Suroor A Khan

Jamia Hamdard University, New Dilli, NCT, India

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Publications (49)62.11 Total impact

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    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.
    No preview · Article · Feb 2014 · American journal of pharmacology and toxicology
  • 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.
    No preview · Article · Jan 2014 · Medicinal Chemistry Research

  • No preview · Article · Jan 2014
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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.
    No preview · Article · Dec 2013 · Medicinal Chemistry Research
  • 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.
    No preview · Article · Aug 2013 · Journal of Enzyme Inhibition and Medicinal Chemistry
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    ABSTRACT: A series of thiazolidin-4-one (2a–h; 3a–h), azetidin-2-one (4a–h) and 1,3,4-oxadiazole (5a–h) derivatives of isoninicotinic acid hydrazide (INH) were synthesized in order to obtain new compounds with potential anti-inflam-matory, analgesic, ulcerogenic and lipid peroxidation activities. The structures of the new compounds were supported by their IR, 1 H-NMR and mass spectral data. All compounds were evaluated for their anti-inflammatory activity by the carrageenan-induced rat paw edema test method. Eleven of the new com-pounds, out of 32, showed very good anti-inflammatory activity in the carra-geenan-induced rat paw edema test, with significant analgesic activity in the tail immersion method together with negligible ulcerogenic action. The com-pounds, which showed less ulcerogenic action, also showed reduced malondial-dehyde content (MDA), which is one of the by-products of lipid peroxidation. The study showed that the compounds inhibited the induction of gastric mu-cosal lesions and it can be suggested from the results that their protective ef-fects may be related to inhibition of lipid peroxidation in the gastric mucosa.
    Preview · Article · Apr 2013 · Journal of the Serbian Chemical Society
  • 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.
    No preview · Article · Apr 2013 · Medicinal Chemistry Research
  • Sachin Malik · Suroor A. Khan · Priya Ahuja · Satish K. Arya
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    ABSTRACT: A series of 5-substituted-arylidene-3-substituted-benzyl-thiazolidine-2,4-dione derivatives were synthesized and studied for their glucose lowering capability against alloxan induced diabetic rats. Compounds 1(b), 1(c), 1(d), 1(e), 2(b) and 2(c) showed appreciable antidiabetic activity compared to standard drug rosiglitazone. The anisaldehyde based thiazolidinedione compounds 1(a) and 2(a) displayed very less activity than the other synthesized compounds. Interestingly, 2-methoxy group containing compound 1(d) showed highest activity.
    No preview · Article · Dec 2012 · LATIN AMERICAN JOURNAL OF PHARMACY
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    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.
    Full-text · Article · Oct 2012 · European Journal of Medicinal Chemistry
  • Darpan Kaushik · Suroor A Khan · Gita Chawla · Bibhu P Panda
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    ABSTRACT: A series of (benzamidostyryl)benzimidazole derivatives were synthesized by hydrolyzing 2-phenyl-4-(substituted)benzylidene-5-oxazolones, the azlactone precursors in an acidic medium and treating the product with substituted o-phenylenediamine (OPDA) in situ. The structures of the synthesized compounds were confirmed by spectral and elemental analyses. All synthesized compounds were screened for their in vito antimicrobial activities against some identifiable strains. Thereby, it was found that only nitro substituted benzimidazoles exhibited good to moderate antibacterial activity, while other derivatives were devoid of any antimicrobial effect.
    No preview · Article · Aug 2012 · Acta poloniae pharmaceutica
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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.
    No preview · Article · Jun 2012 · Medicinal Chemistry Research
  • Suresh Kumar · Darpan Kaushik · Sandhya Bawa · Suroor A Khan
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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.
    No preview · Article · Jan 2012 · Chemical Biology & Drug Design
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    Pooja Mullick · Suroor A. Khan · Surajpal Verma · Ozair Alam
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    ABSTRACT: A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR, (1)H NMR, (13)C NMR and mass spectral data confirmed the structure of the synthesized compounds. The derivatives of these moieties were evaluated for anticonvulsant activity by MES model and neurotoxicity by rotarod method. The synthesized compounds showed good potential for anticonvulsant activity besides this, the compounds also showed neurotoxic effect. It was observed that compounds with OCH(3) at 3,4 position of phenyl ring [5(a-I)1 showed less protection against convulsions as compared to compounds having unsubstituted phenyl ring [4(a-I)].
    Preview · Article · Jul 2011 · ChemInform
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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.
    Full-text · Article · Jul 2011 · Current Analytical Chemistry
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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.
    No preview · Article · Jun 2011 · Journal of Enzyme Inhibition and Medicinal Chemistry
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    Darpan Kaushik · Suroor A Khan
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    ABSTRACT: Insulin resistance is associated with a defect in protein tyrosine phosphorylation in the insulin signal transduction cascade. PTPase enzyme dephosphorylates the active form of insulin receptor and thus attenuates its tyrosine kinase activity, therefore the need of potent PTPase inhibitor is there with that intention the QSAR was performed. Quantitative structure-activity relationship (QSAR) has been established on a series of compounds of novel benzofuran biphenyl/naphthalene's analogs using SYSTAT (Version 7.0) software, for their protein tyrosine phosphatase (PTPase-1B) inhibitor activity, in order to understand the essential structural requirement for binding with the receptor. Among several 2D QSAR models, one for a series was selected on the basis of high correlation coefficient, least standard deviation, & high value of significance for maximum number of subject was considered. The interpreted data signify the essentiality of hydrophobic character at X in the designing of the new PTPase -1B inhibitors of naphthalene analogs but not in biphenyl derivatives as shown in earlier result. Diabetes has recognized as a genetic disorder, where glucose metabolism is altered. The ability of insulin to bring about such a dramatic reversal in the symptoms of diabetes, with a return to a 'near normal' life expectancy, led the medical community to conclude that the problems of etiology and treatment had been resolved, but these conclusions were premature, whereas insulin does return control of blood glucose level and does offset the development of ketoacidosis, it doesn't appear to rectify all of the metabolic defects identifiable in the diabetic. 1 It is thus evident that insulin therapy, as currently is not a panacea for diabetes mellitus. This realization has promoted to a great deal of research toward the development of more effective way of treating the disease and has led to the discovery of various hypoglycemic agents e.g. sulphonylurea, biguanide, recently developed glitazones. Though recently developed glitazones are also monitored for the hepatotoxic effect. Thus there is a need for better and safer hypoglycemic.
    Preview · Article · Apr 2011 · Dhaka University Journal of Pharmaceutical Sciences
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    Pooja Mullick · Suroor A. Khan · Surajpal Verma · Ozair Alam
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    ABSTRACT: A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR, 1H NMR, 13C NMR and mass spectral data confirmed the structure of the newly synthesized compounds. The derivatives of these moieties were evaluated for antimicrobial activity. Most of the synthesized compounds showed good antimicrobial activity at 200 and 100 μg/mL. Compounds showed most significant antibacterial activity against gram negative test organism Escherichia coli and most significant antifungal activity against test organisms Aspergillus niger and Candida albicans. It was observed that compounds with OCH3 at 3, 4 position of phenyl ring [5(a-l)] were more potent against microbes as compared to compounds having unsubstituted phenyl ring [4(a-l)].
    Preview · Article · Dec 2010 · ChemInform
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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.
    No preview · Article · Nov 2010 · European Journal of Medicinal Chemistry
  • 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.
    No preview · Article · Sep 2010 · Natural product research
  • Sadaf J Gilani · Suroor A Khan · Nadeem Siddiqui
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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.
    No preview · Article · Aug 2010 · Bioorganic & medicinal chemistry letters