Suroor A Khan

Jamia Hamdard University, New Delhi, NCT, India

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Publications (45)56 Total impact

  • [Show abstract] [Hide abstract]
    ABSTRACT: The present series of compounds were synthesized with the aim to develop newer anticonvulsant agents that are comparatively more efficacious and safer than the currently used anticonvulsant agents. Various thiazolyl coumarins were synthesized by the reaction of 3-(bromoacetyl)-2H-chromen-2-one with different substituted aryl thiourea. The structures of the synthesized compounds were confirmed by spectral data and elemental analyses. Compounds were tested for anticonvulsant activity utilizing Pen Tylenetetra Zole-induced seizure (PTZ) and Maximal Electroshock Seizure (MES) tests at 30, 100 and 300 mg kg-1 dose level. Neurotoxicity and ethanol potentiation test of the compounds were also assessed at the same dose level. Two compounds of the series 3g and 3j exhibited significant anticonvulsant activity at 30 mg kg-1 dose level with lesser neurotoxicity than the standard drug phenytoin.
    American journal of pharmacology and toxicology 01/2014; 9(2):132-138.
  • Sachin Malik, Suroor A. Khan
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    ABSTRACT: The anticonvulsant study of 25 newly synthesized quinazolin-4(3H)-one substituted 1H and 2H-tetrazoles (6a–6d, 7a–7b, 8a–8i, 8a′–8i′) was executed. The study employing the maximal electroshock and subcutaneous pentylenetetrazole (scPTZ) screens, the ‘gold standards’ in the preliminary anticonvulsant breakthrough and the neurotoxicity study applying the rotorod test unveiled a triad of compounds 6c, 7b and 8i′ as the looms amongst the compendium of synthesized compounds. The quantification data of these compounds following oral administration in rats showcased 7b to endorse a remarkable position in the MES screen with a protective indice (PI) of >39.67 and 6c in the scPTZ delineating a PI > 3.10, respectively. All the potent compounds were destitute of toxicity.
    Medicinal Chemistry Research 01/2014; · 1.61 Impact Factor
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    ABSTRACT: Malaria is the leading infectious disease found in humans, affecting third-world countries. Worldwide, more than two billion people are at risk of malaria, with about 500 million clinical cases of malaria each year and one million deaths. In this focused review, an effort has been made to summarize the reactions of singlet oxygen with organic substrates, their stereoselectivity, stereospecificity and utilization in generating dioxetanes and endoperoxides. The study of production and reactivity indications of this exceptional molecule has emerged as a rich and diverse area in the synthesis of antimalarials like artemisinin and its semisynthetic derivatives, structurally simple 1,2,4-trioxanes, sesquiterpene isonitriles, synthetic cyclic, and other acyclic peroxides. Artermisinin, a mainstay in antimalarial drug therapy, meets the dual challenge posed by drug-resistant parasites and rapid advancement of lethal malarial threat. The cardinal mechanism of peroxidation and ring closure in its production are induced by singlet oxygen and acid. Moreover, its complex structure restricts the complete chemical synthesis of artemisinin. Consequently, the limited availability coupled with increasing demand for artemisinin has paved the way for the preparation of synthetic alternatives of artemisinin and its derivatives. Likewise, past evidence of the structure–activity relationship indicate the importance of singlet oxygen in antimalarial drug synthesis. It is anticipated that this compendium on the chemistry of singlet oxygen will be of use to organic/medicinal chemists and pharmacologists working on antimalarial drug development.
    Medicinal Chemistry Research 12/2013; · 1.61 Impact Factor
  • Sachin Malik, Suroor A Khan
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    ABSTRACT: Abstract A series of novel (5-amino-3-substituted-1, 2, 4-triazin-6-yl) (2-(6-halo-substituted benzo[d]isoxazol-3-yl) pyrrolidin-1-yl) methanone 5a-5r was synthesized. Their anticonvulsant activities were evaluated by the maximal electroshock (MES) test and neurotoxicity was evaluated by the rotorod test. The MES test showed that (5-amino-3-phenyl-1, 2, 4-triazin-6-yl)(2-(6-fluorobenzo[d]isoxazol-3-yl) pyrrolidin-1-yl) methanone 5c was found to be the most potent compound with ED50 value of 6.20 mg/kg (oral/rat) and a protective index (PI = ED50/TD50) value of >48.38, which was much higher than the PI of the reference drug phenytoin. To explain the possible mechanism of action of selected derivatives 5b, 5c, 5i and 5o, their influence on sodium channel was evaluated in vitro.
    Journal of Enzyme Inhibition and Medicinal Chemistry 08/2013; · 1.50 Impact Factor
  • Journal of the Serbian Chemical Society 04/2013; · 0.91 Impact Factor
  • Sadaf J. Gilani, Suroor A. Khan
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    ABSTRACT: A series of 6-substituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole (6a–g) and 1,3,4-oxadiazole (7a–g, 8) derivatives of benzothiazole were synthesized in satisfactory yield and pharmacologically evaluated for their anti-inflammatory, analgesic, ulcerogenic, and lipid peroxidation activities by known experimental models. All the synthesized compounds were in good agreement with elemental and spectral data. Some of the synthesized compounds have significant anti-inflammatory and analgesic activities. Ulcerogenic and irritative action on the gastrointestinal mucosa, in comparison with standard are low.
