این سایت در حال حاضر پشتیبانی نمی شود و امکان دارد داده های نشریات بروز نباشند
Journal of Arthropod-Borne Diseases، جلد ۱۱، شماره ۱، صفحات ۹۵-۱۰۴
عنوان فارسی
چکیده فارسی مقاله
کلیدواژه‌های فارسی مقاله
عنوان انگلیسی Synthesis and Comparison of In Vitro Leishmanicidal Activity of 5-(Nitroheteroaryl)-1, 3, 4-Thiadiazols Containing Cyclic Amine of Piperidin-4-ol at C-2 with Acyclic Amine Analogues against Iranian Strain of Leishmania major (MRHO/IR/75/ER)
چکیده انگلیسی مقاله Background: Cutaneous Leishmaniasis (CL) is endemic in many tropical and subtropical regions of the world. Due to the prolonged duration of therapy, adverse effect and resistance to current drugs in the treatment of CL, the dis­covery of novel, efficient, and safe leishmanicidal drugs is required. The aims of the present study was to synthesis of new compounds based on the active compounds of 5-(5-nitrofuran-2-yl)- and 5-(5-nitrothiophen-2-yl)-1,3,4-thia­diazole bearing the linear amino alcohol of 3-aminopropan-1-ol in the C-2 position of thiadiazole ring and evaluation of their activity against the promastigote and amastigote forms of Leishmania major . Methods: Reaction between the solution of 5-(5-nitro heteroaryl)-2-chloro-1, 3, 4-thiadiazole and piperidin-4-ol in absolute ethanol was performed and the resulting products were evaluated against promastigotes form of L. major with MTT assay and amastigote form of L. major in murine peritoneal macrophages. In addition, the toxicity of these compounds was assessed against mouse peritoneal macrophages with MTT assay. Results: New synthetic compounds 5a-b showed moderate in vitro antileishmanial activity against L. major pro­mastigotes with IC 50 values of 68.9 and 27 µM, respectively. These compounds have also demonstrated a good antiamastigote activity in terms of amastigote number per macrophage, the percentage of macrophage infectivity and infectivity index . Conclusion: Novel cyclic compounds 5a-b were synthesized and exhibited less antipromastigote and antiamastigote activity compared to linear analogues.
کلیدواژه‌های انگلیسی مقاله
نویسندگان مقاله آذر تحقیقی | azar tahghighi
faculty of pharmacy and pharmaceutical sciences research center, tehran university of medical sciences, tehran, iran

سازمان اصلی تایید شده: دانشگاه علوم پزشکی تهران (Tehran university of medical sciences)

علیرضا فرومدی | alireza foroumadi
department of biochemistry, institute of biochemistry and biophysics, university of tehran, tehran, iran

سازمان اصلی تایید شده: مرکز تحقیقات بیوشیمی و بیوفیزیک (Institute of biochemistry and biophysics)

سوسن کبودانیان اردستانی | susan kabudanian ardestani
malaria and vector research group, biotechnology research center, pasteur institute of iran, tehran, iran

سازمان اصلی تایید شده: انستیتو پاستور ایران (Pasteur institute of iran)

سید محمد امین مهدیان | seyed mohammad amin mahdian


نشانی اینترنتی http://jad.tums.ac.ir/index.php/jad/article/view/461
فایل مقاله اشکال در دسترسی به فایل - ./files/site1/rds_journals/77/article-77-429963.pdf
کد مقاله (doi)
زبان مقاله منتشر شده en
موضوعات مقاله منتشر شده
نوع مقاله منتشر شده Original Article
برگشت به: صفحه اول پایگاه   |   نسخه مرتبط   |   نشریه مرتبط   |   فهرست نشریات