino) pyridines as antibacterial agents

Synthesis of some new 2 amino 3 cyano 4 aryl 6 (1 napthyl amino) pyridines as antibacterial agents

Variety of 2-amino-3-cyano-4-aryl-6-(1-napthyl amino)-pyridines 3(a-h) have been synthesized by reacting 1-(1-napthyl amino)-3-aryl-2-propen-1-ones 2(a-h) with malononitrile and ammonium acetate in methanol under reflux condition. Structures of the synthesized compounds were confirmed by the spectral analysis. Furthermore, all the synthesized products were screened for their antibacterial activity.

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