    Medicinal Chemistry Research 04/2013; · 1.61 Impact Factor
  • Mohd Zaheen Hassan, Suroor A Khan, Mohd Amir
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    ABSTRACT: A series of N-(substituted benzothiazol-2-yl)amide derivatives 2a-h and 4a-h were synthesized by the EDC coupling reactions of substituted-benzothiazol-2-amine with 4-oxo-4-phenylbutanoic acid/2-benzoyl benzoic acid and evaluated for their anticonvulsant and neuroprotective effect. N-(6-methoxybenzothiazol-2-yl)-4-oxo-4-phenylbutanamide (2f) emerged as the most effective anticonvulsant with median doses of 40.96mg/kg (MES ED(50)), 85.16mg/kg (scPTZ ED(50)) and 347.6mg/kg (TD(50)). Furthermore, compound 2f displayed promising neuroprotective effect by lowering the levels of MDA and LDH; therefore, it represents a potential lead in search for safer and effective anticonvulsants having neuroprotective effects.
    European journal of medicinal chemistry 10/2012; 58C:206-213. · 3.27 Impact Factor
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    ABSTRACT: A series of quinoline-incorporated substituted thiadiazole were designed and synthesized using appropriate synthetic route keeping in view the structural requirement of pharmacophore and evaluated for anticonvulsant and CNS activities. After intraperitoneal injection to mice, some synthesized derivatives were examined in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazol (scPTZ)-induced seizure and neurotoxicity screens. Those found potent were also evaluated for behavioural impairment and depression activity. Among the compounds tested, 6d and 6e showed protection from seizures in both the animal models at dose level of 30 mg/kg while 7f showed protection against both models at 100 mg/kg dose level. These compounds exhibited lesser CNS depression and neurotoxicity compared with clinically effective drug.
    Chemical Biology &amp Drug Design 01/2012; 79(1):104-11. · 2.47 Impact Factor
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    ABSTRACT: A series of 5,6-dimethoxy-2-{1-[arylamino/alkylamino(thioxo)methyl]-4-piperidyl-methyl}-1-indanones (4a–l) were designed and synthesized by the reaction of 5,6-dimethoxy-2-(piperidin-4-yl-methyl)-indan-1-one with aryl/alkyl isothiocyanates. The anticonvulsant activity was evaluated in animal models by maximal electroshock seizure and subcutaneous pentylenetetrazole tests. The neurotoxic effects were assessed by rotorod and ethanol potentiation tests. Gamma amino butyric acid (GABA) estimation of the selected compounds was performed in rat brain utilizing UV absorbance data. Compounds 4d, 4g, and 4j displayed encouraging anticonvulsant profile against both seizure models with remarkably lower neurotoxicity. These compounds were found to increase the GABA level in rat brain significantly.
    Medicinal Chemistry Research 01/2012; · 1.61 Impact Factor
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    ABSTRACT: A variety of thiadiazolyliminothiazolidinone derivatives (IX) and (XI) are synthesized, which show good potential for anticonvulsant activity and also neurotoxic effect.
    ChemInform 07/2011; 42(29).
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    ABSTRACT: In this study, a series of novel 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole (6a-g) and 1,3,4-oxadiazole (7a-g, 8) were synthesized from N-(6-chlorobenzo[d]thiazol-2-yl) hydrazine carboxamide derivatives of benzothiazole class. Antimicrobial properties of the title compound derivatives were investigated against one Gram (+) bacteria (Staphylococcus aureus), three Gram (-) bacteria (Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae) and five fungi (Candida albicans, Aspergillus niger, Aspergillus flavus, Monascus purpureus and Penicillium citrinum) using serial plate dilution method. The investigation of antibacterial and antifungal screening data revealed that all the tested compounds showed moderate to good inhibition at 12.5-100 µg/mL in DMSO. It has been observed that triazolo-thiadiazole derivatives are found to be more active than 1,3,4-oxadiazole derivatives against all pathogenic bacterial and fungal strains.
    Journal of Enzyme Inhibition and Medicinal Chemistry 06/2011; 26(3):332-40. · 1.50 Impact Factor
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    ABSTRACT: A new high-performance thin-layer chromatographic (HPTLC) method has been established for determination of mycophenolate mofetil in human plasma. Mycophenolate mofetil is used as an important immunosuppressive agent. Chromatographic separation was performed on aluminium plates coated with silica gel 60F 254 ; the mobile phase was a combination of triethylamine buffer (pH 5.3) and acetonitrile in the ratio of 20:80 (v/v) respectively. Densitometric analy-sis of mycophenolate mofetil was performed at 250 nm. The method was rapid (single-step extraction with acetonitrile), sensitive (limit of quantification 15.4 ng per zone), precise (CV 3.71 %), accurate (drug recovery 95.08-100.6%), and linear over the range 100-1200 ng per zone. Recovery of mycophenolate mofetil from plasma samples was 95.8 ± 4.5%. The half-life of mycophenolate mofetil in plasma was 20.4 h at 4°C and 17.8 h at 20°C. Mycophenolate mofetil is stable in human plasma for at least two months at -20°C and can tolerate two freeze-thaw cycles with losses <10%. The method was successfully used to determine therapeutic levels of mycophenolate mofetil.
