Design, docking analysis, identification, and synthesis of novel 3-(((substituted phenyl) amino)methyl)-2-methylquinazolin-4(3&lt;i&gt;H&lt;/i&gt;)-one compounds to fight tuberculosis

Panneerselvam, Theivendren; Sivakumar, A.; Arumugam, S.; Joshi, Shrinivas D.

doi:10.5582/ddt.2016.01048

Cited by 4 publications

(2 citation statements)

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“…[8] Slight change at some point totally switches the activity of the compound, as for the situation, when the terminal methyl gathering of 5-(1-methyl amyl)-5-ethyl barbituric corrosive is drawn one carbon particle closer the core to structures 5-(1,3-dimethyl butyl)-5-ethyl barbituric corrosive changed over tranquilizers mesmerizing movement toward anticonvulsant. [9] 2-methyl-3-o-tolyl; 4(3H)-quinazolinone is a powerful mesmerizing specialist and other 4(3H)-quinazolinone and its subordinates have been accounted for to show pain relieving, sedative, antibacterial, anticancer, anticonvulsant, antihypertensive, mitigating, hostile to tuberculosis, [10] anticonvulsant, [11] and antioxidant, [12] diuretic, muscle relaxant, calming, against hepatitis-A virus, [13] and sedative properties. The majority of the medications utilized in the crude arrangement of medication were from the regular sources, for instance, morphine, quinine, digitalis, ergot, and atropine were gotten from plant sources and their helpful employments.…”

Section: Introductionmentioning

confidence: 99%

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2021

IJPSCR

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The objective of the paper was to design and synthesize new derivatives of ((E)-3-(5-((substitutedphenylamino) methyl)-1,3,4-thiadiazol-2-yl)-2styrylquinazolin-4(3H)-one and evaluated for their anticonvulsant potential. Materials and Methods: Various syntheses of (E)-3-(5-(substitutedaminomethyl)-1,3,4-thiadiazol-2-yl)-2-styrylquinazolin-4(3H)-one derivatives have been synthesized by reacting 2-substituted benzoxazin-4-one with (E)-2-(4-Substituedstyryl)-4H-benzo [d] [1,3]oxazin-4-one. All synthesized compounds have been characterized by the infrared, 1H-NMR, and mass spectral analysis. Proposed compounds have been evaluated for anticonvulsant potential by subcutaneous pentylenetetrazole and maximal electroshock seizure model and compared with the reference drug phenytoin and carbamazepine. Neurotoxicity study of the synthesized compounds was also performed. Results and Discussion: The anticonvulsant evaluation of synthesized compound QNM-1, QNM-2, QNM-4, QNM-6, QNM-9, QNM-11, QNM-13, and QNM-15 has shown seizure protection at 100 mg/kg dose after 30 min and 4 h, so they have good onset of action as quickly reach brain and have prolonged action reveal that compound metabolized slowly, whereas compounds QNM-7, QNM-8, and QNM-12 were moderate active and reveal that their high concentration is required to cross blood-brain barrier. Compounds QNM-3, QNM-5, QNM-10, and QNM-14 were less active. Compounds having chlorine, bromine, fluorine, and nitro in the phenyl moiety have shown good activity when attached to para group but the addition of meta and ortho group of the same may provide least active compounds and in last fluorine compounds have shown comparative less active compounds. Conclusion: The pharmacological evaluation suggests that eight synthesized compounds have shown promising anticonvulsant potential and bulkier compounds can easily penetrate BBB to exert their effect.

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Section: Introductionmentioning

confidence: 99%

Untitled

2021

IJPSCR

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“…[8] Slight change sometime completely reverse the action of the compound, as in the case, when the terminal methyl group of 5-(1-methyl amyl)-5-ethyl barbituric acid is moved one carbon atom nearer the nucleus to forms 5-(1,3-dimethyl butyl)-5-ethyl barbituric acid converted sedatives hypnotic activity toward anticonvulsant. [9] 2-methyl-3-o-tolyl; 4(3H)-quinazolinone is a potent hypnotic agent and other 4(3H)-quinazolinone and its derivatives have been reported to exhibits analgesic, anesthetic, antibacterial, anticancer, anticonvulsant, antihypertensive, anti-inflammatory, anti-tuberculosis, [10] anticonvulsant, [11] and antioxidant, [12] diuretic, muscle relaxant, sedative, anti-hepatitis-A virus, [13] and tranquilizer properties. Most of the drugs used in the primitive system of medicine were from the natural sources, for example, morphine, quinine, digitalis, ergot, and atropine were derived from plant sources and their therapeutic uses.…”

Section: Introductionmentioning

confidence: 99%

Untitled

2020

IJPBA

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Objective: The objective of the paper was to design and synthesize new derivatives of ((E)-3-(5-((substitutedphenylamino)methyl)-1,3,4-thiadiazol-2-yl)-2-styrylquinazolin-4(3H)-one and evaluated for their anticonvulsant potential. Materials and Methods: Various synthesis of (E)-3-(5-(substitutedaminomethyl)-1,3,4-thiadiazol-2-yl)-2-styrylquinazolin-4(3H)-one derivatives has been synthesized by reacting 2-substituted benzoxazin-4-one with (E)-2-(4-Substituedstyryl)-4H-benzo[d] [1,3]oxazin-4-one. All synthesized compounds have been characterized by the infrared, 1 HNMR, and mass spectral analysis. Proposed compounds have been evaluated for anticonvulsant potential by subcutaneous pentylenetetrazole and maximal electroshock seizure model and compared with the reference drug phenytoin and carbamazepine. Neurotoxicity study of the synthesized compounds was also performed. Results and Discussion: The anticonvulsant evaluation of synthesized compound QNM-1, QNM-2, QNM-4, QNM-6, QNM-9, QNM-11, QNM-13, and QNM-15 has shown seizure protection at 100 mg/kg dose after 30 min and 4 h, so they have good onset of action as quickly reach brain and have prolonged action reveal that compound metabolized slowly. Whereas compound QNM-7, QNM-8, and QNM-12 were moderate active and reveal that their high concentration is required to cross blood brain barrier. Compounds QNM-3, QNM-5, QNM-10, and QNM-14 were less active. Compounds having chlorine, bromine, fluorine, and nitro in the phenyl moiety have shown good activity when attached to para group but the addition of meta and ortho group of the same may provide least active compounds and in last fluorine compounds have shown comparative less active compounds. Conclusion: The Pharmacological evaluation suggest that eight synthesized compounds have shown promising anticonvulsant potential and bulkier compounds can easily penetrate BBB to exert their effect.

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