http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
Abdul Latif,Saeed Ahmad Malik,Shafqat Saeed,Naeem Iqbal,Qamar Saeed,Khalid Ali Khan,Chen Ting,Hamed A. Ghramh 한국응용곤충학회 2019 Journal of Asia-Pacific Entomology Vol.22 No.2
Chickpea (Cicer arietinum L.) is an important source of food for people worldwide. In the current study, we studied its pollination biology with special reference to floral visitors along with their visitation rate, frequency and pollen load during 2012 and 2013. We also explored the effect of floral visitors on the capsule weight, seed weight, seed numbers and seed germination. Results revealed three bees, two wasps, five flies, one moth and three butterfly species on the flowers of chickpea. Apis dorsata, A. florea, Amegilla sp. and Eristalinus aeneus were the major species with 434–474, 223–311, 69–74 and 81–136 individuals, respectively in both years. Floral visitors differed significantly in term of visitation frequency with A. florea as the most frequent visitor (9.13–9.86 visits/flower/5 min) followed by E. aeneus (5.43–5.58 visits/flower/5 min) and A. dorsata (1.72–2.31 visits/ flower/5 min) in both years. Similarly, A. florea had statistically highest visitation rate (16.85–19.99 flowers visited/min) followed by E. aeneus (9.73–10.68 flowers visited/min). A. dorsata had significantly higher pollen load on its body (84629–85,104 pollen grains) followed by A. florea (64940–65,135 pollen grains) and Amegilla sp. (64020–65,120 pollen grains). The open-pollinated flowers had significantly higher capsule weight (0.27 ± 0.01 g), seed weight (0.18 ± 0.01 g), seed numbers (1.67 ± 0.07 seeds) and seed germination (95 ± 1.38%) as compared to flowers deprived of pollinators in cages. The results suggested A. florea, A. dorsata and E. aeneus could be effective pollinators of chickpea. Hence these three species can be properly utilized on commercial scale to increase crop yield.
Saeed, Aamer,Shahzad, Danish,Larik, Fayaz Ali,Channar, Pervaiz Ali,Mahfooz, Haroon,Abbas, Qamar,Hassan, Mubashir,Raza, Hussain,Seo, Sung-Yum,Shabir, Ghulam Bangladesh Journals Online 2017 Bangladesh journal of pharmacology Vol.12 No.2
<P><p>A series of 4-aryl-2,6-dimethyl-3,5-bis-N-(aryl)-carbamoyl-1,4-dihydropyri-dines 6a-6h were prepared by using the one-pot three component synthetic method. The target compounds 6a-6h were synthesized by reacting two molar equivalents of ketone functionality and one mole of aromatic aldehydes in ammonium acetate to obtain the desired products. The structures of newly synthesized compounds were characterized by FT-IR, 1H-NMR, 13C-NMR, and elemental analysis. All the synthesized compounds were screened for their elastase inhibition and antioxidant activity. Almost all of the com-pounds 6a-h showed good to excellent activities against elastase enzyme more than the reference drug. Compounds 6d and 6b at 0.2 ± 0.0 µM and 0.2 ± 0.0 µM were found to most potent derivatives against elastase enzyme. Compound 6a exhibited prominent free radical scavenging activity. From the results of the biological activity, we infer that some derivatives can serve as lead molecules in pharmacology.</p><p><strong>Video Clip of Methodology</strong>:</p><p>3 min 13 sec <a href='https://youtube.com/v/gPLdpGpZhR8'>Full Screen</a> <a href='https://youtube.com/watch?v=gPLdpGpZhR8'>Alternate</a></p></P>
Mahar, Jamaluddin,Saeed, Aamer,Belfield, Kevin D.,Ali Larik, Fayaz,Ali Channar, Pervaiz,Ali Kazi, Mehar,Abbas, Qamar,Hassan, Mubashir,Raza, Hussain,Seo, Sung-Yum Elsevier 2019 Bioorganic chemistry Vol.84 No.-