    Current Analytical Chemistry 01/2011; 700. · 1.56 Impact Factor
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    ABSTRACT: A series of 24 title compounds of type (IX) is prepared and tested in vitro against various bacterial and fungal strains.
    ChemInform 12/2010; 41(52).
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    ABSTRACT: A number of 5-(4-substituted phenyl)-2-(substituted benzylsulfanyl)-4-(substituted phenyl)-6-methyl-1,4-dihydro-5-pyrimidine carboxamides (1-30) were designed and synthesized keeping in view the structural requirements as suggested in the pharmacophore model for antihypertensive activity. All the synthesized compounds were tested for antihypertensive activity by non-invasive blood pressure (NIBP) measurements (tail-cuff method) in rats. Almost all the tested compounds displayed considerable decrease in the blood pressure as compared to control. Thirteen compounds showed significant antihypertensive activity comparable to the standard drug nifedipine.
    European journal of medicinal chemistry 11/2010; 45(11):5113-9. · 3.27 Impact Factor
  • Sunita Rani, Suroor A Khan, M Ali
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    ABSTRACT: Phytochemical investigation of the seeds of Althea officinalis L. (Malvaceae) led to the isolation of three new phytoconstituents, identified as n-hexacos-2-enyl-1,5-olide (altheahexacosanyl lactone), 2beta-hydroxycalamene (altheacalamene) and 5,6-dihydroxycoumarin-5-dodecanoate-6beta-D-glucopyranoside (altheacoumarin glucoside), along with the known phytoconstituents lauric acid, beta-sitosterol and lanosterol. The structures of these compounds were established on the basis of spectral analysis and chemical reactions.
    Natural product research 09/2010; 24(14):1358-64. · 1.01 Impact Factor
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    ABSTRACT: The significance of this study was to prepare various isoniazid derivatives by introducing the isoniazid core into several molecules to explore the possibilities of some altered biological activities. Series of 6-substituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole (3a-g) and 1,3,4-oxadiazole (4a-g and 5) derivatives of isoniazid were synthesized in satisfactory yield and pharmacologically evaluated for their anti-inflammatory, analgesic, ulcerogenic, and lipid peroxidation activities by known experimental models.
    Bioorganic & medicinal chemistry letters 08/2010; 20(16):4762-5. · 2.65 Impact Factor
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    ABSTRACT: A series of 4-thiazolidinones bearing a sulfonamide group (4a-w) were prepared by cyclizing various 5-bromo-2-methoxy-N'-[(1E)-arylmethylene/arylethylidene]benzenesulfonohydrazides. All the compounds were characterized by IR, (1)H NMR, and elemental analysis. The compounds were tested for their anticonvulsant activity utilizing MES and scPTZ animal models. The majority of the compounds exhibited significant activity against both animal models; however, compounds 4c, 4m, and 4o displayed promising activity and could be considered as leads for further investigations.
    Journal of Enzyme Inhibition and Medicinal Chemistry 03/2010; 25(4):485-91. · 1.50 Impact Factor
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    ABSTRACT: A number of N-(4,6-substituted diphenylpyrimidin-2-yl) semicarbazones (4a-t) were synthesized and tested for their anticonvulsant activity against the two seizure models, maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ). All the synthesized compounds possessed the four essential pharmacophoric elements for good anticonvulsant activity. Most of the compounds displayed good anticonvulsant activity with lesser neurotoxicity. To assess the unwanted effects of the compounds on liver, estimation of enzymes and proteins was carried out.
    European journal of medicinal chemistry 02/2010; 45(6):2467-72. · 3.27 Impact Factor
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    ABSTRACT: A novel HPTLC method has been developed and validated for quantitative determination of omeprazole (OPZ) in capsule dosage form. The method was validated according to the International Conference on Harmonization guidelines for accuracy, precision, linearity, specificity, and robustness. HPTLC aluminum sheets precoated with silica gel 60F24 were used as the stationary phase and chloroform-methanol (9 + 1) as the mobile phase. The mobile phase was found to give compact bands for OPZ (Rf value of 0.39 +/- 0.12) in densitometric analysis in the absorbance mode at 302 nm. The linear regression analysis data for the calibration plots showed good linearity (r2 = 0.997) with respect to peak area in the concentration range 50-3000 ng/band. The mean values of the slope and intercept were 9.896 +/- 0.0753 and 1870.761 +/- 16.866, respectively. The method was also applied for stability testing of OPZ in different stress conditions and found to be accurate, linear, precise, robust, specific, and stability indicating. The method proposed can be used for QC and stability testing of different dosage forms such as tablets and capsules, as well as for bulk drug analysis of OPZ.
    Journal of AOAC International 01/2010; 93(3):787-91. · 1.23 Impact Factor
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    Acta poloniae pharmaceutica 01/2010; 67(4):429-37. · 0.67 Impact Factor