Design, Synthesis and Antimicrobial Activities of 1-(4-Oxo-3-(4-Fluorophenyl)-3h-Quinazolin- 2-Yl)-4-(Substituted) Thiosemicarbazide Derivatives

Alagarsamy,; Appani, Ramgopal; Sulthana, M. T.; Narendar, B.; Solomon, V. Raja

doi:10.4067/s0717-97072016000200002

Cited by 8 publications

(3 citation statements)

References 18 publications

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“…The recent role of these moieties in microbial infections has led to the development of new antimicrobial agents (Figure 1, III-VI) (Saripinar et al, 1996;Milczarska et al, 1999;Pandeya et al, 2005;Sriram et al, 2005;Karalı et al, 2007;Turan-Zitouni et al, 2008;Guzel et al, 2008;Sriram et al, 2009;Pavan et al, 2010). This research effort is a continuation of our aims on the way to develop potent antimicrobial & antitubercular agents using the benzopyrimidine scaffold by a pharmacophore hybrid approach (Figure 1) (Meunier, 2008;Alagarsamy et al, 2016). In this research, substituted thiosemicarbazide group was placed at 2 nd position & 4-methylphenyl group was placed at 3 rd position of benzopyrimidine nucleus.…”

Section: Introductionmentioning

confidence: 97%

Case report Human urinary tract myiasis in Al-Amara city/ Iraq

Khallawi¹,

Jazaa²

2018

Int. J. Res. Ph. Sci.

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Myiasis has been defined as infestation with larvae of Diptera,on live animals and human. There are three main families of Diptera cause Myiasis,Oestridae (bot and warble flies); Calliphoridae(blowflies) and Sarcophagidae (flesh fly). Larvae of Fannia scalaris is the most frequent cause of urinary myiasis. Clinically,Myiasis is classified as dermal,respiratory system,nasopharyngeal,ophthalmic,auricular,gastric,rectal,intestinal and finally urinary myiasis which is the most uncommon type in human,because cloth protection and inaccessibility of genital area to flies prevents them from laying eggs,Psychoda albipennis (P. albipennis) can flourish in the environment of a moist bathroom and may cause urogenital myiasis in humans. The urine specimen was taken from the patient who contracted from this larvae and the specimen was examined to detect and identify this larvae. The larvae are feeding on bacteria. The prevention criteria to prevent the myiasis are including the good hygiene during defection and micturition.

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Section: Introductionmentioning

confidence: 97%

Case report Human urinary tract myiasis in Al-Amara city/ Iraq

Khallawi¹,

Jazaa²

2018

Int. J. Res. Ph. Sci.

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“…1S and ▶Fig. 1 [16][17][18] and studied their anti-HIV, antitubercular and antibacterial activities against selected gram positive and negative bacteria.…”

Section: Introductionmentioning

confidence: 99%

Design and Synthesis of Novel 1-substituted-3-(3-(3-nitrophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-yl amino) Isothioureas for their Anti-HIV, Antibacterial Activities, Graph Theoretical Analysis, Insilico Modeling, Prediction of Toxicity and Metabolic Studies

2020

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In the present study, we have placed the substituted thiosemicarbazide moiety at the C-2 position and 3-nitrophenyl group at N-3 position of benzopyrimidines and studied their antitubercular, anti-HIV and antibacterial activities against selected gram positive and negative bacteria. The target compounds 1-substituted-3-(3-(3-nitrophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-ylamino) isothioureas (PTS1 – PTS15 ) were obtained by the reaction of 2-hydrazino-3-(3-nitrophenyl) benzopyrimidin-4(3 H)-one (5) with different alkyl/aryl isothiocyanates followed by methylation with dimethyl sulphate. All synthesized compounds were screened for their antitubercular, anti-HIV and antibacterial activity against selective gram positive and gram negative bacteria by agar dilution method. Among the series, compound 2-methyl-3-(3-(3-nitrophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-ylamino)-1-(3-chlorophenyl)isothiourea (PTS14) shown most potent activity against Klebsiella pneumoniae, Proteus vulgaris and Staphylococcus aureus; PTS14 exhibited the antitubercular activity at the minimum microgram of 1.56 µg/mL and anti-HIV activity at 0.96 µg/mL against HIV1 and HIV2 and offers potential for further optimization and development to new antitubercular and anti-HIV agents. The results obtained from this study confirm that the synthesized and biologically evaluated benzopyrimidines showed promising antimicrobial, antitubercular and anti-HIV activities and are new scaffolds for antimicrobial activity.

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“…This research effort is a continuation of our aims on the way to develop potent antimicrobial & antitubercular agents using the benzopyrimidine scaffold by a pharmacophore hybrid approach (Figure 1) (Meunier, 2008;Alagarsamy et al, 2016). In this research, substituted thiosemicarbazide group was placed at 2 nd position & 4-methylphenyl group was placed at 3 rd position of benzopyrimidine nucleus.…”

Section: Introductionmentioning

confidence: 99%

AntiHIV, antitubercular and antibacterial activities of novel 1-substituted-3-(3-(4-methylphenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-yl amino) isothioureas

Narendhar¹,

Chitra²,

Alagarsamy³

2019

ijrps

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In this research, substituted thiosemicarbazide group was placed at 2nd position & 4-methylphenyl group was placed at 3rd position of condensed pyrimidine nucleus. Entire prepared title analogues were examined for its antibacterial, antitubercular, & anti HIV activities against selected bacteria & virus. The target compounds 1-substituted-3-(3-(4-methylphenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-ylamino)isothioureas (TTS01 – TTS10) were synthesized from 2-hydrazino-3-(4-methylphenyl)benzopyrimidin-4(3H)-one (5) by reacting with various alkyl/aryl isothiocyanates followed by methylation with dimethyl sulphate. Among the test compounds, 2-methyl-3-(3-(4-methylphenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-ylamino)-1-(3-chlorophenyl) isothiourea (TTS09) and 2-methyl-3-(3-(4-methylphenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-yl amino)-1-(4-nitrophenyl) isothiourea (TTS06) shown most potent activity against S. epidermidis, S. Aureus, and P. vulgaris 3 µg/ml MIC. Compounds TTS06 & TTS09 exhibited the antitubercular activity with 12.5 µg/ml MIC and antiHIV activity at 9.06 and 8.56 µg/ml, respectively against HIV1 and HIV2. Thus for further optimization & development of novel antitubercular and antiHIV drugs, compounds TTS06 & TTS09 may act as a pilot derivative.

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Design, Synthesis and Antimicrobial Activities of 1-(4-Oxo-3-(4-Fluorophenyl)-3h-Quinazolin- 2-Yl)-4-(Substituted) Thiosemicarbazide Derivatives

Cited by 8 publications

References 18 publications

Case report Human urinary tract myiasis in Al-Amara city/ Iraq

Case report Human urinary tract myiasis in Al-Amara city/ Iraq

Design and Synthesis of Novel 1-substituted-3-(3-(3-nitrophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-yl amino) Isothioureas for their Anti-HIV, Antibacterial Activities, Graph Theoretical Analysis, Insilico Modeling, Prediction of Toxicity and Metabolic Studies

AntiHIV, antitubercular and antibacterial activities of novel 1-substituted-3-(3-(4-methylphenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-yl amino) isothioureas

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