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BIOLOGICALLY ACTIVE 2-R-5-AMINO-1,3,4-THIADIAZOLE DERIVATIVES

机译:具有生物活性的2-R-5-AMINO-1,3,4-噻二唑衍生物

摘要

The present invention pertains to the field of medicine, more precisely to that of pharmacology, and essentially relates to biologically active synthetic diazoles that consist of 2-R-5-amino-1,3,4-thiadiazole derivatives. These substances are mainly intended for use in medical practice for treating chlamydiae-mediated viral diseases as well as diseases resulting in immunodeficiency, including malignant tumours. The purpose of the present invention is to create new chemical compounds which have a high antiviral and an anti-microbial (anti-chlamydia) activity, which stimulate the production of endogenous interferons in the organism and which also have anti-aggregating, analgesic and psycho-depressive actions. This invention involves synthesising a new group of substances that consist of 2-R-5-amino-1,3,4-thiadiazole derivatives of general formula (1) where R1 is selected from the group comprising alkyl, aryl and -CH2-CH2C(0)NH-N=CH-Z, provided that Z is aryl or piperonyl, while R2 is selected from the group comprising H and (a), provided that Y is aryl or heteroaryl. This invention further relates to general methods for producing these substances, to 4 examples of the synthesis of said substances, to the identification results of each of the 42 synthesised substances as well as to data concerning the experimental verification of the substance biological activity relative to known preparations used for the same purposes.
机译:本发明涉及医学领域,更确切地说涉及药理学领域,并且基本上涉及由2-R-5-氨基-1,3,4-噻二唑衍生物组成的生物活性合成二唑。这些物质主要用于医学实践中,以治疗衣原体介导的病毒性疾病以及导致免疫缺陷的疾病,包括恶性肿瘤。本发明的目的是创建具有高抗病毒和抗微生物(抗衣原体)活性的新化合物,其可刺激生物体中内源性干扰素的产生,并且还具有抗聚集,镇痛和抑制精神病的作用。抑郁的行为。本发明涉及合成一组新的由通式(1)的2-R-5-氨基-1,3,4-噻二唑衍生物组成的物质,其中R1选自烷基,芳基和-CH2-CH2C (0)NH-N = CH-Z,条件是Z是芳基或胡椒基,而R 2选自包括H和(a)的基团,条件是Y是芳基或杂芳基。本发明进一步涉及生产这些物质的一般方法,所述物质的4个合成实例,42种合成物质中每一种的鉴定结果,以及有关相对于已知物质的生物活性的实验验证的数据。用于相同目的的制剂。

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