<P><B>Abstract</B></P> <P>A novel series of silyl-yne containing chalcone derivatives <B>5a-5j</B> was synthesized by exploiting Sonogashira coupling reaction and Claisen-Schimdt condensation reaction. The synthesized derivative were characterized by spectroscopic and elemental analysis. The selective inhibition of carbonic anhydrases is considered critical in the field of medicinal chemistry because carbonic anhydrases exits in several isoforms. Synthesized compounds were subjected to carbonic anhydrase –II assay. Except <B>5j</B>, the other derivatives exhibited better potential than standard acetazolamide. Compound <B>5e</B> was found to be potent derivative in the series with IC<SUB>50</SUB> value 0.054 ± 0.001 µM. Binding analysis revealed that most potent derivative 5e binds in the active site of CA-II and single π-π stacking interaction was observed between ring structure of ligand and Phe129 having bond length 4.90 Å. Pharmacokinetics elicited that compounds obey Lipinski’s rule and show significant drug score.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Sonogashira coupling reaction was used to synthesized novel silicon containing alkyne compounds. </LI> <LI> Synthesized compounds were evaluated against carbonic anhydrase II enzyme. </LI> <LI> Binding analysis and pharmacokinetics was explored. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Sajid-ur-Rehman,Saeed, Aamer,Saddique, Gufran,Ali Channar, Pervaiz,Ali Larik, Fayaz,Abbas, Qamar,Hassan, Mubashir,Raza, Hussain,Fattah, Tanzeela Abdul,Seo, Sung-Yum Elsevier 2018 Bioorganic & medicinal chemistry Vol.26 No.12
<P><B>Abstract</B></P> <P>To seek the new medicinal potential of sulfadiazine drug, the free amino group of sulfadiazine was exploited to obtain acyl/aryl thioureas using simple and straightforward protocol. Acyl/aryl thioureas are well recognized bioactive pharmacophore containing moieties. A new series (<B>4a</B>–<B>4j</B>) of sulfadiazine derived acyl/aryl thioureas was synthesized and characterized through spectroscopic and elemental analysis. The synthesized derivatives <B>4a</B>–<B>4j</B> were subjected to calf intestinal alkaline phosphatase (CIAP) activity. The derivative <B>4a</B>–<B>4j</B> showed better inhibition potential compared to standard monopotassium phosphate (MKP). The compound <B>4c</B> exhibited higher potential in the series with IC<SUB>50</SUB> 0.251 ± 0.012 µM (standard KH<SUB>2</SUB>PO<SUB>4</SUB> 4.317 ± 0.201 µM). Lineweaver-Burk plots revealed that most potent derivative <B>4c</B> inhibition CIAP via mixed type pathway. Pharmacological investigations showed that synthesized compounds <B>4a</B>–<B>4j</B> obey Lipinsk’s rule. ADMET parameters evaluation predicted that these molecule show significant lead like properties with minimum possible toxicity and can serve as templates in drug designing. The synthetic compounds show none mutagenic and irritant behavior. Molecular docking analysis showed that compound <B>4c</B> interacts with Asp273, His317 and Arg166 amino acid residues.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Sulfadiazine based acyl/aryl thioureas has been synthesized and were screen against calf intestinal alkaline phosphatase (CIAP). </LI> <LI> Compound <B>4c</B> was found to be potent derivative in the series. </LI> <LI> Lineweaver-Burk plots revealed mixed type of enzyme inhibition mechanism. </LI> <LI> All the derivatives <B>4a</B>–<B>4j</B> obey Lipinski’s Rule. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Larik, Fayaz Ali,Saeed, Aamer,Channar, Pervaiz Ali,Muqadar, Urooj,Abbas, Qamar,Hassan, Mubashir,Seo, Sung-Yum,Bolte, Michael S.E.C.T. [etc.] 2017 European journal of medicinal chemistry Vol.141 No.-
