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In vitro anti-plasmodial activity of new synthetic derivatives of 1-(heteroaryl)-2-((5-nitroheteroaryl)methylene) hydrazine

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Asian Pacific Journal of Tropical Medicine 2021年第3期14卷 128-138页

作者： Azar Tahghighi Akram Abouie Mehrizi Sedigheh zakeri Malaria and Vector Research Group Biotechnology Research CenterPasteur Institute of IranTehranIran department of Clinical Research Pasteur Institute of IranTehranIran

Objective:To evaluate new compounds synthesized by integrating quinoline,quinazoline,and acridine rings with the active moiety of(5-nitroheteroaryl)methylene ***:A new series of compounds(1a,1b,2a,2b,3a,and 3b)were synthesized and evaluated for cytotoxicity against COS-7 cells using the MTT *** vitro anti-plasmodial activity of the compounds was measured against CQ-sensitive(3d7)and CQ-resistant(K1)Plasmodium(P.)falciparum strains.β-hematin assay was performed to assess the inhibitory effects ofβ-hematin formation for new ***:The synthetic compounds had anti-plasmodial activity against blood-stage of 3d7[IC50=(0.328-5.483)μM]and K1[IC50=(0.622-7.746)μM]strains of ***,with no cytotoxicity against COS-7 cells in effective *** 1a,1b,and 2b were the most effective derivatives against *** 3d7 and K1 *** on theβ-hematin assay,the inhibition ofβ-hematin formation is the main mechanism of the inhibitory effect of these ***:The synthetic compounds could inhibit the erythrocytic stages of CQ-sensitive and resistant *** strains without toxicity towards mammalian *** 1b,2a,and 2b had comparable anti-plasmodial activity against both CQ-sensitive(3d7)and resistant(K1)*** *** compounds may be promising lead structures for the development of new anti-malarial drugs.

关键词： Plasmodium 5-nitroheteroaryl Hydrazine Quinoline Quinazoline Acridine

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The Inhibition Effects of Alkoxyl Thiourea derivatives toward the Growth of Isolated Oscillatoria sp. from Kenyir Lake, Terengganu

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Journal of Environmental Science and Engineering(A) 2015年第8期4卷 389-394页

作者： Nor Azman Kasan Siti Zafirah Mohamad Yusof Naqiyyu Bazz Ramli Wan M. Khairul hazlina aham.d zakeri Institute of Tropical Aquaculture (AKUATROP) University Malaysia Terengganu Kuala Terengganu 21030 Malaysia School of Fisheries and Aquaculture Science Universiti Malaysia Terengganu Kuala Terengganu 21030 Malaysia School of Fundamental Science Universiti Malaysia Terengganu Kuala Terengganu 21030 Malaysia

In controlling eutrophication phenomenon, there were conventional methods which lead to negative effects to aquatic environment. This study was aimed to investigate the usage of synthesized thiourea compounds to inhibit the growth of Oscillatoria sp. in Kenyir lake, Terengganu, Malaysia. The inhibition effects of four eco-friendly alkoxyl thiourea derivatives compounds named as N-（（4-（decyloxy）phenyl）carbamothioyl）-4-methyl benzamide, N-（（4-（decyloxy）phenyl）carbamothioyl）-4-nitro benzamide, 4-chloro-N-（（4-（decyloxy）phenyl）carbamothioyl） benzamide and N-（（4-（decyloxy）phenyl）carbamothioyl） benzamide were examined onto the growth culture of Oscillatoria sp. These compounds were tested in 30 mL of Oscillatoria sp. cultures with different concentration of 16 μg·mL-1, 18 μg·mL-1, 20 μg·mL-1, 24 μg·mL-1 and 28 μg·mL-1respectively. The treatment flasks were supplied with an aerator for 24 hours under continuous illumination at 25 ℃. Chlorophyll-a concentration were extracted to calculate the inhibition percentage of each treatment. Overall, all these compounds showed inhibition effects towards the growth of Oscillatoria sp., with the highest inhibition of 37% by N-（（4-（decyloxy）phenyl）carbamothioyl）-4-methyl benzamide at the concentration of 18μg·mL-1. The methyl group that attach to the synthesized compound may contribute to the effectiveness of the compound which act as an algae inhibitor. However, extensive studies still need to be conducted in order to investigate the mechanism on how this compound reacts with Oscillatoria sp..

关键词： Eutrophication alkoxyl thiourea Oscillatoria sp. chlorophyll-a inhibition effect.

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Randomized controlled trial of Letrozole versus Clomiphene citrate for induction of ovulation in polycystic ovarian syndrome (PCOS): A Malaysian experience

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Open Journal of Obstetrics and Gynecology 2013年第5期3卷 11-17页

作者： Nik hazlina Nik Hussain Munawwirah Ismail Murizah Mohd. Zain Pu Chan Yeu Roszaman Ramli Wan Mohd Zahiruddin Wan Mohammad department of Obstetrics and Gynaecology Hospital Sultanah Bahiyah Alor Setar Malaysia department of Obstetrics and Gynaecology International Islamic University Kuantan Malaysia School of Medical Sciences Universiti Sains Malaysia and Hospital Universiti Sains Malaysia Kelantan Malaysia

Background: The purpose of this study was to compare the effectiveness of Letrozole versus Clomiphene citrate for ovulation induction in polycystic ovarian syndrome (PCOS) with infertility. Methods: This was a prospective randomized trial involving 150 women with PCOS attending the Infertility Clinic at three hospitals in Malaysia. during the initial visit, anthropometric measurements and baseline investigations were performed. Patients were randomized to 5.0 mg Letrozole daily (75 patients) or 100 mg Clomiphene citrate daily (75 patients) from the fifth until the ninth day of menstruation. Serial transvaginal scans were performed to see the dominant follicles, endometrial thickness and number of follicles. Transvaginal scans were performed serially to look for evidence of ovulation. Results: The subjects were homogenously distributed. The difference between Letrozole and Clomiphene citrate for ovulation rate was 59 (78.7%) versus 40 (53.3%). Patients taking Letrozole exhibited a mean endometrial thickness (ET) at mid cycle of menses (day 11-d14) of9.2 mm(Sd ± 2.3) versus8.4 mm(Sd ± 2.2) for patients taking Clomiphene citrate, and these differences were statistically significant

关键词： Polycystic Ovarian Syndrome Ovulation Induction Clomiphene Citrate Letrozole

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