<P><B>Abstract</B></P> <P>A series of novel 1-pentanoyl-3-arylthioureas was designed as new mushroom tyrosinase inhibitors and free radical scavengers. The title compounds were obtained in excellent yield and characterized by FTIR, <SUP>1</SUP>H NMR, <SUP>13</SUP>C NMR and X-ray crystallography in case of compound (<B>4a</B>). The inhibitory effects on mushroom tyrosinase and DPPH were evaluated and it was observed that 1-Pentanoyl-3-(4-methoxyphenyl) thiourea (<B>4f</B>) showed tyrosinase inhibitory activity (IC<SUB>50</SUB> 1.568 ± 0.01 mM) comparable to Kojic acid (IC<SUB>50</SUB> 16.051 ± 1.27 mM). Interestingly compound <B>4f</B> exhibited higher antioxidant potential compared to other derivatives. The docking studies of synthesized 1-Pentanoyl-3-arylthioureas analogues were also carried out against tyrosinase protein (PDBID 2ZMX) to compare the binding affinities with IC<SUB>50</SUB> values. The predicted binding affinities are in good agreement with the IC<SUB>50</SUB> values as compound (<B>4f</B>) showed highest binding affinity (−7.50 kcal/mol) compared to others derivatives. The kinetic mechanism analyzed by Line-weavere Burk plots exhibited that compound (<B>4f</B>) inhibit the enzyme inhibits the tyrosinase non-competitively to form an enzyme inhibitor complex. The inhibition constants Ki calculated from Dixon plots for compound (<B>4f</B>) is 1.10 μM. It was also found from kinetic analysis that derivative <B>4f</B> irreversible enzyme inhibitor complex. It is proposed on the basis of our investigation that title compound (<B>4f</B>) may serve as lead structure for the design of more potent tyrosinase inhibitors.</P> <P><B>Highlights</B></P> <P> <UL> <LI> A small library of novel 1-Pentanoyl-3-arylthioureas (<B>4a-4j</B>) synthesized. </LI> <LI> Mushroom tyrosinase inhibition and free radical scavenging activity were evaluated. </LI> <LI> Most of the compounds show excellent activity, particularly <B>4f</B> higher than the standard. </LI> <LI> The kinetic mechanism proposed <B>4f</B> is non-competitive inhibitor of mushroom tyrosinase. </LI> <LI> Molecular docking, druglikeness, Ramachandran graph, Chemo-informatics and Lipinski's rule were studied. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Waqar Jaleel,Shafqat SAEED,Qamar Saeed,Muhammad Nadir NAQQASH,Muhammad Umair SIAL,Qurat Ul AINE,Lei YANYUAN,Zhao RUI,Yurong HE,Lihua LU 한국곤충학회 2019 Entomological Research Vol.49 No.4
Plutella xylostella is an important pest of cruciferous crops worldwide. However, information regarding the age‐stage, two‐sex life parameters of P. xylostella, which is vital for designing more effective control methods, is currently lacking. The present study reports age‐stage, two‐sex life table parameters for P. xylostella on napa cabbage (Brassica oleracea var. napa), white cabbage (B. oleracea var. capitata), and cauliflower (B. oleracea var. botrytis) under laboratory conditions at 25 ± 2°C, 50–60% relative humidity, and a 16‐h light : 8‐h dark photoperiod. The time for development from an egg to a male or female adult P. xylostella on white cabbage (mean [± SE] 41.15 ± 0.54 and 39.50 ± 0.54 days, respectively) was significantly longer than that on cauliflower and napa cabbage. Furthermore, P. xylostella fecundity on cauliflower (261.90 ± 4.53 eggs female) was significantly highest than on napa cabbage and white cabbage. Intrinsic rate of increase (r) and finite rate of increase (λ) were highest on cauliflower 0.182 day−1 and 1.199 day−1 respectively as comparison to napa cabbage and white cabbage. The highest gross reproductive rate (GRR) and net reproductive rates (R0) of P. xylostella 65.87 and 52.58 respectively on cauliflower then those of other hosts. The findings of the present study indicate that cauliflower is the most suitable cultivar (host) for the development of P. xylostella. Based on these findings, crops like cauliflower can be used as trap crops when napa cabbage and white cabbage are the main crops.
Larik, Fayaz Ali,Faisal, Muhammad,Saeed, Aamer,Channar, Pervaiz Ali,Korabecny, Jan,Jabeen, Farukh,Mahar, Ihsan Ali,Kazi, Mehar Ali,Abbas, Qamar,Murtaza, Ghulam,Khan, Gul Shahzada,Hassan, Mubashir,Seo, Academic Press 2019 Bioorganic chemistry Vol.86 No.-
<P><B>Abstract</B></P> <P>The increasing resistance of pathogens to common antibiotics, as well as the need to control urease activity to improve the yield of soil nitrogen fertilization in agricultural applications, has stimulated the development of novel classes of molecules that target urease as an enzyme. In this context, the newly developed compounds on the basis of 1-heptanoyl-3-arylthiourea family were evaluated for Jack bean urease enzyme inhibition activity to validate their role as potent inhibitors of this enzyme. 1-Heptanoyl-3-arylthioureas were obtained in excellent yield and characterized through spectral and elemental analysis. All the compounds displayed remarkable potency against urease inhibition as compared to thiourea standard. It was found that novel compounds fulfill the criteria of drug-likeness by obeying Lipinski’s rule of five. Particularly compound <B>4a</B> and <B>4c</B> can serve as lead molecules in 4D (drug designing discovery and development). Kinetic mechanism and molecular docking studies also carried out to delineate the mode of inhibition and binding affinity of the molecules.</P> <P><B>Highlights</B></P> <P> <UL> <LI> A new family of 1-heptanoyl-3-arylthioureas (<B>4a-4j</B>) was synthesized in excellent yield. </LI> <LI> The synthesized 1-heptanoyl-3-arylthiourea family were evaluated for Jack bean urease enzyme inhibition activity. </LI> <LI> Particularly compound <B>4a</B> and <B>4c</B> can serve as lead molecules in 4D (drug designing discovery and development). </LI> <LI> Kinetic mechanism and molecular docking studies also carried out to delineate the mode of inhibition and binding affinity. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Shehzadi, Syeda Aaliya,Khan, Imtiaz,Saeed, Aamer,Larik, Fayaz Ali,Channar, Pervaiz Ali,Hassan, Mubashir,Raza, Hussain,Abbas, Qamar,Seo, Sung-Yum Academic Press 2019 Bioorganic chemistry Vol.84 No.-
<P><B>Abstract</B></P> <P>An efficient one-pot four-component strategy involving aldehydes, amines, alkynes and isothiocyanates has been developed to access a novel series of thiazolidine-2-imines (<B>5a-x</B>). This process operates under the action of a cooperative catalysis composed of Cu(I) and Zn(II) delivering the desired five-membered heterocyclic compounds in good to excellent yields. Notably, this transformation avoids the use of pre-formed imines or propargylamines and proceeds <I>via</I> an intramolecular 5-<I>exo-dig</I> hydrothiolation reaction of the <I>in situ</I> formed propargyl thiourea. Furthermore, the biological application of these motifs was demonstrated in terms of their strong acetylcholinesterase (AChE) inhibitory activity where compound <B>5s</B> was identified as the lead AChE inhibitor with an IC<SUB>50</SUB> value of 0.0023 ± 0.0002 μM, 88-folds stronger inhibition than standard drug (neostigmine methyl sulphate; IC<SUB>50</SUB> = 0.203 ± 0.004 μM). Molecular docking analysis reinforced the <I>in vitro</I> biological activity results revealing the formation of several useful interactions of the potent lead with amino acid residues in the active site of the enzyme.</P> <P><B>Highlights</B></P> <P> <UL> <LI> One-pot four component methodology was developed under Cu/Zn dual catalysis. </LI> <LI> A diverse range of thiazolidin-2-imines was prepared in excellent yields. </LI> <LI> Good functional group tolerance and broad substrate scope were explored. </LI> <LI> Potent inhibitors (<B>5b</B>, <B>5i</B>, <B>5s</B>, <B>5t</B>) of acetylcholinesterase were identified. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>